Achillion Pharmaceuticals, Inc.

United States of America

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IPC Class
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings 74
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings 73
C07D 471/04 - Ortho-condensed systems 66
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings 45
C07D 513/04 - Ortho-condensed systems 45
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05 - Pharmaceutical, veterinary and sanitary products 5
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1.

HETEROARYL COMPOUNDS FOR TREATMENT OF COMPLEMENT FACTOR D MEDIATED DISORDERS

      
Application Number 17800013
Status Pending
Filing Date 2021-02-19
First Publication Date 2025-06-19
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Wiles, Jason Allan
  • Gadhachanda, Venkat Rao

Abstract

Compounds, methods of use, and processes for making inhibitors of complement factor D or a pharmaceutically acceptable salt or composition thereof are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade. The inhibitors of factor D described herein reduce the excessive activation of complement.

IPC Classes  ?

  • C07D 487/04 - Ortho-condensed systems
  • A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
  • A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • A61K 31/5386 - 1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 471/04 - Ortho-condensed systems
  • C07D 498/20 - Spiro-condensed systems
  • C07D 513/04 - Ortho-condensed systems
  • C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or

2.

PHARMACEUTICAL COMPOUNDS FOR THE TREATMENT OF COMPLEMENT MEDIATED DISORDERS

      
Application Number 18027506
Status Pending
Filing Date 2021-09-22
First Publication Date 2025-05-29
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Wiles, Jason Allan
  • Gadhachanda, Venkat Rao
  • Onyango, Evans O.

Abstract

This disclosure provides pharmaceutical compounds to treat medical disorders, such as complement-mediated disorders, including complement C1-mediated disorders.

IPC Classes  ?

  • C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
  • A61K 31/4025 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
  • A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
  • A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
  • A61K 31/426 - 1,3-Thiazoles
  • A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
  • A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
  • C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 471/04 - Ortho-condensed systems
  • C07D 487/08 - Bridged systems
  • C07D 491/107 - Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
  • C07D 491/113 - Spiro-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring

3.

THERAPEUTIC REGIMENS FOR TREATMENT OF PAROXYSMAL NOCTURNAL HEMOGLOBINURIA

      
Application Number 18784478
Status Pending
Filing Date 2024-07-25
First Publication Date 2025-01-30
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Huang, Mingjun
  • Patel, Dharaben
  • Podos, Steven D.

Abstract

Provided herein are methods for treating a subject with PNH comprising administering to a subject a therapeutically effective amount of complement component C5 (C5) inhibitor, complement component C3 (C3) inhibitor, or complement factor B (CFB) inhibitor in combination with a therapeutically effective amount of small molecule complement factor D (CFD) inhibitor of Formula I or Formula II, or a pharmaceutically acceptable salt thereof.

IPC Classes  ?

  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61K 39/00 - Medicinal preparations containing antigens or antibodies
  • A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
  • A61P 7/00 - Drugs for disorders of the blood or the extracellular fluid
  • C07K 16/18 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans

4.

Aryl, heteroaryl, and heterocyclic compounds for treatment of immune and inflammatory disorders

      
Application Number 18418560
Grant Number 12338230
Status In Force
Filing Date 2024-01-22
First Publication Date 2024-06-20
Grant Date 2025-06-24
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Wiles, Jason Allan
  • Phadke, Avinash S.
  • Deshpande, Milind
  • Agarwal, Atul
  • Chen, Dawei
  • Gadhachanda, Venkat Rao
  • Hashimoto, Akihiro
  • Pais, Godwin
  • Wang, Qiuping
  • Wang, Xiangzhu
  • Greenlee, William

Abstract

Compounds, methods of use, and processes for making inhibitors of complement Factor D are provided comprising Formula I, I″ and I′″ or a pharmaceutically acceptable salt or composition thereof. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduces the excessive activation of complement.

IPC Classes  ?

  • C07D 407/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
  • A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
  • A61P 37/00 - Drugs for immunological or allergic disorders
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • C07D 403/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing aromatic rings
  • C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
  • C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 471/04 - Ortho-condensed systems
  • C07D 487/04 - Ortho-condensed systems
  • C07D 487/22 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups in which the condensed system contains four or more hetero rings
  • C07D 493/04 - Ortho-condensed systems
  • C07D 513/04 - Ortho-condensed systems
  • C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
  • C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system

5.

Macrocyclic compounds for treatment of medical disorders

      
Application Number 18196002
Grant Number 12297205
Status In Force
Filing Date 2023-05-11
First Publication Date 2024-02-22
Grant Date 2025-05-13
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Wiles, Jason Allan
  • Phadke, Avinash S.
  • Chen, Dawei
  • Gadhachanda, Venkat Rao
  • Barrish, Joel Charles
  • Agarwal, Atul
  • Eastman, Kyle J.

Abstract

Macrocyclic Complement Factor D inhibitors, pharmaceutical compositions, and uses thereof, as well as processes for their manufacture are provided. The compounds provided include Formula I, Formula II, Formula III, Formula IV, Formula V, Formula VI, Formula VII, and Formula VIII or a pharmaceutically acceptable salt, prodrug, isotopic analog, N-oxide, or isolated isomer thereof, optionally in a pharmaceutically acceptable composition. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade.

IPC Classes  ?

  • C07D 487/08 - Bridged systems
  • A61P 7/00 - Drugs for disorders of the blood or the extracellular fluid
  • A61P 7/02 - Antithrombotic agentsAnticoagulantsPlatelet aggregation inhibitors
  • A61P 31/12 - Antivirals
  • C07D 487/18 - Bridged systems
  • C07D 498/08 - Bridged systems
  • C07D 513/08 - Bridged systems
  • C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or

6.

Aryl, heteroaryl, and heterocyclic pharmaceutical compounds for treatment of medical disorders

      
Application Number 18196128
Grant Number 12162860
Status In Force
Filing Date 2023-05-11
First Publication Date 2023-11-09
Grant Date 2024-12-10
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Wiles, Jason Allan
  • Phadke, Avinash S.
  • Deshpande, Milind
  • Agarwal, Atul
  • Chen, Dawei
  • Gadhachanda, Venkat Rao
  • Hashimoto, Akihiro
  • Pais, Godwin
  • Wang, Qiuping
  • Wang, Xiangzhu
  • Barrish, Joel Charles
  • Greenlee, William
  • Eastman, Kyle J.

Abstract

Complement Factor D inhibitors, pharmaceutical compositions, and uses thereof, as well as processes for their manufacture are provided. The compounds provided include Formula I, Formula II, Formula III, Formula IV, and Formula V, or a pharmaceutically acceptable salt, prodrug, isotopic analog, N-oxide, or isolated isomer thereof, optionally in a pharmaceutically acceptable composition. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade.

IPC Classes  ?

  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 471/04 - Ortho-condensed systems
  • C07D 471/08 - Bridged systems
  • C07D 491/107 - Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
  • C07D 498/10 - Spiro-condensed systems
  • C07F 5/02 - Boron compounds

7.

Aryl, heteroaryl, and heterocyclic compounds for treatment of medical disorders

      
Application Number 18124427
Grant Number 12139497
Status In Force
Filing Date 2023-03-21
First Publication Date 2023-09-14
Grant Date 2024-11-12
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Wiles, Jason Allan
  • Phadke, Avinash S.
  • Deshpande, Milind
  • Agarwal, Atul
  • Chen, Dawei
  • Gadhachanda, Venkat Rao
  • Hashimoto, Akihiro
  • Pais, Godwin
  • Wang, Qiuping
  • Wang, Xiangzhu

Abstract

Compounds, methods of use, and processes for making inhibitors of complement Factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is an aryl, heteroaryl or heterocycle (R32) are provided. The inhibitors of Factor D described herein reduce the excessive activation of complement.

IPC Classes  ?

  • C07D 513/04 - Ortho-condensed systems
  • A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
  • A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
  • A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
  • A61K 31/416 - 1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
  • A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
  • A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
  • A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • A61K 38/00 - Medicinal preparations containing peptides
  • A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
  • A61P 3/06 - Antihyperlipidemics
  • A61P 9/00 - Drugs for disorders of the cardiovascular system
  • A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
  • A61P 11/00 - Drugs for disorders of the respiratory system
  • A61P 13/00 - Drugs for disorders of the urinary system
  • A61P 13/02 - Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
  • A61P 17/00 - Drugs for dermatological disorders
  • A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
  • A61P 21/00 - Drugs for disorders of the muscular or neuromuscular system
  • A61P 25/00 - Drugs for disorders of the nervous system
  • A61P 25/02 - Drugs for disorders of the nervous system for peripheral neuropathies
  • A61P 27/00 - Drugs for disorders of the senses
  • A61P 27/02 - Ophthalmic agents
  • A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
  • A61P 37/02 - Immunomodulators
  • A61P 43/00 - Drugs for specific purposes, not provided for in groups
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
  • C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 417/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 471/04 - Ortho-condensed systems
  • C07D 487/04 - Ortho-condensed systems
  • C07D 493/04 - Ortho-condensed systems
  • C07D 495/04 - Ortho-condensed systems

8.

OCULAR DRUG DEPOT FOR COMPLEMENT-MEDIATED DISORDERS

      
Application Number 17909228
Status Pending
Filing Date 2021-03-09
First Publication Date 2023-04-27
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Huang, Mingjun
  • Zelenkofske, Steven
  • Boyer, David
  • Rivera, Jose
  • Wiles, Jason Allan

Abstract

This disclosure provides an ocular tissue depot of a selected complement factor D (CFD) inhibitor for the extended treatment of an ocular disorder mediated by complement factor D. In particular, the disclosure includes the creation of a drug depot within the choroid-retina pigmented epithelium (C-RPE) and/or the iris-ciliary body (I-CB) of the eye by means of the systemic (oral or parenteral) administration of the compound, where the compound accumulates in ocular tissue and is released over an extended period for the treatment of a posterior and/or anterior eye disorder.

IPC Classes  ?

  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61P 27/02 - Ophthalmic agents

9.

Morphic forms of danicopan

      
Application Number 17272924
Grant Number 11814363
Status In Force
Filing Date 2019-09-06
First Publication Date 2023-03-30
Grant Date 2023-11-14
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Phadke, Avinash
  • Hashimoto, Akihiro
  • Ma, Wei
  • Katrincic, Lee M.

Abstract

This invention provides stable, highly crystalline forms of Complement factor D inhibitors Compound 1 for advantageous therapeutic pharmaceutical efficacy and dosage form stability.

IPC Classes  ?

  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings

10.

PHARMACEUTICAL COMPOUNDS FOR THE TREATMENT OF COMPLEMENT MEDIATED DISORDERS

      
Application Number 17440665
Status Pending
Filing Date 2020-03-20
First Publication Date 2023-03-16
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Wiles, Jason Allan
  • Gadhachanda, Venkat Rao
  • Eastman, Kyle J.

Abstract

This disclosure provides pharmaceutical compounds to treat medical disorders, such as complement-mediated disorders, including complement Cl-mediated disorders.

IPC Classes  ?

  • C07D 491/113 - Spiro-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
  • C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 207/16 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
  • C07D 333/38 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
  • C07F 7/08 - Compounds having one or more C—Si linkages
  • C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
  • C07D 471/08 - Bridged systems

11.

Pharmaceutical compounds for treatment of medical disorders

      
Application Number 17872104
Grant Number 12006307
Status In Force
Filing Date 2022-07-25
First Publication Date 2023-03-09
Grant Date 2024-06-11
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Wiles, Jason Allan
  • Phadke, Avinash S.
  • Deshpande, Milind
  • Agarwal, Atul
  • Chen, Dawei
  • Gadhachanda, Venkat Rao
  • Hashimoto, Akihiro
  • Pais, Godwin
  • Wang, Qiuping
  • Wang, Xiangzhu
  • Barrish, Joel Charles
  • Greenlee, William
  • Eastman, Kyle J.

Abstract

Complement Factor D inhibitors, pharmaceutical compositions, and uses thereof, as well as processes for their manufacture are provided. The compounds provided include Formula I, Formula II, Formula III, and Formula IV or a pharmaceutically acceptable salt, prodrug, isotopic analog, N-oxide, or isolated isomer thereof, optionally in a pharmaceutically acceptable composition. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade.

IPC Classes  ?

  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 403/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing aromatic rings
  • C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
  • C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 471/04 - Ortho-condensed systems
  • C07D 493/04 - Ortho-condensed systems
  • C07D 495/04 - Ortho-condensed systems
  • C07D 513/04 - Ortho-condensed systems
  • C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system

12.

PHARMACEUTICAL COMPOUNDS FOR THE TREATMENT OF COMPLEMENT FACTOR D MEDICAL DISORDERS

      
Application Number 17267362
Status Pending
Filing Date 2019-08-20
First Publication Date 2023-01-26
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Wiles, Jason Allan
  • Gadhachanda, Venkat Rao
  • Eastman, Kyle J.
  • Pais, Godwin

Abstract

Compounds, methods of use, and processes for making inhibitors of complement factor D or a pharmaceutically acceptable salt or composition thereof are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade. The inhibitors of factor D described herein reduce the excessive activation of complement.

IPC Classes  ?

  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 491/052 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
  • C07D 471/04 - Ortho-condensed systems
  • C07D 487/04 - Ortho-condensed systems
  • C07D 451/02 - Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.02,4] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamineCyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.02,4] nonane ring systems, e.g. tropaneCyclic acetals thereof
  • C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
  • C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or

13.

Aryl, heteroaryl, and heterocyclic pharmaceutical compounds for treatment of medical disorders

      
Application Number 17366670
Grant Number 11708351
Status In Force
Filing Date 2021-07-02
First Publication Date 2022-12-15
Grant Date 2023-07-25
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Wiles, Jason Allan
  • Phadke, Avinash S.
  • Deshpande, Milind
  • Agarwal, Atul
  • Chen, Dawei
  • Gadhachanda, Venkat Rao
  • Hashimoto, Akihiro
  • Pais, Godwin
  • Wang, Qiuping
  • Wang, Xiangzhu
  • Barrish, Joel Charles
  • Greenlee, William
  • Eastman, Kyle J.

Abstract

Complement Factor D inhibitors, pharmaceutical compositions, and uses thereof, as well as processes for their manufacture are provided. The compounds provided include Formula I, Formula II, Formula III, Formula IV, and Formula V, or a pharmaceutically acceptable salt, prodrug, isotopic analog, N-oxide, or isolated isomer thereof, optionally in a pharmaceutically acceptable composition. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade.

IPC Classes  ?

  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 471/04 - Ortho-condensed systems
  • C07D 471/08 - Bridged systems
  • C07D 491/107 - Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
  • C07D 498/10 - Spiro-condensed systems
  • C07F 5/02 - Boron compounds

14.

Macrocyclic compounds for the treatment of medical disorders

      
Application Number 17272923
Grant Number 11814391
Status In Force
Filing Date 2019-09-06
First Publication Date 2022-12-01
Grant Date 2023-11-14
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Wiles, Jason Allan
  • Gadhachanda, Venkat Rao
  • Eastman, Kyle J.
  • Pais, Godwin

Abstract

Compounds, methods of use, and processes for making inhibitors of complement factor D or a pharmaceutically acceptable salt or composition thereof are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade. The inhibitors of factor D described herein reduce excessive activation of complement.

IPC Classes  ?

  • C07D 471/16 - Peri-condensed systems
  • C07D 487/08 - Bridged systems
  • C07D 487/18 - Bridged systems
  • C07D 498/18 - Bridged systems
  • C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
  • A61K 31/4162 - 1,2-Diazoles condensed with heterocyclic ring systems
  • A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
  • A61P 37/00 - Drugs for immunological or allergic disorders

15.

Aryl, heteroaryl, and heterocyclic compounds for treatment of immune and inflammatory disorders

      
Application Number 17835098
Grant Number 11926617
Status In Force
Filing Date 2022-06-08
First Publication Date 2022-10-06
Grant Date 2024-03-12
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Wiles, Jason Allan
  • Phadke, Avinash S.
  • Deshpande, Milind
  • Agarwal, Atul
  • Chen, Dawei
  • Gadhachanda, Venkat Rao
  • Hashimoto, Akihiro
  • Pais, Godwin
  • Wang, Qiuping
  • Wang, Xiangzhu
  • Greenlee, William

Abstract

Compounds, methods of use, and processes for making inhibitors of complement Factor D are provided comprising Formula I, I″ and I′″ or a pharmaceutically acceptable salt or composition thereof. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduces the excessive activation of complement.

IPC Classes  ?

  • C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 471/04 - Ortho-condensed systems
  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
  • C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 487/04 - Ortho-condensed systems
  • C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
  • C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 407/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 403/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing aromatic rings
  • C07D 513/04 - Ortho-condensed systems
  • C07D 487/22 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups in which the condensed system contains four or more hetero rings
  • A61P 37/00 - Drugs for immunological or allergic disorders
  • A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
  • A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
  • C07D 493/04 - Ortho-condensed systems

16.

PHARMACEUTICAL COMPOUNDS FOR THE TREATMENT OF COMPLEMENT MEDIATED DISORDERS

      
Application Number US2021051559
Publication Number 2022/066774
Status In Force
Filing Date 2021-09-22
Publication Date 2022-03-31
Owner ACHILLION PHARMACEUTICALS, INC. (USA)
Inventor
  • Wiles, Jason Allan
  • Gadhachanda, Venkat Rao
  • Onyango, Evans O.

Abstract

This disclosure provides pharmaceutical compounds to treat medical disorders, such as complement-mediated disorders, including complement C1-mediated disorders.

IPC Classes  ?

  • A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
  • A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
  • A61K 31/4025 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
  • C07D 207/04 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
  • C07D 333/30 - Hetero atoms other than halogen
  • C07D 333/36 - Nitrogen atoms

17.

Targeted dosing for the treatment of complement mediated disorders

      
Application Number 17414057
Grant Number 12239645
Status In Force
Filing Date 2019-12-17
First Publication Date 2022-03-17
Grant Date 2025-03-04
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Huang, Mingjun
  • Podos, Steven D.

Abstract

max, providing additional safety margin and better dosing flexibility.

IPC Classes  ?

  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61P 7/06 - Antianaemics

18.

Macrocyclic compounds for treatment of medical disorders

      
Application Number 17314155
Grant Number 11718626
Status In Force
Filing Date 2021-05-07
First Publication Date 2021-09-30
Grant Date 2023-08-08
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Wiles, Jason Allan
  • Phadke, Avinash S.
  • Chen, Dawei
  • Gadhachanda, Venkat Rao
  • Barrish, Joel Charles
  • Agarwal, Atul
  • Eastman, Kyle J.

Abstract

Macrocyclic Complement Factor D inhibitors, pharmaceutical compositions, and uses thereof, as well as processes for their manufacture are provided. The compounds provided include Formula I, Formula II, Formula III, Formula IV, Formula V, Formula VI, Formula VII, and Formula VIII or a pharmaceutically acceptable salt, prodrug, isotopic analog, N-oxide, or isolated isomer thereof, optionally in a pharmaceutically acceptable composition. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade.

IPC Classes  ?

19.

OCULAR DRUG DEPOT FOR COMPLEMENT-MEDIATED DISORDERS

      
Application Number US2021021563
Publication Number 2021/183555
Status In Force
Filing Date 2021-03-09
Publication Date 2021-09-16
Owner ACHILLION PHARMACEUTICALS, INC. (USA)
Inventor
  • Huang, Mingjun
  • Zelenkofske, Steven
  • Boyer, David
  • Rivera, Jose
  • Wiles, Jason

Abstract

This disclosure provides an ocular tissue depot of a selected complement factor D (CFD) inhibitor for the extended treatment of an ocular disorder mediated by complement factor D. In particular, the disclosure includes the creation of a drug depot within the choroid-retina pigmented epithelium (C-RPE) and/or the iris-ciliary body (I-CB) of the eye by means of the systemic (oral or parenteral) administration of the compound, where the compound accumulates in ocular tissue and is released over an extended period for the treatment of a posterior and/or anterior eye disorder.

IPC Classes  ?

  • C07D 513/04 - Ortho-condensed systems
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 471/04 - Ortho-condensed systems

20.

HETEROARYL COMPOUNDS FOR TREATMENT OF COMPLEMENT FACTOR D MEDIATED DISORDERS

      
Application Number US2021018871
Publication Number 2021/168320
Status In Force
Filing Date 2021-02-19
Publication Date 2021-08-26
Owner ACHILLION PHARMACEUTICALS, INC. (USA)
Inventor
  • Wiles, Jason, Allan
  • Gadhachanda, Venkat, Rao

Abstract

Compounds, methods of use, and processes for making inhibitors of complement factor D or a pharmaceutically acceptable salt or composition thereof are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade. The inhibitors of factor D described herein reduce the excessive activation of complement.

IPC Classes  ?

  • C07H 21/02 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with ribosyl as saccharide radical
  • C07H 21/04 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with deoxyribosyl as saccharide radical

21.

COMPLEMENT ALTERNATIVE PATHWAY-ASSOCIATED NEPHROPATHY BIOMARKERS

      
Application Number 17058547
Status Pending
Filing Date 2019-05-28
First Publication Date 2021-07-15
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Huang, Mingjun
  • Podos, Steven D.
  • Yang, Wengang
  • Zhao, Yongsen

Abstract

Provided herein are methods for using determinative urinary biomarkers for identifying a human subject suffering from an alternative pathway (AP)-associated nephropathy. Also provided herein is a method for using determinative urinary biomarkers to determine whether a human subject suffering from a complement mediated nephropathy is likely to respond to an inhibitor of the alternative complement pathway (“AP”) in treating the complement mediated nephropathy. Further provided herein is a method for using urinary biomarkers to assess the therapeutic response of a human subject suffering from an AP-associated nephropathy receiving inhibitors of the complement alternative pathway (AP inhibitors).

IPC Classes  ?

  • G01N 33/68 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving proteins, peptides or amino acids
  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine

22.

Amino compounds for treatment of immune and inflammatory disorders

      
Application Number 17135184
Grant Number 11649223
Status In Force
Filing Date 2020-12-28
First Publication Date 2021-04-29
Grant Date 2023-05-16
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Wiles, Jason Allan
  • Phadke, Avinash S.
  • Deshpande, Milind
  • Agarwal, Atul
  • Chen, Dawei
  • Gadhachanda, Venkat Rao
  • Hashimoto, Akihiro
  • Pais, Godwin
  • Wang, Qiuping
  • Wang, Xiangzhu
  • Greenlee, William

Abstract

Compounds, methods of use, and processes for making inhibitors of complement Factor D are provided comprising Formula I, I″ and I′″ or a pharmaceutically acceptable salt or composition thereof. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduces the excessive activation of complement.

IPC Classes  ?

  • A61K 31/416 - 1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
  • A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
  • A61K 31/5025 - PyridazinesHydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
  • C07D 231/56 - BenzopyrazolesHydrogenated benzopyrazoles
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 471/04 - Ortho-condensed systems
  • C07D 487/04 - Ortho-condensed systems
  • A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
  • A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
  • A61P 27/02 - Ophthalmic agents
  • C07D 495/04 - Ortho-condensed systems
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • C07D 209/12 - Radicals substituted by oxygen atoms
  • C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 513/04 - Ortho-condensed systems
  • C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
  • C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links

23.

Amide compounds for treatment of immune and inflammatory disorders

      
Application Number 17134909
Grant Number 11649229
Status In Force
Filing Date 2020-12-28
First Publication Date 2021-04-22
Grant Date 2023-05-16
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Wiles, Jason Allan
  • Phadke, Avinash S.
  • Deshpande, Milind
  • Agarwal, Atul
  • Chen, Dawei
  • Gadhachanda, Venkat Rao
  • Hashimoto, Akihiro
  • Pais, Godwin
  • Wang, Qiuping
  • Wang, Xiangzhu
  • Greenlee, William

Abstract

Compounds, methods of use, and processes for making inhibitors of complement Factor D are provided comprising Formula I, I″ and I′″ or a pharmaceutically acceptable salt or composition thereof. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduces the excessive activation of complement.

IPC Classes  ?

  • A61K 31/416 - 1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
  • A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
  • A61K 31/5025 - PyridazinesHydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
  • C07D 231/56 - BenzopyrazolesHydrogenated benzopyrazoles
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 471/04 - Ortho-condensed systems
  • C07D 487/04 - Ortho-condensed systems
  • A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
  • A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
  • A61P 27/02 - Ophthalmic agents
  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
  • C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 513/04 - Ortho-condensed systems
  • C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system

24.

PHARMACEUTICAL COMPOUNDS FOR THE TREATMENT OF COMPLEMENT MEDIATED DISORDERS

      
Application Number US2020024017
Publication Number 2020/198062
Status In Force
Filing Date 2020-03-20
Publication Date 2020-10-01
Owner ACHILLION PHARMACEUTICALS, INC. (USA)
Inventor
  • Wiles, Jason, Allan
  • Gadhachanda, Venkat, Rao
  • Eastman, Kyle, J.

Abstract

This disclosure provides pharmaceutical compounds to treat medical disorders, such as complement-mediated disorders, including complement Cl -mediated disorders.

IPC Classes  ?

  • A61K 31/401 - ProlineDerivatives thereof, e.g. captopril
  • A61K 31/4025 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
  • C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • A61P 37/00 - Drugs for immunological or allergic disorders

25.

Aryl, heteroaryl, and heterocyclic compounds for treatment of immune and inflammatory disorders

      
Application Number 16867475
Grant Number 11407738
Status In Force
Filing Date 2020-05-05
First Publication Date 2020-08-20
Grant Date 2022-08-09
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Wiles, Jason Allan
  • Phadke, Avinash S.
  • Deshpande, Milind
  • Agarwal, Atul
  • Chen, Dawei
  • Gadhachanda, Venkat Rao
  • Hashimoto, Akihiro
  • Pais, Godwin
  • Wang, Qiuping
  • Wang, Xiangzhu
  • Greenlee, William

Abstract

Compounds, methods of use, and processes for making inhibitors of complement Factor D are provided comprising Formula I, I″ and I′″ or a pharmaceutically acceptable salt or composition thereof. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduces the excessive activation of complement.

IPC Classes  ?

  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 471/04 - Ortho-condensed systems
  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
  • C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 487/04 - Ortho-condensed systems
  • C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
  • C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 407/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 403/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing aromatic rings
  • C07D 513/04 - Ortho-condensed systems
  • C07D 487/22 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups in which the condensed system contains four or more hetero rings
  • A61P 37/00 - Drugs for immunological or allergic disorders
  • A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
  • A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
  • C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
  • C07D 493/04 - Ortho-condensed systems

26.

TARGETED DOSING FOR THE TREATMENT OF COMPLEMENT MEDIATED DISORDERS

      
Application Number US2019066999
Publication Number 2020/131974
Status In Force
Filing Date 2019-12-17
Publication Date 2020-06-25
Owner ACHILLION PHARMACEUTICALS, INC. (USA)
Inventor
  • Huang, Mingjun
  • Podos, Steven, D.

Abstract

troughmaxmax, providing additional safety margin and better dosing flexibility.

IPC Classes  ?

  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 471/04 - Ortho-condensed systems

27.

Quinazoline and indole compounds to treat medical disorders

      
Application Number 16774117
Grant Number 11248000
Status In Force
Filing Date 2020-01-28
First Publication Date 2020-05-28
Grant Date 2022-02-15
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Wiles, Jason Allan
  • Phadke, Avinash

Abstract

Compounds, methods of use, and processes for making inhibitors of Complement Factor B are provided.

IPC Classes  ?

  • C07D 491/056 - Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 239/94 - Nitrogen atoms
  • C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 487/08 - Bridged systems
  • A61K 31/662 - Phosphorus acids or esters thereof having P—C bonds, e.g. foscarnet, trichlorfon
  • C07F 9/38 - Phosphonic acids [R—P(:O)(OH)2]Thiophosphonic acids
  • C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 451/02 - Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.02,4] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamineCyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.02,4] nonane ring systems, e.g. tropaneCyclic acetals thereof
  • C07D 471/02 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups in which the condensed system contains two hetero rings

28.

MORPHIC FORMS OF COMPLEMENT FACTOR D INHIBITORS

      
Application Number US2019053012
Publication Number 2020/069024
Status In Force
Filing Date 2019-09-25
Publication Date 2020-04-02
Owner ACHILLION PHARMACEUTICALS, INC. (USA)
Inventor
  • Phadke, Avinash, P.
  • Hashimoto, Akihiro
  • Andres, Mark

Abstract

This invention provides stable, highly crystalline forms of Complement Factor D inhibitor Compound 3 for therapeutic applications.

IPC Classes  ?

  • A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
  • A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
  • A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil

29.

Therapeutic regimens for treatment of paroxysmal nocturnal hemoglobinuria

      
Application Number 16700910
Grant Number 12076319
Status In Force
Filing Date 2019-12-02
First Publication Date 2020-04-02
Grant Date 2024-09-03
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Huang, Mingjun
  • Patel, Dharaben
  • Podos, Steven D.

Abstract

Provided herein are methods for treating a subject with PNH comprising administering to a subject a therapeutically effective amount of complement component C5 (C5) inhibitor, complement component C3 (C3) inhibitor, or complement factor B (CFB) inhibitor in combination with a therapeutically effective amount of small molecule complement factor D (CFD) inhibitor of Formula I or Formula II, or a pharmaceutically acceptable salt thereof.

IPC Classes  ?

  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61K 39/00 - Medicinal preparations containing antigens or antibodies
  • A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
  • A61P 7/00 - Drugs for disorders of the blood or the extracellular fluid
  • C07K 16/18 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans

30.

MACROCYCLIC COMPOUNDS FOR THE TREATMENT OF MEDICAL DISORDERS

      
Application Number US2019050065
Publication Number 2020/051532
Status In Force
Filing Date 2019-09-06
Publication Date 2020-03-12
Owner ACHILLION PHARMACEUTICALS, INC. (USA)
Inventor
  • Wiles, Jason, Allan
  • Gahhachanda, Venkat, Rao
  • Eastman, Kyle, J.
  • Godwin, Pais

Abstract

Compounds, methods of use, and processes for making inhibitors of complement factor D or a pharmaceutically acceptable salt or composition thereof are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade. The inhibitors of factor D described herein reduce excessive activation of complement.

IPC Classes  ?

  • A61K 31/416 - 1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
  • A61P 37/00 - Drugs for immunological or allergic disorders

31.

MORPHIC FORMS OF COMPLEMENT FACTOR D INHIBITORS

      
Application Number US2019050073
Publication Number 2020/051538
Status In Force
Filing Date 2019-09-06
Publication Date 2020-03-12
Owner ACHILLION PHARMACEUTICALS, INC. (USA)
Inventor Phadke, Avinash, P.

Abstract

This invention provides stable, highly crystalline forms of Complement factor D inhibitors Compound 1 and Compound 2 for advantageous therapeutic pharmaceutical efficacy and dosage form stability.

IPC Classes  ?

  • C07D 487/04 - Ortho-condensed systems
  • C07D 471/00 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups
  • C07D 471/04 - Ortho-condensed systems
  • C07D 487/00 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups
  • C07D 487/02 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups in which the condensed system contains two hetero rings

32.

Aryl, heteroaryl, and heterocyclic pharmaceutical compounds for treatment of medical disorders

      
Application Number 16555914
Grant Number 11084800
Status In Force
Filing Date 2019-08-29
First Publication Date 2020-03-05
Grant Date 2021-08-10
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Wiles, Jason Allan
  • Phadke, Avinash S.
  • Deshpande, Milind
  • Agarwal, Atul
  • Chen, Dawei
  • Gadhachanda, Venkat Rao
  • Hashimoto, Akihiro
  • Pais, Godwin
  • Wang, Qiuping
  • Wang, Xiangzhu
  • Barrish, Joel Charles
  • Greenlee, William
  • Eastman, Kyle J.

Abstract

Complement Factor D inhibitors, pharmaceutical compositions, and uses thereof, as well as processes for their manufacture are provided. The compounds provided include Formula I, Formula II, Formula III, Formula IV, and Formula V, or a pharmaceutically acceptable salt, prodrug, isotopic analog, N-oxide, or isolated isomer thereof, optionally in a pharmaceutically acceptable composition. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade.

IPC Classes  ?

  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07F 5/02 - Boron compounds
  • C07D 471/08 - Bridged systems
  • C07D 471/04 - Ortho-condensed systems
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 491/107 - Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
  • C07D 498/10 - Spiro-condensed systems

33.

PHARMACEUTICAL COMPOUNDS FOR THE TREATMENT OF COMPLEMENT FACTOR D MEDICAL DISORDERS

      
Application Number US2019047252
Publication Number 2020/041301
Status In Force
Filing Date 2019-08-20
Publication Date 2020-02-27
Owner ACHILLION PHARMACEUTICALS, INC. (USA)
Inventor
  • Wiles, Jason, Allan
  • Gadhachanda, Venkat, Rao
  • Eastman, Kyle, J.
  • Pais, Godwin

Abstract

Compounds, methods of use, and processes for making inhibitors of complement factor D or a pharmaceutically acceptable salt or composition thereof are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade. The inhibitors of factor D described herein reduce the excessive activation of complement.

IPC Classes  ?

  • C07C 229/06 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton
  • C07C 233/75 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
  • C07C 311/21 - Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring

34.

Aryl, heteroaryl, and heterocyclic compounds for treatment of complement mediated disorders

      
Application Number 16672114
Grant Number 12065459
Status In Force
Filing Date 2019-11-01
First Publication Date 2020-02-27
Grant Date 2024-08-20
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Wiles, Jason Allan
  • Gadhachanda, Venkat Rao
  • Wang, Qiuping
  • Pais, Godwin
  • Hashimoto, Akihiro
  • Chen, Dawei
  • Wang, Xiangzhu
  • Agarwal, Atul
  • Deshpande, Milind
  • Phadke, Avinash S.

Abstract

32) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.

IPC Classes  ?

  • C07F 9/572 - Five-membered rings
  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 31/404 - Indoles, e.g. pindolol
  • A61K 31/4045 - Indole-alkylaminesAmides thereof, e.g. serotonin, melatonin
  • A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
  • A61K 31/4162 - 1,2-Diazoles condensed with heterocyclic ring systems
  • A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
  • A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
  • A61K 31/4188 - 1,3-Diazoles condensed with heterocyclic ring systems, e.g. biotin, sorbinil
  • A61K 31/4192 - 1,2,3-Triazoles
  • A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
  • A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
  • A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
  • A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
  • A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
  • A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • A61K 31/549 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame having two or more nitrogen atoms in the same ring, e.g. hydrochlorothiazide
  • A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
  • A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
  • A61K 31/683 - Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
  • C07B 59/00 - Introduction of isotopes of elements into organic compounds
  • C07D 209/12 - Radicals substituted by oxygen atoms
  • C07D 209/14 - Radicals substituted by nitrogen atoms, not forming part of a nitro radical
  • C07D 209/30 - IndolesHydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
  • C07D 209/40 - Nitrogen atoms, not forming part of a nitro radical, e.g. isatin semicarbazone
  • C07D 209/42 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
  • C07D 209/44 - Iso-indolesHydrogenated iso-indoles
  • C07D 209/88 - CarbazolesHydrogenated carbazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the ring system
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 403/08 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing alicyclic rings
  • C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
  • C07D 413/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 417/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 471/04 - Ortho-condensed systems
  • C07D 471/08 - Bridged systems
  • C07D 487/04 - Ortho-condensed systems
  • C07D 487/14 - Ortho-condensed systems
  • C07D 491/113 - Spiro-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
  • C07D 495/04 - Ortho-condensed systems
  • C07D 513/04 - Ortho-condensed systems
  • C07F 5/02 - Boron compounds
  • C07F 7/08 - Compounds having one or more C—Si linkages
  • C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
  • C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings

35.

Macrocyclic compounds for treatment of medical disorders

      
Application Number 16555930
Grant Number 11053253
Status In Force
Filing Date 2019-08-29
First Publication Date 2020-01-02
Grant Date 2021-07-06
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Wiles, Jason Allan
  • Phadke, Avinash S.
  • Chen, Dawei
  • Gadhachanda, Venkat Rao
  • Barrish, Joel Charles
  • Agarwal, Atul
  • Eastman, Kyle J.

Abstract

Macrocyclic Complement Factor D inhibitors, pharmaceutical compositions, and uses thereof, as well as processes for their manufacture are provided. The compounds provided include Formula I, Formula II, Formula III, Formula IV, Formula V, Formula VI, Formula VII, and Formula VIII or a pharmaceutically acceptable salt, prodrug, isotopic analog, N-oxide, or isolated isomer thereof, optionally in a pharmaceutically acceptable composition. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade.

IPC Classes  ?

36.

Pharmaceutical compounds for treatment of medical disorders

      
Application Number 16555946
Grant Number 11447465
Status In Force
Filing Date 2019-08-29
First Publication Date 2019-12-19
Grant Date 2022-09-20
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Wiles, Jason Allan
  • Phadke, Avinash S.
  • Deshpande, Milind
  • Agarwal, Atul
  • Chen, Dawei
  • Gadhachanda, Venkat Rao
  • Hashimoto, Akihiro
  • Pais, Godwin
  • Wang, Qiuping
  • Wang, Xiangzhu
  • Barrish, Joel Charles
  • Greenlee, William
  • Eastman, Kyle J.

Abstract

Complement Factor D inhibitors, pharmaceutical compositions, and uses thereof, as well as processes for their manufacture are provided. The compounds provided include Formula I, Formula II, Formula III, and Formula IV or a pharmaceutically acceptable salt, prodrug, isotopic analog, N-oxide, or isolated isomer thereof, optionally in a pharmaceutically acceptable composition. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade.

IPC Classes  ?

  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 403/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing aromatic rings
  • C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
  • C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 471/04 - Ortho-condensed systems
  • C07D 493/04 - Ortho-condensed systems
  • C07D 495/04 - Ortho-condensed systems
  • C07D 513/04 - Ortho-condensed systems
  • C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system

37.

COMPLEMENT ALTERNATIVE PATHWAY-ASSOCIATED NEPHROPATHY BIOMARKERS

      
Application Number US2019034210
Publication Number 2019/227102
Status In Force
Filing Date 2019-05-28
Publication Date 2019-11-28
Owner ACHILLION PHARMACEUTICALS, INC. (USA)
Inventor
  • Huang, Mingjun
  • Podos, Steven, D.
  • Yang, Wengang
  • Zhao, Yongsen

Abstract

Provided herein are methods for using determinative urinary biomarkers for identifying a human subject suffering from an alternative pathway (AP)-associated nephropathy. Also provided herein is a method for using determinative urinary biomarkers to determine whether a human subject suffering from a complement mediated nephropathy is likely to respond to an inhibitor of the alternative complement pathway ("AP") in treating the complement mediated nephropathy. Further provided herein is a method for using urinary biomarkers to assess the therapeutic response of a human subject suffering from an AP-associated nephropathy receiving inhibitors of the complement alternative pathway (AP inhibitors).

IPC Classes  ?

  • C07K 16/18 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans
  • C07K 16/40 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against enzymes
  • A61K 31/33 - Heterocyclic compounds
  • A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
  • A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
  • A61K 31/41 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
  • A61K 31/435 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
  • A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum

38.

Aryl, heteroaryl, and heterocyclic compounds for treatment of medical disorders

      
Application Number 16351203
Grant Number 10822352
Status In Force
Filing Date 2019-03-12
First Publication Date 2019-07-11
Grant Date 2020-11-03
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Wiles, Jason Allan
  • Phadke, Avinash S.
  • Deshpande, Milind
  • Agarwal, Atul
  • Chen, Dawei
  • Gadhachanda, Venkat Rao
  • Hashimoto, Akihiro
  • Pais, Godwin
  • Wang, Qiuping
  • Wang, Xiangzhu

Abstract

Compounds, methods of use, and processes for making inhibitors of complement Factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is an aryl, heteroaryl or heterocycle (R32) are provided. The inhibitors of Factor D described herein reduce the excessive activation of complement.

IPC Classes  ?

  • A61P 25/00 - Drugs for disorders of the nervous system
  • A61P 25/02 - Drugs for disorders of the nervous system for peripheral neuropathies
  • A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
  • A61P 9/00 - Drugs for disorders of the cardiovascular system
  • A61P 11/00 - Drugs for disorders of the respiratory system
  • A61P 13/02 - Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
  • A61P 13/00 - Drugs for disorders of the urinary system
  • A61P 21/00 - Drugs for disorders of the muscular or neuromuscular system
  • A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
  • A61P 17/00 - Drugs for dermatological disorders
  • A61P 27/02 - Ophthalmic agents
  • A61P 27/00 - Drugs for disorders of the senses
  • A61P 43/00 - Drugs for specific purposes, not provided for in groups
  • A61P 3/06 - Antihyperlipidemics
  • A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
  • A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
  • C07D 487/04 - Ortho-condensed systems
  • C07D 513/04 - Ortho-condensed systems
  • C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 493/04 - Ortho-condensed systems
  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 495/04 - Ortho-condensed systems
  • C07D 471/04 - Ortho-condensed systems
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings

39.

Aryl, heteroaryl, and heterocyclic compounds for treatment of complement mediated disorders

      
Application Number 16276139
Grant Number 10464956
Status In Force
Filing Date 2019-02-14
First Publication Date 2019-06-20
Grant Date 2019-11-05
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Wiles, Jason Allan
  • Gadhachanda, Venkat Rao
  • Wang, Qiuping
  • Pais, Godwin
  • Hashimoto, Akihiro
  • Chen, Dawei
  • Wang, Xiangzhu
  • Agarwal, Atul
  • Deshpande, Milind
  • Phadke, Avinash S.

Abstract

32) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.

IPC Classes  ?

  • C07D 495/14 - Ortho-condensed systems
  • C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • A61K 31/4045 - Indole-alkylaminesAmides thereof, e.g. serotonin, melatonin
  • A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
  • A61K 31/4162 - 1,2-Diazoles condensed with heterocyclic ring systems
  • C07F 9/572 - Five-membered rings
  • C07F 7/08 - Compounds having one or more C—Si linkages
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 209/42 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
  • C07D 471/08 - Bridged systems
  • C07D 209/30 - IndolesHydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
  • C07D 209/44 - Iso-indolesHydrogenated iso-indoles
  • C07D 209/88 - CarbazolesHydrogenated carbazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the ring system
  • C07D 209/12 - Radicals substituted by oxygen atoms
  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
  • A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
  • A61K 31/404 - Indoles, e.g. pindolol
  • A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
  • A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
  • A61K 31/4188 - 1,3-Diazoles condensed with heterocyclic ring systems, e.g. biotin, sorbinil
  • A61K 31/4192 - 1,2,3-Triazoles
  • A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
  • A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
  • A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
  • A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61K 31/549 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame having two or more nitrogen atoms in the same ring, e.g. hydrochlorothiazide
  • A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
  • A61K 31/683 - Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
  • C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
  • C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
  • C07D 513/04 - Ortho-condensed systems
  • C07B 59/00 - Introduction of isotopes of elements into organic compounds
  • C07D 471/04 - Ortho-condensed systems
  • C07D 209/14 - Radicals substituted by nitrogen atoms, not forming part of a nitro radical
  • C07D 209/40 - Nitrogen atoms, not forming part of a nitro radical, e.g. isatin semicarbazone
  • C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 487/14 - Ortho-condensed systems
  • C07D 491/113 - Spiro-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
  • C07D 495/04 - Ortho-condensed systems
  • C07D 413/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 403/08 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing alicyclic rings
  • C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
  • C07D 487/04 - Ortho-condensed systems
  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07F 5/02 - Boron compounds
  • C07D 417/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

40.

Amino compounds for treatment of complement mediated disorders

      
Application Number 16246832
Grant Number 10689409
Status In Force
Filing Date 2019-01-14
First Publication Date 2019-05-16
Grant Date 2020-06-23
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Gadhachanda, Venkat Rao
  • Hashimoto, Akihiro
  • Pais, Godwin
  • Wang, Qiuping
  • Chen, Dawei
  • Wang, Xiangzhu
  • Agarwal, Atul
  • Deshpande, Milind
  • Wiles, Jason Allan
  • Phadke, Avinash

Abstract

32) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.

IPC Classes  ?

  • C07D 471/04 - Ortho-condensed systems
  • C07F 9/572 - Five-membered rings
  • C07D 209/42 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
  • C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 417/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
  • C07F 5/02 - Boron compounds
  • C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07F 7/08 - Compounds having one or more C—Si linkages
  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 487/04 - Ortho-condensed systems
  • C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
  • C07D 403/08 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing alicyclic rings
  • C07D 413/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
  • A61K 31/404 - Indoles, e.g. pindolol
  • A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
  • A61K 31/4162 - 1,2-Diazoles condensed with heterocyclic ring systems
  • A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
  • A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
  • A61K 31/4188 - 1,3-Diazoles condensed with heterocyclic ring systems, e.g. biotin, sorbinil
  • A61K 31/4192 - 1,2,3-Triazoles
  • A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
  • A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
  • A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
  • A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61K 31/549 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame having two or more nitrogen atoms in the same ring, e.g. hydrochlorothiazide
  • A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
  • A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
  • A61K 31/683 - Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
  • C07B 59/00 - Introduction of isotopes of elements into organic compounds
  • C07D 209/14 - Radicals substituted by nitrogen atoms, not forming part of a nitro radical
  • C07D 209/40 - Nitrogen atoms, not forming part of a nitro radical, e.g. isatin semicarbazone
  • C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 487/14 - Ortho-condensed systems
  • C07D 491/113 - Spiro-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
  • C07D 495/04 - Ortho-condensed systems
  • C07D 513/04 - Ortho-condensed systems
  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 31/4045 - Indole-alkylaminesAmides thereof, e.g. serotonin, melatonin
  • A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
  • A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • C07D 209/12 - Radicals substituted by oxygen atoms
  • C07D 209/30 - IndolesHydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
  • C07D 209/44 - Iso-indolesHydrogenated iso-indoles
  • C07D 209/88 - CarbazolesHydrogenated carbazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the ring system
  • C07D 471/08 - Bridged systems

41.

Quinazoline and indole compounds to treat medical disorders

      
Application Number 16226378
Grant Number 10961252
Status In Force
Filing Date 2018-12-19
First Publication Date 2019-05-09
Grant Date 2021-03-30
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Wiles, Jason Allan
  • Phadke, Avinash

Abstract

Compounds, methods of use, and processes for making inhibitors of Complement Factor B are provided.

IPC Classes  ?

  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 491/056 - Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
  • C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 239/94 - Nitrogen atoms
  • C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 487/08 - Bridged systems
  • A61K 31/662 - Phosphorus acids or esters thereof having P—C bonds, e.g. foscarnet, trichlorfon
  • C07F 9/38 - Phosphonic acids [R—P(:O)(OH)2]Thiophosphonic acids
  • C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 451/02 - Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.02,4] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamineCyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.02,4] nonane ring systems, e.g. tropaneCyclic acetals thereof
  • C07D 471/02 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups in which the condensed system contains two hetero rings

42.

Phosphonate compounds for treatment of complement mediated disorders

      
Application Number 16162162
Grant Number 10301336
Status In Force
Filing Date 2018-10-16
First Publication Date 2019-03-21
Grant Date 2019-05-28
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Wiles, Jason Allan
  • Hashimoto, Akihiro
  • Gadhachanda, Venkat Rao
  • Pais, Godwin
  • Wang, Qiuping
  • Chen, Dawei
  • Wang, Xiangzhu
  • Agarwal, Atul
  • Deshpande, Milind
  • Phadke, Avinash

Abstract

32) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.

IPC Classes  ?

  • A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
  • C07F 9/572 - Five-membered rings
  • A61K 31/4045 - Indole-alkylaminesAmides thereof, e.g. serotonin, melatonin
  • A61K 31/404 - Indoles, e.g. pindolol
  • A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
  • A61K 31/4162 - 1,2-Diazoles condensed with heterocyclic ring systems
  • A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
  • A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
  • A61K 31/4188 - 1,3-Diazoles condensed with heterocyclic ring systems, e.g. biotin, sorbinil
  • A61K 31/4192 - 1,2,3-Triazoles
  • A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
  • A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
  • A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
  • A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61K 31/549 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame having two or more nitrogen atoms in the same ring, e.g. hydrochlorothiazide
  • A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
  • A61K 31/683 - Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
  • C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
  • C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
  • C07D 513/04 - Ortho-condensed systems
  • C07B 59/00 - Introduction of isotopes of elements into organic compounds
  • C07D 209/14 - Radicals substituted by nitrogen atoms, not forming part of a nitro radical
  • C07D 209/40 - Nitrogen atoms, not forming part of a nitro radical, e.g. isatin semicarbazone
  • C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 487/14 - Ortho-condensed systems
  • C07D 491/113 - Spiro-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
  • C07D 495/04 - Ortho-condensed systems
  • C07D 413/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 403/08 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing alicyclic rings
  • C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
  • C07D 487/04 - Ortho-condensed systems
  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07F 5/02 - Boron compounds
  • C07D 471/04 - Ortho-condensed systems
  • C07D 417/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07F 7/08 - Compounds having one or more C—Si linkages
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 209/42 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
  • C07D 471/08 - Bridged systems
  • C07D 209/30 - IndolesHydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
  • C07D 209/44 - Iso-indolesHydrogenated iso-indoles
  • C07D 209/88 - CarbazolesHydrogenated carbazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the ring system
  • C07D 209/12 - Radicals substituted by oxygen atoms
  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate

43.

Ether compounds for treatment of complement mediated disorders

      
Application Number 16164632
Grant Number 10550140
Status In Force
Filing Date 2018-10-18
First Publication Date 2019-02-14
Grant Date 2020-02-04
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Wiles, Jason Allan
  • Gadhachanda, Venkat Rao
  • Pais, Godwin
  • Hashimoto, Akihiro
  • Wang, Qiuping
  • Chen, Dawei
  • Wang, Xiangzhu
  • Agarwal, Atul
  • Deshpande, Milind
  • Phadke, Avinash S.

Abstract

32) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.

IPC Classes  ?

  • C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07F 9/572 - Five-membered rings
  • C07D 209/42 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
  • C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 471/04 - Ortho-condensed systems
  • C07D 417/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
  • C07F 5/02 - Boron compounds
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07F 7/08 - Compounds having one or more C—Si linkages
  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 487/04 - Ortho-condensed systems
  • C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
  • C07D 403/08 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing alicyclic rings
  • C07D 413/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
  • A61K 31/404 - Indoles, e.g. pindolol
  • A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
  • A61K 31/4162 - 1,2-Diazoles condensed with heterocyclic ring systems
  • A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
  • A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
  • A61K 31/4188 - 1,3-Diazoles condensed with heterocyclic ring systems, e.g. biotin, sorbinil
  • A61K 31/4192 - 1,2,3-Triazoles
  • A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
  • A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
  • A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
  • A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61K 31/549 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame having two or more nitrogen atoms in the same ring, e.g. hydrochlorothiazide
  • A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
  • A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
  • A61K 31/683 - Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
  • C07B 59/00 - Introduction of isotopes of elements into organic compounds
  • C07D 209/14 - Radicals substituted by nitrogen atoms, not forming part of a nitro radical
  • C07D 209/40 - Nitrogen atoms, not forming part of a nitro radical, e.g. isatin semicarbazone
  • C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 487/14 - Ortho-condensed systems
  • C07D 491/113 - Spiro-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
  • C07D 495/04 - Ortho-condensed systems
  • C07D 513/04 - Ortho-condensed systems
  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 31/4045 - Indole-alkylaminesAmides thereof, e.g. serotonin, melatonin
  • A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
  • A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • C07D 209/12 - Radicals substituted by oxygen atoms
  • C07D 209/30 - IndolesHydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
  • C07D 209/44 - Iso-indolesHydrogenated iso-indoles
  • C07D 209/88 - CarbazolesHydrogenated carbazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the ring system
  • C07D 471/08 - Bridged systems

44.

THERAPEUTIC REGIMENS FOR TREATMENT OF PAROXYSMAL NOCTURNAL HEMOGLOBINURIA

      
Application Number US2018045057
Publication Number 2019/028284
Status In Force
Filing Date 2018-08-02
Publication Date 2019-02-07
Owner ACHILLION PHARMACEUTICALS, INC. (USA)
Inventor
  • Huang, Mingjun
  • Patel, Dharaben
  • Podos, Steven, D.

Abstract

Provided herein are methods for treating a subject with PNH comprising administering to a subject a therapeutically effective amount of complement component C5 (C5) inhibitor, complement component C3 (C3) inhibitor, or complement factor B (CFB) inhibitor in combination with a therapeutically effective amount of small molecule complement factor D (CFD) inhibitor of Formula I or Formula II, or a pharmaceutically acceptable salt thereof.

IPC Classes  ?

  • A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
  • A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
  • A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 471/04 - Ortho-condensed systems

45.

Compounds for treatment of complement mediated disorders

      
Application Number 16148622
Grant Number 10428095
Status In Force
Filing Date 2018-10-01
First Publication Date 2019-01-31
Grant Date 2019-10-01
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Wiles, Jason Allan
  • Phadke, Avinash S.
  • Wang, Xiangzhu
  • Chen, Dawei
  • Hashimoto, Akihiro
  • Gadhachanda, Venkat Rao
  • Pais, Godwin
  • Wang, Qiuping
  • Agarwal, Atul
  • Deshpande, Milind

Abstract

Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.

IPC Classes  ?

  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07F 9/572 - Five-membered rings
  • C07D 209/42 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
  • C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 471/04 - Ortho-condensed systems
  • C07D 417/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07F 7/08 - Compounds having one or more C—Si linkages
  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 487/04 - Ortho-condensed systems
  • C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
  • C07D 403/08 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing alicyclic rings
  • C07D 413/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07F 5/02 - Boron compounds
  • C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
  • C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
  • A61K 31/404 - Indoles, e.g. pindolol
  • A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
  • A61K 31/4162 - 1,2-Diazoles condensed with heterocyclic ring systems
  • A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
  • A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
  • A61K 31/4188 - 1,3-Diazoles condensed with heterocyclic ring systems, e.g. biotin, sorbinil
  • A61K 31/4192 - 1,2,3-Triazoles
  • A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
  • A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
  • A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
  • A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61K 31/549 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame having two or more nitrogen atoms in the same ring, e.g. hydrochlorothiazide
  • A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
  • A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
  • A61K 31/683 - Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
  • C07B 59/00 - Introduction of isotopes of elements into organic compounds
  • C07D 209/14 - Radicals substituted by nitrogen atoms, not forming part of a nitro radical
  • C07D 209/40 - Nitrogen atoms, not forming part of a nitro radical, e.g. isatin semicarbazone
  • C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 487/14 - Ortho-condensed systems
  • C07D 491/113 - Spiro-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
  • C07D 495/04 - Ortho-condensed systems
  • C07D 513/04 - Ortho-condensed systems
  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 31/4045 - Indole-alkylaminesAmides thereof, e.g. serotonin, melatonin
  • A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
  • A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • C07D 209/12 - Radicals substituted by oxygen atoms
  • C07D 209/30 - IndolesHydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
  • C07D 209/44 - Iso-indolesHydrogenated iso-indoles
  • C07D 209/88 - CarbazolesHydrogenated carbazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the ring system
  • C07D 471/08 - Bridged systems

46.

Aryl, heteroaryl, and heterocyclic compounds for treatment of complement mediated disorders

      
Application Number 16140148
Grant Number 10253053
Status In Force
Filing Date 2018-09-24
First Publication Date 2019-01-24
Grant Date 2019-04-09
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Wiles, Jason Allan
  • Gadhachanda, Venkat Rao
  • Wang, Qiuping
  • Pais, Godwin
  • Hashimoto, Akihiro
  • Chen, Dawei
  • Wang, Xiangzhu
  • Agarwal, Atul
  • Deshpande, Milind
  • Phadke, Avinash S.

Abstract

32) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.

IPC Classes  ?

  • C07D 471/04 - Ortho-condensed systems
  • C07D 471/08 - Bridged systems
  • C07D 487/04 - Ortho-condensed systems
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
  • C07D 413/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 417/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07F 9/572 - Five-membered rings
  • C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 209/42 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
  • C07D 209/30 - IndolesHydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
  • C07D 209/44 - Iso-indolesHydrogenated iso-indoles
  • C07D 209/88 - CarbazolesHydrogenated carbazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the ring system
  • C07D 209/12 - Radicals substituted by oxygen atoms
  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 31/4045 - Indole-alkylaminesAmides thereof, e.g. serotonin, melatonin
  • A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
  • A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
  • A61K 31/404 - Indoles, e.g. pindolol
  • A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
  • A61K 31/4162 - 1,2-Diazoles condensed with heterocyclic ring systems
  • A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
  • A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
  • A61K 31/4188 - 1,3-Diazoles condensed with heterocyclic ring systems, e.g. biotin, sorbinil
  • A61K 31/4192 - 1,2,3-Triazoles
  • A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
  • A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
  • A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
  • A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61K 31/549 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame having two or more nitrogen atoms in the same ring, e.g. hydrochlorothiazide
  • A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
  • A61K 31/683 - Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
  • C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
  • C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
  • C07D 513/04 - Ortho-condensed systems
  • C07B 59/00 - Introduction of isotopes of elements into organic compounds
  • C07D 209/14 - Radicals substituted by nitrogen atoms, not forming part of a nitro radical
  • C07D 209/40 - Nitrogen atoms, not forming part of a nitro radical, e.g. isatin semicarbazone
  • C07D 487/14 - Ortho-condensed systems
  • C07D 491/113 - Spiro-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
  • C07D 495/04 - Ortho-condensed systems
  • C07D 403/08 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing alicyclic rings
  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07F 5/02 - Boron compounds
  • C07F 7/08 - Compounds having one or more C—Si linkages

47.

Aryl, heteroaryl, and heterocyclic compounds for treatment of medical disorders

      
Application Number 16010081
Grant Number 10287301
Status In Force
Filing Date 2018-06-15
First Publication Date 2018-10-25
Grant Date 2019-05-14
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Wiles, Jason Allan
  • Phadke, Avinash S.
  • Deshpande, Milind
  • Agarwal, Atul
  • Chen, Dawei
  • Gadhachanda, Venkat Rao
  • Hashimoto, Akihiro
  • Pais, Godwin
  • Wang, Qiuping
  • Wang, Xiangzhu

Abstract

Compounds, methods of use, and processes for making inhibitors of complement Factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is an aryl, heteroaryl or heterocycle (R32) are provided. The inhibitors of Factor D described herein reduce the excessive activation of complement.

IPC Classes  ?

  • C07D 513/04 - Ortho-condensed systems
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 471/04 - Ortho-condensed systems
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 487/04 - Ortho-condensed systems
  • C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
  • C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 495/04 - Ortho-condensed systems
  • C07D 493/04 - Ortho-condensed systems
  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

48.

ARYL, HETEROARY, AND HETEROCYCLIC PHARMACEUTICAL COMPOUNDS FOR TREATMENT OF MEDICAL DISORDERS

      
Application Number US2018020528
Publication Number 2018/160889
Status In Force
Filing Date 2018-03-01
Publication Date 2018-09-07
Owner ACHILLION PHARMACEUTICALS, INC. (USA)
Inventor
  • Wiles, Jason, Allan
  • Phadke, Avinash, S.
  • Deshpande, Milind
  • Agarwal, Atul
  • Chen, Dawei
  • Gadhachanda, Venkat, Rao
  • Hashimoto, Akihiro
  • Pais, Godwin
  • Wang, Qiuping
  • Wang, Xiangzhu
  • Barrish, Joel, Charles
  • Greenlee, William
  • Eastman, Kyle, J.

Abstract

Complement Factor D inhibitors, pharmaceutical compositions, and uses thereof, as well as processes for their manufacture are provided. The compounds provided include Formula I, Formula II, Formula III, Formula IV, and Formula V, or a pharmaceutically acceptable salt, prodrug, isotopic analog, N-oxide, or isolated isomer thereof, optionally in a pharmaceutically acceptable composition. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade.

IPC Classes  ?

  • C07D 403/08 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing alicyclic rings
  • C07F 9/572 - Five-membered rings

49.

MACROCYCLIC COMPOUNDS FOR TREATMENT OF MEDICAL DISORDERS

      
Application Number US2018020531
Publication Number 2018/160892
Status In Force
Filing Date 2018-03-01
Publication Date 2018-09-07
Owner ACHILLION PHARMACEUTICALS, INC. (USA)
Inventor
  • Wiles, Jason, Allan
  • Phadke, Avinash, S.
  • Chen, Dawei
  • Gadhachanda, Venkat, Rao
  • Barrish, Joel, Charles
  • Agarwal, Atul
  • Eastman, Kyle, J.

Abstract

Macrocyclic Complement Factor D inhibitors, pharmaceutical compositions, and uses thereof, as well as processes for their manufacture are provided. The compounds provided include Formula I, Formula II, Formula III, Formula IV, Formula V, Formula VI, Formula VII, and Formula VIII or a pharmaceutically acceptable salt, prodrug, isotopic analog, N-oxide, or isolated isomer thereof, optionally in a pharmaceutically acceptable composition. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade.

IPC Classes  ?

  • A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
  • A61P 31/12 - Antivirals
  • C07D 498/08 - Bridged systems

50.

PHARMACEUTICAL COMPOUNDS FOR TREATMENT OF MEDICAL DISORDERS

      
Application Number US2018020530
Publication Number 2018/160891
Status In Force
Filing Date 2018-03-01
Publication Date 2018-09-07
Owner ACHILLION PHARMACEUTICAL, INC. (USA)
Inventor
  • Wiles, Jason Allan
  • Phadke, Avinash S.
  • Deshpande, Milind
  • Agarwal, Atul
  • Chen, Dawei
  • Gadhachanda, Venkat Rao
  • Hashimoto, Akihiro
  • Pais, Godwin
  • Wang, Qiuping
  • Wang, Xiangzhu
  • Barrish, Joel Charles
  • Greenlee, William
  • Eastman, Kyle J.

Abstract

Complement Factor D inhibitors, pharmaceutical compositions, and uses thereof, as well as processes for their manufacture are provided. The compounds provided include Formula I, Formula II, Formula III, and Formula IV or a pharmaceutically acceptable salt, prodrug, isotopic analog, N-oxide, or isolated isomer thereof, optionally in a pharmaceutically acceptable composition. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade.

IPC Classes  ?

  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 487/04 - Ortho-condensed systems

51.

WEC3G

      
Application Number 1414741
Status Registered
Filing Date 2018-01-05
Registration Date 2018-01-05
Owner Achillion Pharmaceuticals, Inc. (USA)
NICE Classes  ?
  • 41 - Education, entertainment, sporting and cultural services
  • 44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services

Goods & Services

Educational services, namely, providing information about the treatment of kidney disease (term considered too vague by the International Bureau - rule 13 (2) (b) of the Common Regulations). Providing medical information.

52.

TOGETHER, WE ARE C3G

      
Application Number 1415253
Status Registered
Filing Date 2018-01-05
Registration Date 2018-01-05
Owner Achillion Pharmaceuticals, Inc. (USA)
NICE Classes  ?
  • 41 - Education, entertainment, sporting and cultural services
  • 44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services

Goods & Services

Educational services, namely, providing information about the treatment of kidney disease (term considered too vague by the International Bureau - rule 13 (2) (b) of the Common Regulations). Providing medical information.

53.

Compounds for treatment of immune inflammatory disorders

      
Application Number 15905537
Grant Number 10807952
Status In Force
Filing Date 2018-02-26
First Publication Date 2018-07-19
Grant Date 2020-10-20
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Wiles, Jason Allan
  • Phadke, Avinash S.
  • Deshpande, Milind
  • Agarwal, Atul
  • Chen, Dawei
  • Gadhachanda, Venkat Rao
  • Hashimoto, Akihiro
  • Pais, Godwin
  • Wang, Qiuping
  • Wang, Xiangzhu
  • Greenlee, William

Abstract

Compounds, methods of use, and processes for making inhibitors of complement Factor D are provided comprising Formula I, I″ and I′″ or a pharmaceutically acceptable salt or composition thereof. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduces the excessive activation of complement.

IPC Classes  ?

  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 209/12 - Radicals substituted by oxygen atoms
  • C07D 487/04 - Ortho-condensed systems
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • C07D 513/04 - Ortho-condensed systems
  • C07D 231/56 - BenzopyrazolesHydrogenated benzopyrazoles
  • C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
  • A61P 27/02 - Ophthalmic agents
  • A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
  • C07D 207/16 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
  • C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 471/04 - Ortho-condensed systems
  • C07D 495/04 - Ortho-condensed systems

54.

Amide compounds for treatment of immune and inflammatory disorders

      
Application Number 15905461
Grant Number 10919884
Status In Force
Filing Date 2018-02-26
First Publication Date 2018-07-05
Grant Date 2021-02-16
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Wiles, Jason Allan
  • Phadke, Avinash S.
  • Deshpande, Milind
  • Agarwal, Atul
  • Chen, Dawei
  • Gadhachanda, Venkat Rao
  • Hashimoto, Akihiro
  • Pais, Godwin
  • Wang, Qiuping
  • Wang, Xiangzhu
  • Greenlee, William

Abstract

Compounds, methods of use, and processes for making inhibitors of complement Factor D are provided comprising Formula I, I″ and I′″ or a pharmaceutically acceptable salt or composition thereof. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduces the excessive activation of complement.

IPC Classes  ?

  • A61K 31/416 - 1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
  • A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
  • A61K 31/5025 - PyridazinesHydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
  • C07D 231/56 - BenzopyrazolesHydrogenated benzopyrazoles
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 471/04 - Ortho-condensed systems
  • C07D 487/04 - Ortho-condensed systems
  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
  • C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 513/04 - Ortho-condensed systems
  • C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system

55.

Disubstituted compounds for treatment of medical disorders

      
Application Number 15905504
Grant Number 11001600
Status In Force
Filing Date 2018-02-26
First Publication Date 2018-06-28
Grant Date 2021-05-11
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Wiles, Jason Allan
  • Phadke, Avinash S.
  • Deshpande, Milind
  • Agarwal, Atul
  • Chen, Dawei
  • Gadhachanda, Venkat Rao
  • Hashimoto, Akihiro
  • Pais, Godwin
  • Wang, Qiuping
  • Wang, Xiangzhu

Abstract

Compounds, methods of use, and processes for making inhibitors of complement Factor D are provided comprising Formula I, or a pharmaceutically acceptable salt or composition thereof. The inhibitors of Factor D described herein reduce the excessive activation of complement, and are useful to treat disorders mediated by the complement system.

IPC Classes  ?

  • C07F 9/6512 - Six-membered rings having the nitrogen atoms in positions 1 and 3
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 471/04 - Ortho-condensed systems
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • A61P 27/02 - Ophthalmic agents
  • A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
  • A61P 9/00 - Drugs for disorders of the cardiovascular system
  • A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
  • A61P 11/00 - Drugs for disorders of the respiratory system
  • A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]

56.

Amino compounds for treatment of medical disorders

      
Application Number 15905427
Grant Number 10660876
Status In Force
Filing Date 2018-02-26
First Publication Date 2018-06-28
Grant Date 2020-05-26
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Wiles, Jason Allan
  • Phadke, Avinash S.
  • Deshpande, Milind
  • Agarwal, Atul
  • Chen, Dawei
  • Gadhachanda, Venkat Rao
  • Hashimoto, Akihiro
  • Pais, Godwin
  • Wang, Qiuping
  • Wang, Xiangzhu

Abstract

32) are provided. The inhibitors of Factor D described herein reduce the excessive activation of complement.

IPC Classes  ?

  • A61K 31/404 - Indoles, e.g. pindolol
  • C07D 471/04 - Ortho-condensed systems
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 471/08 - Bridged systems
  • C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 487/04 - Ortho-condensed systems
  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
  • A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
  • A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • A61K 31/5383 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
  • A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole

57.

Aryl, heteroaryl, and heterocyclic compounds for treatment of immune and inflammatory disorders

      
Application Number 15905524
Grant Number 10662175
Status In Force
Filing Date 2018-02-26
First Publication Date 2018-06-28
Grant Date 2020-05-26
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Wiles, Jason Allan
  • Phadke, Avinash S.
  • Deshpande, Milind
  • Agarwal, Atul
  • Chen, Dawei
  • Gadhachanda, Venkat Rao
  • Hashimoto, Akihiro
  • Pais, Godwin
  • Wang, Qiuping
  • Wang, Xiangzhu
  • Greenlee, William

Abstract

Compounds, methods of use, and processes for making inhibitors of complement Factor D are provided comprising Formula I, I″ and I′″ or a pharmaceutically acceptable salt or composition thereof. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduces the excessive activation of complement.

IPC Classes  ?

  • C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
  • C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 471/04 - Ortho-condensed systems
  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
  • C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 487/04 - Ortho-condensed systems
  • C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
  • C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 407/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 403/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing aromatic rings
  • C07D 513/04 - Ortho-condensed systems
  • C07D 487/22 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups in which the condensed system contains four or more hetero rings
  • A61P 37/00 - Drugs for immunological or allergic disorders
  • A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
  • A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
  • C07D 493/04 - Ortho-condensed systems

58.

Amino compounds for treatment of immune and inflammatory disorders

      
Application Number 15905535
Grant Number 10906887
Status In Force
Filing Date 2018-02-26
First Publication Date 2018-06-28
Grant Date 2021-02-02
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Wiles, Jason Allan
  • Phadke, Avinash S.
  • Deshpande, Milind
  • Agarwal, Atul
  • Chen, Dawei
  • Gadhachanda, Venkat Rao
  • Hashimoto, Akihiro
  • Pais, Godwin
  • Wang, Qiuping
  • Wang, Xiangzhu
  • Greenlee, William

Abstract

Compounds, methods of use, and processes for making inhibitors of complement Factor D are provided comprising Formula I, I″ and I′″ or a pharmaceutically acceptable salt or composition thereof. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduces the excessive activation of complement.

IPC Classes  ?

  • A61K 31/416 - 1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
  • A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
  • A61K 31/5025 - PyridazinesHydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
  • C07D 231/56 - BenzopyrazolesHydrogenated benzopyrazoles
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 471/04 - Ortho-condensed systems
  • C07D 487/04 - Ortho-condensed systems
  • C07D 495/04 - Ortho-condensed systems
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • C07D 209/12 - Radicals substituted by oxygen atoms
  • C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 513/04 - Ortho-condensed systems
  • C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
  • C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links

59.

ODALASVIR POLYMORPHS AND METHODS OF MANUFACTURE THEREOF

      
Application Number US2017054512
Publication Number 2018/064585
Status In Force
Filing Date 2017-09-29
Publication Date 2018-04-05
Owner
  • JANSSEN PHARMACEUTICALS, INC. (USA)
  • ACHILLION PHARMACEUTICALS, INC. (USA)
Inventor
  • Phadke, Avinash
  • Chen, Dawei
  • Holan, Jan

Abstract

The invention provides Odalasvir polymorphs, hydrates, and solvates that exhibit advantageous properties, including purity, useful for the preparation of a therapeutic formulation.

IPC Classes  ?

  • A61K 31/439 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
  • A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
  • A61K 31/555 - Heterocyclic compounds containing heavy metals, e.g. hemin, hematin, melarsoprol
  • A61P 31/14 - Antivirals for RNA viruses
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 471/08 - Bridged systems

60.

Substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero- heteraphanes and metallocenes useful for treating HCV infections

      
Application Number 15804842
Grant Number 10092547
Status In Force
Filing Date 2017-11-06
First Publication Date 2018-03-01
Grant Date 2018-10-09
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Wiles, Jason Allan
  • Wang, Qiuping
  • Hashimoto, Akihiro
  • Pais, Godwin
  • Wang, Xiangzhu
  • Gadhachanda, Venkat
  • Phadke, Avinash
  • Deshpande, Milind
  • Chen, Dawei

Abstract

useful as antiviral agents. In certain embodiments disclosed herein M is a group —P-A-P— where A is Certain substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. Pharmaceutical compositions/and combinations containing one or more substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes and a pharmaceutically acceptable carrier are also provided by this disclosure. Methods for treating viral infections, including Hepatitis C viral infections are provided by the disclosure.

IPC Classes  ?

  • A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
  • C07F 17/02 - Metallocenes of metals of Groups 8, 9 or 10 of the Periodic Table
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 209/42 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
  • C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • C07F 15/02 - Iron compounds
  • A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
  • A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
  • C07D 453/06 - Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing iso-quinuclidine ring systems
  • C07D 491/113 - Spiro-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
  • A61K 31/422 - Oxazoles not condensed and containing further heterocyclic rings
  • C07F 5/02 - Boron compounds
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 471/08 - Bridged systems
  • C07D 491/10 - Spiro-condensed systems
  • C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
  • A61K 31/555 - Heterocyclic compounds containing heavy metals, e.g. hemin, hematin, melarsoprol
  • A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
  • A61K 31/439 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine

61.

Aryl, heteroaryl, and heterocyclic compounds for treatment of complement mediated disorders

      
Application Number 15711794
Grant Number 10081645
Status In Force
Filing Date 2017-09-21
First Publication Date 2018-02-01
Grant Date 2018-09-25
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Wiles, Jason Allan
  • Gadhachanda, Venkat Rao
  • Wang, Qiuping
  • Pais, Godwin
  • Hashimoto, Akihiro
  • Chen, Dawei
  • Wang, Xiangzhu
  • Agarwal, Atul
  • Deshpande, Milind
  • Phadke, Avinash S.

Abstract

32) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.

IPC Classes  ?

  • A61K 31/4025 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
  • A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
  • A61K 31/4427 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems
  • A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
  • A61K 31/4188 - 1,3-Diazoles condensed with heterocyclic ring systems, e.g. biotin, sorbinil
  • A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
  • A61K 31/4192 - 1,2,3-Triazoles
  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 471/04 - Ortho-condensed systems
  • C07D 513/04 - Ortho-condensed systems
  • C07F 9/572 - Five-membered rings
  • C07D 417/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07F 7/08 - Compounds having one or more C—Si linkages
  • C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 209/42 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
  • A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
  • C07B 59/00 - Introduction of isotopes of elements into organic compounds
  • C07D 209/14 - Radicals substituted by nitrogen atoms, not forming part of a nitro radical
  • C07D 209/40 - Nitrogen atoms, not forming part of a nitro radical, e.g. isatin semicarbazone
  • C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 487/14 - Ortho-condensed systems
  • C07D 491/113 - Spiro-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
  • A61K 31/404 - Indoles, e.g. pindolol
  • A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
  • A61K 31/4162 - 1,2-Diazoles condensed with heterocyclic ring systems
  • A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
  • A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
  • A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
  • A61K 31/549 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame having two or more nitrogen atoms in the same ring, e.g. hydrochlorothiazide
  • A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
  • C07D 495/04 - Ortho-condensed systems
  • A61K 31/683 - Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
  • C07D 413/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 403/08 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing alicyclic rings
  • C07D 487/04 - Ortho-condensed systems
  • C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
  • C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
  • C07F 5/02 - Boron compounds

62.

Ether compounds for treatment of complement mediated disorders

      
Application Number 15676411
Grant Number 10106563
Status In Force
Filing Date 2017-08-14
First Publication Date 2018-01-25
Grant Date 2018-10-23
Owner Achillion Pharmaecuticals, Inc. (USA)
Inventor
  • Wiles, Jason Allan
  • Gadhachanda, Venkat Rao
  • Pais, Godwin
  • Hashimoto, Akihiro
  • Wang, Qiuping
  • Chen, Dawei
  • Wang, Xiangzhu
  • Agarwal, Atul
  • Deshpande, Milind
  • Phadke, Avinash S.

Abstract

32) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.

IPC Classes  ?

  • C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • A61K 31/404 - Indoles, e.g. pindolol
  • C07F 9/572 - Five-membered rings
  • C07D 417/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07F 7/08 - Compounds having one or more C—Si linkages
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 209/42 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
  • C07D 513/04 - Ortho-condensed systems
  • A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
  • C07B 59/00 - Introduction of isotopes of elements into organic compounds
  • C07D 209/14 - Radicals substituted by nitrogen atoms, not forming part of a nitro radical
  • C07D 209/40 - Nitrogen atoms, not forming part of a nitro radical, e.g. isatin semicarbazone
  • C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 487/14 - Ortho-condensed systems
  • C07D 491/113 - Spiro-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
  • A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
  • A61K 31/4162 - 1,2-Diazoles condensed with heterocyclic ring systems
  • A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
  • A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
  • A61K 31/4188 - 1,3-Diazoles condensed with heterocyclic ring systems, e.g. biotin, sorbinil
  • A61K 31/4192 - 1,2,3-Triazoles
  • A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
  • A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
  • A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
  • A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61K 31/549 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame having two or more nitrogen atoms in the same ring, e.g. hydrochlorothiazide
  • A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
  • C07D 495/04 - Ortho-condensed systems
  • A61K 31/683 - Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
  • C07D 413/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 403/08 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing alicyclic rings
  • C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
  • C07D 487/04 - Ortho-condensed systems
  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
  • C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
  • C07F 5/02 - Boron compounds
  • C07D 471/04 - Ortho-condensed systems

63.

COMBINATION DRUG TREATMENT FOR HEPATITIS C INFECTION

      
Application Number US2017043352
Publication Number 2018/017994
Status In Force
Filing Date 2017-07-21
Publication Date 2018-01-25
Owner
  • JANSSEN PHARMACEUTICALS, INC. (USA)
  • ACHILLION PHARMACEUTICALS, INC. (USA)
Inventor
  • Beumont, Maria Gloria
  • Bijnens, Lieve
  • Blatt, Lawrence M.
  • Chanda, Sushmita Mukherjee
  • Fry, John
  • Jans, Eugene
  • Kakuda, Thomas Naoki
  • Mahadevan, Sivi
  • Mertens, Roel
  • Picchio, Gaston Rafael
  • Van Dijck, Alex
  • Van Remoortere, Peter
  • Apelian, David
  • Chen, Dawei
  • Deshpande, Milind
  • Hui, James
  • Phadke, Avinash

Abstract

A method for the treatment of hepatitis C infection genotype 1, 2, 4, 5, or 6 is provided comprising administering an effective amount of a combination of Compound (I), Compound (II), and Compound (III), or independently optionally their pharmaceutically acceptable salt, solvate or hydrate, optionally in a solid fixed dose composition.

IPC Classes  ?

64.

Compounds for treatment of complement mediated disorders

      
Application Number 15700550
Grant Number 10087203
Status In Force
Filing Date 2017-09-11
First Publication Date 2018-01-25
Grant Date 2018-10-02
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Wiles, Jason Allan
  • Phadke, Avinash S.
  • Wang, Xiangzhu
  • Chen, Dawei
  • Hashimoto, Akihiro
  • Gadhachanda, Venkat Rao
  • Pais, Godwin
  • Wang, Qiuping
  • Agarwal, Atul
  • Deshpande, Milind

Abstract

Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.

IPC Classes  ?

  • C07D 513/04 - Ortho-condensed systems
  • A61K 31/429 - Thiazoles condensed with heterocyclic ring systems
  • A61K 31/433 - Thiadiazoles
  • A61K 31/4162 - 1,2-Diazoles condensed with heterocyclic ring systems
  • C07F 9/572 - Five-membered rings
  • C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
  • C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
  • C07F 7/08 - Compounds having one or more C—Si linkages
  • C07F 5/02 - Boron compounds
  • C07D 495/04 - Ortho-condensed systems
  • C07D 487/14 - Ortho-condensed systems
  • C07D 487/04 - Ortho-condensed systems
  • C07D 471/04 - Ortho-condensed systems
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 417/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 413/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
  • C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 403/08 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing alicyclic rings
  • C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 209/42 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
  • C07D 209/40 - Nitrogen atoms, not forming part of a nitro radical, e.g. isatin semicarbazone
  • C07D 209/14 - Radicals substituted by nitrogen atoms, not forming part of a nitro radical
  • C07B 59/00 - Introduction of isotopes of elements into organic compounds
  • A61K 31/683 - Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
  • A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
  • A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
  • A61K 31/549 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame having two or more nitrogen atoms in the same ring, e.g. hydrochlorothiazide
  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
  • A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
  • A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
  • A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
  • A61K 31/4192 - 1,2,3-Triazoles
  • A61K 31/4188 - 1,3-Diazoles condensed with heterocyclic ring systems, e.g. biotin, sorbinil
  • A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
  • A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
  • A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
  • C07D 491/113 - Spiro-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
  • A61K 31/404 - Indoles, e.g. pindolol

65.

COMBINATION THERAPY REGIMEN FOR TREATMENT OF SELECTED HCV GENOTYPES

      
Application Number US2017043346
Publication Number 2018/017989
Status In Force
Filing Date 2017-07-21
Publication Date 2018-01-25
Owner
  • JANSSEN PHARMACEUTICALS, INC. (USA)
  • ACHILLION PHARMACEUTICALS, INC. (USA)
Inventor
  • Beumont, Maria, Gloria
  • Bijnens, Lieve
  • Blatt, Lawrence, M.
  • Chanda, Sushmita, Mukherjee
  • Fry, John
  • Jans, Eugene
  • Kakuda, Thomas, Naoki
  • Mahadevan, Sivi
  • Mertens, Roel
  • Picchio, Gaston, Rafael
  • Van Dijck, Alex
  • Van Remoortere, Peter
  • Apelian, David
  • Chen, Dawei
  • Deshpande, Milind
  • Hui, James
  • Phadke, Avinash

Abstract

A method for the treatment of hepatitis C infection genotype 1, 2, 4, 5, or 6, but not genotype 3 is provided comprising administering an effective amount of a combination of Compound (I), Compound (II), and Compound (III), or independently optionally their pharmaceutically acceptable salt, solvate or hydrate, optionally in a solid fixed dose composition.

IPC Classes  ?

  • A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
  • A61K 9/00 - Medicinal preparations characterised by special physical form

66.

TOGETHER, WE ARE C3G

      
Application Number 187639600
Status Registered
Filing Date 2018-01-08
Registration Date 2020-11-04
Owner Achillion Pharmaceuticals, Inc. (USA)
NICE Classes  ?
  • 41 - Education, entertainment, sporting and cultural services
  • 44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services

Goods & Services

(1) Educational services, namely, providing medical information about the treatment of kidney disease (2) Providing medical information in the field of the treatment of kidney diseases

67.

QUINAZOLINE AND INDOLE COMPOUNDS TO TREAT MEDICAL DISORDERS

      
Application Number US2017039587
Publication Number 2018/005552
Status In Force
Filing Date 2017-06-27
Publication Date 2018-01-04
Owner ACHILLION PHARMACEUTICALS, INC. (USA)
Inventor
  • Wiles, Jason Allan
  • Phadke, Avinash

Abstract

Compounds, methods of use, and processes for making inhibitors of Complement Factor B are provided.

IPC Classes  ?

  • A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
  • A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings

68.

Carbamate, ester, and ketone compounds for treatment of complement mediated disorders

      
Application Number 15638081
Grant Number 10370394
Status In Force
Filing Date 2017-06-29
First Publication Date 2017-10-19
Grant Date 2019-08-06
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Wiles, Jason Allan
  • Gadhachanda, Venkat Rao
  • Pais, Godwin
  • Hashimoto, Akihiro
  • Wang, Qiuping
  • Chen, Dawei
  • Wang, Xiangzhu
  • Agarwal, Atul
  • Deshpande, Milind
  • Phadke, Avinash S.

Abstract

32) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.

IPC Classes  ?

  • C07D 209/12 - Radicals substituted by oxygen atoms
  • C07D 209/30 - IndolesHydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07F 9/572 - Five-membered rings
  • C07D 209/42 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
  • C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 471/04 - Ortho-condensed systems
  • C07D 417/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07F 7/08 - Compounds having one or more C—Si linkages
  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 487/04 - Ortho-condensed systems
  • C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
  • C07D 403/08 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing alicyclic rings
  • C07D 413/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07F 5/02 - Boron compounds
  • C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
  • C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
  • A61K 31/404 - Indoles, e.g. pindolol
  • A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
  • A61K 31/4162 - 1,2-Diazoles condensed with heterocyclic ring systems
  • A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
  • A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
  • A61K 31/4188 - 1,3-Diazoles condensed with heterocyclic ring systems, e.g. biotin, sorbinil
  • A61K 31/4192 - 1,2,3-Triazoles
  • A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
  • A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
  • A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
  • A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61K 31/549 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame having two or more nitrogen atoms in the same ring, e.g. hydrochlorothiazide
  • A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
  • A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
  • A61K 31/683 - Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
  • C07B 59/00 - Introduction of isotopes of elements into organic compounds
  • C07D 209/14 - Radicals substituted by nitrogen atoms, not forming part of a nitro radical
  • C07D 209/40 - Nitrogen atoms, not forming part of a nitro radical, e.g. isatin semicarbazone
  • C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 487/14 - Ortho-condensed systems
  • C07D 491/113 - Spiro-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
  • C07D 495/04 - Ortho-condensed systems
  • C07D 513/04 - Ortho-condensed systems
  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 31/4045 - Indole-alkylaminesAmides thereof, e.g. serotonin, melatonin
  • A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
  • A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • C07D 209/44 - Iso-indolesHydrogenated iso-indoles
  • C07D 209/88 - CarbazolesHydrogenated carbazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the ring system
  • C07D 471/08 - Bridged systems

69.

Amide compounds for treatment of complement mediated disorders

      
Application Number 15638076
Grant Number 10428094
Status In Force
Filing Date 2017-06-29
First Publication Date 2017-10-19
Grant Date 2019-10-01
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Wiles, Jason Allan
  • Wang, Qiuping
  • Gadhachanda, Venkat Rao
  • Pais, Godwin
  • Hashimoto, Akihiro
  • Chen, Dawei
  • Wang, Xiangzhu
  • Agarwal, Atul
  • Deshpande, Milind
  • Phadke, Avinash S.

Abstract

32) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.

IPC Classes  ?

  • C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07F 9/572 - Five-membered rings
  • C07D 209/42 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 471/04 - Ortho-condensed systems
  • C07D 417/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07F 7/08 - Compounds having one or more C—Si linkages
  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 487/04 - Ortho-condensed systems
  • C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
  • C07D 403/08 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing alicyclic rings
  • C07D 413/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07F 5/02 - Boron compounds
  • C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
  • C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
  • A61K 31/404 - Indoles, e.g. pindolol
  • A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
  • A61K 31/4162 - 1,2-Diazoles condensed with heterocyclic ring systems
  • A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
  • A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
  • A61K 31/4188 - 1,3-Diazoles condensed with heterocyclic ring systems, e.g. biotin, sorbinil
  • A61K 31/4192 - 1,2,3-Triazoles
  • A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
  • A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
  • A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
  • A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61K 31/549 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame having two or more nitrogen atoms in the same ring, e.g. hydrochlorothiazide
  • A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
  • A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
  • A61K 31/683 - Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
  • C07B 59/00 - Introduction of isotopes of elements into organic compounds
  • C07D 209/14 - Radicals substituted by nitrogen atoms, not forming part of a nitro radical
  • C07D 209/40 - Nitrogen atoms, not forming part of a nitro radical, e.g. isatin semicarbazone
  • C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 487/14 - Ortho-condensed systems
  • C07D 491/113 - Spiro-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
  • C07D 495/04 - Ortho-condensed systems
  • C07D 513/04 - Ortho-condensed systems
  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 31/4045 - Indole-alkylaminesAmides thereof, e.g. serotonin, melatonin
  • A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
  • A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • C07D 209/12 - Radicals substituted by oxygen atoms
  • C07D 209/30 - IndolesHydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
  • C07D 209/44 - Iso-indolesHydrogenated iso-indoles
  • C07D 209/88 - CarbazolesHydrogenated carbazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the ring system
  • C07D 471/08 - Bridged systems

70.

Phosphonate compounds for treatment of complement mediated disorders

      
Application Number 15607120
Grant Number 10100072
Status In Force
Filing Date 2017-05-26
First Publication Date 2017-09-14
Grant Date 2018-10-16
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Wiles, Jason Allan
  • Hashimoto, Akihiro
  • Gadhachanda, Venkat Rao
  • Pais, Godwin
  • Wang, Qiuping
  • Chen, Dawei
  • Wang, Xiangzhu
  • Agarwal, Atul
  • Deshpande, Milind
  • Phadke, Avinash

Abstract

32) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.

IPC Classes  ?

  • C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
  • C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
  • C07F 9/572 - Five-membered rings
  • C07F 7/08 - Compounds having one or more C—Si linkages
  • C07F 5/02 - Boron compounds
  • C07B 59/00 - Introduction of isotopes of elements into organic compounds
  • C07D 495/04 - Ortho-condensed systems
  • A61K 31/683 - Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
  • A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
  • A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole

71.

Amino compounds for treatment of complement mediated disorders

      
Application Number 15463701
Grant Number 10189869
Status In Force
Filing Date 2017-03-20
First Publication Date 2017-07-06
Grant Date 2019-01-29
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Gadhachanda, Venkat Rao
  • Hashimoto, Akihiro
  • Pais, Godwin
  • Wang, Qiuping
  • Chen, Dawei
  • Wang, Xiangzhu
  • Agarwal, Atul
  • Deshpande, Milind
  • Wiles, Jason Allan
  • Phadke, Avinash S.

Abstract

32) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.

IPC Classes  ?

  • A61K 31/416 - 1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
  • C07F 9/572 - Five-membered rings
  • C07D 209/42 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
  • C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 471/04 - Ortho-condensed systems
  • C07D 417/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07F 7/08 - Compounds having one or more C—Si linkages
  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 487/04 - Ortho-condensed systems
  • C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
  • C07D 403/08 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing alicyclic rings
  • C07D 413/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07F 5/02 - Boron compounds
  • C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
  • C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
  • A61K 31/404 - Indoles, e.g. pindolol
  • A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
  • A61K 31/4162 - 1,2-Diazoles condensed with heterocyclic ring systems
  • A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
  • A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
  • A61K 31/4188 - 1,3-Diazoles condensed with heterocyclic ring systems, e.g. biotin, sorbinil
  • A61K 31/4192 - 1,2,3-Triazoles
  • A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
  • A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
  • A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
  • A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61K 31/549 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame having two or more nitrogen atoms in the same ring, e.g. hydrochlorothiazide
  • A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
  • A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
  • A61K 31/683 - Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
  • C07B 59/00 - Introduction of isotopes of elements into organic compounds
  • C07D 209/14 - Radicals substituted by nitrogen atoms, not forming part of a nitro radical
  • C07D 209/40 - Nitrogen atoms, not forming part of a nitro radical, e.g. isatin semicarbazone
  • C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 487/14 - Ortho-condensed systems
  • C07D 491/113 - Spiro-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
  • C07D 495/04 - Ortho-condensed systems
  • C07D 513/04 - Ortho-condensed systems
  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 31/4045 - Indole-alkylaminesAmides thereof, e.g. serotonin, melatonin
  • A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
  • A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • C07D 209/12 - Radicals substituted by oxygen atoms
  • C07D 209/30 - IndolesHydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
  • C07D 209/44 - Iso-indolesHydrogenated iso-indoles
  • C07D 209/88 - CarbazolesHydrogenated carbazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the ring system
  • C07D 471/08 - Bridged systems

72.

Substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes useful for treating HCV infections

      
Application Number 15437117
Grant Number 09833440
Status In Force
Filing Date 2017-02-20
First Publication Date 2017-06-08
Grant Date 2017-12-05
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Wiles, Jason Allan
  • Wang, Qiuping
  • Hashimoto, Akihiro
  • Pais, Godwin
  • Wang, Xiangzhu
  • Gadhachanda, Venkat
  • Phadke, Avinash
  • Deshpande, Milind
  • Chen, Dawei

Abstract

useful as antiviral agents. In certain embodiments disclosed herein M is a group —P-A-P— where A is Certain substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. Pharmaceutical compositions/and combinations containing one or more substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes and a pharmaceutically acceptable carrier are also provided by this disclosure. Methods for treating viral infections, including Hepatitis C viral infections are provided by the disclosure.

IPC Classes  ?

  • A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 471/08 - Bridged systems
  • C07D 491/10 - Spiro-condensed systems
  • C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
  • A61K 31/439 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
  • A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
  • A61K 31/555 - Heterocyclic compounds containing heavy metals, e.g. hemin, hematin, melarsoprol
  • C07F 17/02 - Metallocenes of metals of Groups 8, 9 or 10 of the Periodic Table
  • A61K 31/422 - Oxazoles not condensed and containing further heterocyclic rings
  • A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
  • A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
  • C07D 453/06 - Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing iso-quinuclidine ring systems
  • C07D 491/113 - Spiro-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
  • C07F 15/02 - Iron compounds
  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 9/20 - Pills, lozenges or tablets
  • C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • C07D 209/42 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
  • C07F 5/02 - Boron compounds

73.

Miscellaneous Design

      
Application Number 1339891
Status Registered
Filing Date 2017-01-05
Registration Date 2017-01-05
Owner Achillion Pharmaceuticals, Inc. (USA)
NICE Classes  ? 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

Pharmaceutical preparations for the treatment of immunomodulatory diseases, conditions and disorders, immune system diseases, conditions and disorders, complement-mediated diseases and disorders, autoimmune diseases and disorders, renal diseases and disorders, blood system diseases and disorders and infectious diseases and disorders.

74.

ACHILLION

      
Application Number 1339233
Status Registered
Filing Date 2017-01-05
Registration Date 2017-01-05
Owner Achillion Pharmaceuticals, Inc. (USA)
NICE Classes  ? 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

Pharmaceutical preparations for the treatment of immunomodulatory diseases, conditions and disorders, immune system diseases, conditions and disorders, complement-mediated diseases and disorders, autoimmune diseases and disorders, renal diseases and disorders, blood system diseases and disorders and infectious diseases and disorders.

75.

COMBINATION THERAPY REGIMEN FOR TREATMENT OF HCV

      
Application Number US2016054561
Publication Number 2017/059147
Status In Force
Filing Date 2016-09-29
Publication Date 2017-04-06
Owner
  • JANSSEN PHARMACEUTICALS, INC. (USA)
  • ACHILLION PHARMACEUTICALS, INC. (USA)
Inventor
  • Beumont, Maria Gloria
  • Bijnens, Lieve
  • Blatt, Lawrence, M.
  • Chanda, Sushmita, Mukherjee
  • Fry, John
  • Jans, Eugene
  • Kakuda, Thomas, Naoki
  • Mahadevan, Sivi
  • Mertens, Roel
  • Picchio, Gaston, Rafael
  • Van Dijck, Alex
  • Van Remoortere, Peter
  • Apelian, David
  • Chen, Dawei
  • Deshpande, Milind
  • Hui, James
  • Phadke, Avinash

Abstract

A composition, including a fixed dose composition, comprising Compound (I), Compound (II), and Compound (III) for the treatment of hepatitis C, and methods of manufacture thereof.

IPC Classes  ?

  • A61P 31/14 - Antivirals for RNA viruses
  • A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
  • A61K 31/522 - Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir

76.

COMBINATION THERAPY REGIMEN FOR TREATMENT OF HCV

      
Application Number 15281050
Status Pending
Filing Date 2016-09-29
First Publication Date 2017-03-30
Owner
  • JANSSEN PHARMACEUTICALS, INC. (USA)
  • ACHILLION PHARMACEUTICALS, INC. (USA)
Inventor
  • Beumont, Maria Gloria
  • Bijnens, Lieve
  • Blatt, Lawrence M.
  • Chanda, Sushmita Mukherjee
  • Fry, John
  • Jans, Eugene
  • Kakuda, Thomas Naoki
  • Mahadevan, Sivi
  • Mertens, Roel
  • Picchio, Gaston Rafael
  • Van Dijck, Alex
  • Van Remoortere, Peter
  • Apelian, David
  • Chen, Dawei
  • Deshphande, Milind
  • Hui, James
  • Phadke, Avinash

Abstract

A composition, including a fixed dose composition, comprising Compound (I), Compound (II), and Compound (III) for the treatment of hepatitis C, and methods of manufacture thereof.

IPC Classes  ?

  • A61K 31/7072 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
  • A61K 9/10 - DispersionsEmulsions
  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
  • A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles

77.

Aryl, heteroaryl, and heterocyclic compounds for treatment of medical disorders

      
Application Number 15247399
Grant Number 10011612
Status In Force
Filing Date 2016-08-25
First Publication Date 2017-03-09
Grant Date 2018-07-03
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Wiles, Jason Allan
  • Phadke, Avinash S.
  • Deshpande, Milind
  • Agarwal, Atul
  • Chen, Dawei
  • Gadhachanda, Venkat Rao
  • Hashimoto, Akihiro
  • Pais, Godwin
  • Wang, Qiuping
  • Wang, Xiangzhu

Abstract

32) are provided. The inhibitors of Factor D described herein reduce the excessive activation of complement.

IPC Classes  ?

  • C07D 513/04 - Ortho-condensed systems
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 471/04 - Ortho-condensed systems
  • C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 487/04 - Ortho-condensed systems
  • C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
  • C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 495/04 - Ortho-condensed systems
  • C07D 493/04 - Ortho-condensed systems

78.

AMINO COMPOUNDS FOR TREATMENT OF MEDICAL DISORDERS

      
Application Number US2016048693
Publication Number 2017/035351
Status In Force
Filing Date 2016-08-25
Publication Date 2017-03-02
Owner ACHILLION PHARMACEUTICALS, INC. (USA)
Inventor
  • Wiles, Jason, Allan
  • Phadke, Avinash, S.
  • Deshpande, Milind
  • Agarwal, Atul
  • Chen, Dawei
  • Gadhachanda, Venkat, Rao
  • Hashimoto, Akihiro
  • Pais, Godwin
  • Wang, Qiuping
  • Wang, Xiangzhu

Abstract

Compounds, methods of use, and processes for making inhibitors of complement Factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is an amino substituent (R32) are provided. The inhibitors of Factor D described herein reduce the excessive activation of complement.

IPC Classes  ?

  • A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
  • A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
  • A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 471/04 - Ortho-condensed systems

79.

CARBAMATE, ESTER, AND KETONE COMPOUNDS FOR TREATMENT OF MEDICAL DISORDERS

      
Application Number US2016048695
Publication Number 2017/035352
Status In Force
Filing Date 2016-08-25
Publication Date 2017-03-02
Owner ACHILLION PHARMACEUTICALS, INC. (USA)
Inventor
  • Wiles, Jason, Allan
  • Phadke, Avinash, S.
  • Deshpande, Milind
  • Agarwal, Atul
  • Chen, Dawei
  • Gadhachanda, Venkat Rao
  • Hashimoto, Akihiro
  • Pais, Godwin
  • Wang, Qiuping
  • Wang, Xiangzhu

Abstract

Compounds, methods of use, and processes for making inhibitors of complement Factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is a carbamate, ester, or ketone substituent (R32) are provided. The inhibitors of Factor D described herein reduce the excessive activation of complement.

IPC Classes  ?

  • A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
  • A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
  • A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 471/04 - Ortho-condensed systems

80.

ARYL, HETEROARYL, AND HETEROCYCLIC COMPOUNDS FOR TREATMENT OF MEDICAL DISORDERS

      
Application Number US2016048696
Publication Number 2017/035353
Status In Force
Filing Date 2016-08-25
Publication Date 2017-03-02
Owner ACHILLION PHARMACEUTICALS, INC. (USA)
Inventor
  • Wiles, Jason, Allan
  • Phadke, Avinash, S.
  • Deshpande, Milind
  • Agarwal, Atul
  • Chen, Dawei
  • Gadhachanda, Venkat, Rao
  • Hashimoto, Akihiro
  • Pais, Godwin
  • Wang, Qiuping
  • Wang, Xiangzhu

Abstract

Compounds, methods of use, and processes for making inhibitors of complement Factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is an aryl, heteroaryl or heterocycle (R32) are provided. The inhibitors of Factor D described herein reduce the excessive activation of complement.

IPC Classes  ?

  • A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
  • A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
  • A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 471/04 - Ortho-condensed systems

81.

ETHER COMPOUNDS FOR TREATMENT OF MEDICAL DISORDERS

      
Application Number US2016048701
Publication Number 2017/035355
Status In Force
Filing Date 2016-08-25
Publication Date 2017-03-02
Owner ACHILLION PHARMACEUTICALS, INC. (USA)
Inventor
  • Wiles, Jason, Allan
  • Phadke, Avinash, S.
  • Deshpande, Milind
  • Agarwal, Atul
  • Chen, Dawei
  • Gadhachanda, Venkat, Rao
  • Hashimoto, Akihiro
  • Pais, Godwin
  • Wang, Qiuping
  • Wang, Xiangzhu

Abstract

Compounds, methods of use, and processes for making inhibitors of complement Factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is an ether substituent (R32) are provided. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduce the excessive activation of complement.

IPC Classes  ?

  • A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
  • A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
  • A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 471/04 - Ortho-condensed systems

82.

COMPOUNDS FOR THE TREATMENT OF MEDICAL DISORDERS

      
Application Number US2016048707
Publication Number 2017/035360
Status In Force
Filing Date 2016-08-25
Publication Date 2017-03-02
Owner ACHILLION PHARMACEUTICALS, INC. (USA)
Inventor
  • Wiles, Jason, Allan
  • Phadke, Avinash, S.
  • Deshpande, Milind
  • Agarwal, Atul
  • Chen, Dawei
  • Gadhachanda, Venkat, Rao
  • Hashimoto, Akihiro
  • Pais, Godwin
  • Wang, Qiuping
  • Wang, Xiangzhu

Abstract

Compounds, methods of use, and processes for making inhibitors of complement Factor D comprising Formula (I), or a pharmaceutically acceptable salt or composition thereof The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduce the excessive activation of complement.

IPC Classes  ?

  • A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
  • A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
  • A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 471/04 - Ortho-condensed systems

83.

COMPOUNDS FOR TREATMENT OF IMMUNE AND INFLAMMATORY DISORDERS

      
Application Number US2016048787
Publication Number 2017/035408
Status In Force
Filing Date 2016-08-25
Publication Date 2017-03-02
Owner ACHILLION PHARMACEUTICALS, INC. (USA)
Inventor
  • Wiles, Jason, Allan
  • Phadke, Avinash, S.
  • Deshpande, Milind
  • Agarwal, Atul
  • Chen, Dawei
  • Gadhachanda, Venkat, Rao
  • Hashimoto, Akihiro
  • Pais, Godwin
  • Wang, Qiuping
  • Wang, Xiangzhu
  • Greenlee, William

Abstract

Compounds, methods of use, and processes for making inhibitors of complement Factor D are provided comprising Formula I, I" and I'" or a pharmaceutically acceptable salt or composition thereof. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduces the excessive activation of complement.

IPC Classes  ?

  • A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
  • A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
  • A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 471/04 - Ortho-condensed systems

84.

ETHER COMPOUNDS FOR TREATMENT OF IMMUNE AND INFLAMMATORY DISORDERS

      
Application Number US2016048793
Publication Number 2017/035411
Status In Force
Filing Date 2016-08-25
Publication Date 2017-03-02
Owner ACHILLION PHARMACEUTICALS, INC. (USA)
Inventor
  • Wiles, Jason Allan
  • Phadke, Avinash S.
  • Deshpande, Milind
  • Agarwal, Atul
  • Chen, Dawei
  • Gadhachanda, Venkat Rao
  • Hashimoto, Akihiro
  • Pais, Godwin
  • Wang, Qiuping
  • Wang, Xiangzhu
  • Greenlee, William

Abstract

Compounds, methods of use, and processes for making inhibitors of complement Factor D are provided comprising Formula I, I" and I‴ or a pharmaceutically acceptable salt or composition thereof. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduces the excessive activation of complement.

IPC Classes  ?

  • A01N 43/00 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds

85.

PHOSPHONATE COMPOUNDS FOR TREATMENT OF IMMUNE AND INFLAMMATORY DISORDERS

      
Application Number US2016048799
Publication Number 2017/035417
Status In Force
Filing Date 2016-08-25
Publication Date 2017-03-02
Owner ACHILLION PHARMACEUTICALS, INC. (USA)
Inventor
  • Wiles, Jason, Allan
  • Phadke, Avinash, S.
  • Deshpande, Milind
  • Agarwal, Atul
  • Chen, Dawei
  • Gadhachanda, Venkat, Rao
  • Hashimoto, Akihiro
  • Pais, Godwin
  • Wang, Qiuping
  • Wang, Xiangzhu
  • Greenlee, William

Abstract

Compounds, methods of use, and processes for making inhibitors of complement Factor D are provided comprising Formula I, I" and I''' or a pharmaceutically acceptable salt or composition thereof. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduce the excessive activation of complement.

IPC Classes  ?

  • A61K 31/66 - Phosphorus compounds
  • C07D 487/04 - Ortho-condensed systems
  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings

86.

DISUBSTITUTED COMPOUNDS FOR TREATMENT OF IMMUNE AND INFLAMMATORY DISORDERS

      
Application Number US2016048800
Publication Number 2017/035418
Status In Force
Filing Date 2016-08-25
Publication Date 2017-03-02
Owner ACHILLION PHARMACEUTICALS, INC. (USA)
Inventor
  • Wiles, Jason, Allan
  • Phadke, Avinash, S.
  • Deshpande, Milind
  • Agarwal, Atul
  • Chen, Dawei
  • Gadhachanda, Venkat, Rao
  • Hashimoto, Akihiro
  • Pais, Godwin
  • Wang, Qiuping
  • Wang, Xiangzhu
  • Greenlee, William

Abstract

Compounds, methods of use, and processes for making inhibitors of complement Factor D are provided comprising Formula I, I" and I"' or a pharmaceutically acceptable salt or composition thereof. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduce the excessive activation of complement.

IPC Classes  ?

  • A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
  • A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
  • A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 471/04 - Ortho-condensed systems

87.

Ether compounds for treatment of medical disorders

      
Application Number 15247410
Grant Number 10385097
Status In Force
Filing Date 2016-08-25
First Publication Date 2017-03-02
Grant Date 2019-08-20
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Wiles, Jason Allan
  • Phadke, Avinash S.
  • Deshpande, Milind
  • Agarwal, Atul
  • Chen, Dawei
  • Gadhachanda, Venkat Rao
  • Hashimoto, Akihiro
  • Pais, Godwin
  • Wang, Qiuping
  • Wang, Xiangzhu

Abstract

32) are provided. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduce the excessive activation of complement.

IPC Classes  ?

  • C07K 5/06 - Dipeptides
  • C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
  • C07K 5/078 - Dipeptides the first amino acid being heterocyclic, e.g. Pro, His, Trp
  • C07F 9/572 - Five-membered rings
  • C07K 5/02 - Peptides having up to four amino acids in a fully defined sequenceDerivatives thereof containing at least one abnormal peptide link
  • C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 209/12 - Radicals substituted by oxygen atoms

88.

Phosphonate compounds for treatment of medical disorders

      
Application Number 15247424
Grant Number 10000516
Status In Force
Filing Date 2016-08-25
First Publication Date 2017-03-02
Grant Date 2018-06-19
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Wiles, Jason Allan
  • Phadke, Avinash S.
  • Deshpande, Milind
  • Agarwal, Atul
  • Chen, Dawei
  • Gadhachanda, Venkat Rao
  • Hashimoto, Akihiro
  • Pais, Godwin
  • Wang, Qiuping
  • Wang, Xiangzhu

Abstract

32) are provided. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduces the excessive activation of complement.

IPC Classes  ?

  • C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
  • C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system

89.

Compounds for the treatment of medical disorders

      
Application Number 15247429
Grant Number 10092584
Status In Force
Filing Date 2016-08-25
First Publication Date 2017-03-02
Grant Date 2018-10-09
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Wiles, Jason Allan
  • Phadke, Avinash S.
  • Deshpande, Milind
  • Agarwal, Atul
  • Chen, Dawei
  • Gadhachanda, Venkat Rao
  • Hashimoto, Akihiro
  • Pais, Godwin
  • Wang, Qiuping
  • Wang, Xiangzhu

Abstract

Compounds, methods of use, and processes for making inhibitors of complement Factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduce the excessive activation of complement.

IPC Classes  ?

  • A61K 31/4162 - 1,2-Diazoles condensed with heterocyclic ring systems
  • A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
  • A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
  • A61K 31/695 - Silicon compounds
  • A61K 31/404 - Indoles, e.g. pindolol
  • A61K 31/4155 - 1,2-Diazoles not condensed and containing further heterocyclic rings
  • A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
  • A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
  • A61K 31/4192 - 1,2,3-Triazoles
  • A61K 31/422 - Oxazoles not condensed and containing further heterocyclic rings
  • A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
  • A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
  • A61K 31/4745 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
  • A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
  • A61K 31/498 - Pyrazines or piperazines ortho- or peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61K 31/538 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
  • A61K 31/549 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame having two or more nitrogen atoms in the same ring, e.g. hydrochlorothiazide
  • A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole

90.

Amide compounds for treatment of medical disorders

      
Application Number 15247440
Grant Number 10138225
Status In Force
Filing Date 2016-08-25
First Publication Date 2017-03-02
Grant Date 2018-11-27
Owner Achillion Pharmaceuticals, Inc. (USA)
Inventor
  • Wiles, Jason Allan
  • Phadke, Avinash S.
  • Deshpande, Milind
  • Agarwal, Atul
  • Chen, Dawei
  • Gadhachanda, Venkat Rao
  • Hashimoto, Akihiro
  • Pais, Godwin
  • Wang, Qiuping
  • Wang, Xiangzhu

Abstract

32) are provided. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein are capable of reducing the excessive activation of complement.

IPC Classes  ?

  • A61K 31/416 - 1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
  • A61K 31/404 - Indoles, e.g. pindolol
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 471/08 - Bridged systems
  • C07D 513/04 - Ortho-condensed systems
  • C07D 495/04 - Ortho-condensed systems

91.

ALKYNE COMPOUNDS FOR TREATMENT OF MEDICAL DISORDERS

      
Application Number US2016048688
Publication Number 2017/035348
Status In Force
Filing Date 2016-08-25
Publication Date 2017-03-02
Owner ACHILLION PHARMACEUTICALS, INC. (USA)
Inventor
  • Wiles, Jason, Allan
  • Phadke, Avinash, S.
  • Deshpande, Milind
  • Agarwal, Atul
  • Chen, Dawei
  • Gadhachanda, Venkat, Rao
  • Hashimoto, Akihiro
  • Pais, Godwin
  • Wang, Qiuping
  • Wang, Xiangzhu

Abstract

Compounds, methods of use, and processes for making inhibitors of complement Factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is alkyne substituent (R32) are provided. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein can reduce the excessive activation of complement.

IPC Classes  ?

  • A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
  • A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
  • A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 471/04 - Ortho-condensed systems

92.

AMIDE COMPOUNDS FOR TREATMENT OF MEDICAL DISORDERS

      
Application Number US2016048690
Publication Number 2017/035349
Status In Force
Filing Date 2016-08-25
Publication Date 2017-03-02
Owner ACHILLION PHARMACEUTICALS, INC. (USA)
Inventor
  • Wiles, Jason, Allan
  • Phadke, Avinash, S.
  • Deshpande, Milind
  • Agarwal, Atul
  • Chen, Dawei
  • Gadhachanda, Venkat, Rao
  • Hashimoto, Akihiro
  • Pais, Godwin
  • Wang, Qiuping
  • Wang, Xiangzhu

Abstract

Compounds, methods of use, and processes for making inhibitors of complement Factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is an amide substituent (R32) are provided. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein are capable of reducing the excessive activation of complement.

IPC Classes  ?

  • A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
  • A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
  • A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 471/04 - Ortho-condensed systems

93.

PHOSPHONATE COMPOUNDS FOR TREATMENT OF MEDICAL DISORDERS

      
Application Number US2016048704
Publication Number 2017/035357
Status In Force
Filing Date 2016-08-25
Publication Date 2017-03-02
Owner ACHILLION PHARMACEUTICALS, INC. (USA)
Inventor
  • Wang, Qiuping
  • Gadhachanda, Venkat, Rao
  • Wang, Xiangzhu
  • Deshpande, Milind
  • Pais, Godwin
  • Chen, Dawei
  • Wiles, Jason, Allan
  • Hashimoto, Akihiro
  • Phadke, Avinash, S.
  • Agarwal, Atul

Abstract

Compounds, methods of use, and processes for making inhibitors of complement Factor D comprising Formula (I), or a pharmaceutically acceptable salt or composition thereof wherein R¹² or R¹³ on the A group is a phosphonate substituent (R³²) are provided. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduces the excessive activation of complement.

IPC Classes  ?

  • C07F 9/40 - Esters thereof
  • C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • A61K 31/401 - ProlineDerivatives thereof, e.g. captopril

94.

DISUBSTITUTED COMPOUNDS FOR THE TREATMENT OF MEDICAL DISORDERS

      
Application Number US2016048709
Publication Number 2017/035361
Status In Force
Filing Date 2016-08-25
Publication Date 2017-03-02
Owner ACHILLION PHARMACEUTICALS, INC. (USA)
Inventor
  • Wiles, Jason, Allan
  • Phadke, Avinash, S.
  • Deshpande, Millind
  • Agarwal, Atul
  • Chen, Dawei
  • Gadhachanda, Venkat, Rao
  • Hashimoto, Akihiro
  • Pais, Godwin
  • Wang, Qiuping
  • Wang, Xiangzhu

Abstract

Compounds, methods of use, and processes for making inhibitors of complement Factor D are provided comprising Formula (I), or a pharmaceutically acceptable salt or composition thereof. The inhibitors of Factor D described herein reduce the excessive activation of complement, and are useful to treat disorders mediated by the complement system.

IPC Classes  ?

  • A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
  • A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
  • A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 471/04 - Ortho-condensed systems

95.

USE OF COMPLEMENT PATHWAY INHIBITOR COMPOUNDS TO MITIGATE ADOPTIVE T-CELL THERAPY ASSOCIATED ADVERSE IMMUNE RESPONSES

      
Application Number US2016048710
Publication Number 2017/035362
Status In Force
Filing Date 2016-08-25
Publication Date 2017-03-02
Owner ACHILLION PHARMACEUTICALS, INC. (USA)
Inventor
  • Huang, Mingjun
  • Fisherman, Jason

Abstract

This invention provides methods for treating adoptive T-cell therapy-associated adverse inflammatory responses, for example, cytokine release syndrome and tumor lysis syndrome, using complement pathway inhibitor compounds.

IPC Classes  ?

  • A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
  • C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
  • A61K 31/4025 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim

96.

AMIDE COMPOUNDS FOR TREATMENT OF IMMUNE AND INFLAMMATORY DISORDERS

      
Application Number US2016048779
Publication Number 2017/035401
Status In Force
Filing Date 2016-08-25
Publication Date 2017-03-02
Owner ACHILLION PHARMACEUTICALS, INC. (USA)
Inventor
  • Wiles, Jason, Allan
  • Phadke, Avinash, S.
  • Deshpande, Milind
  • Agarwal, Atul
  • Chen, Dawei
  • Gadhachanda, Venkat, Rao
  • Hashimoto, Akihiro
  • Pais, Godwin
  • Wang, Qiuping
  • Wang, Xiangzhu
  • Greenlee, William

Abstract

Compounds, methods of use, and processes for making inhibitors of complement Factor D are provided comprising Formula I, I" and I"' or a pharmaceutically acceptable salt or composition thereof. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduces the excessive activation of complement.

IPC Classes  ?

  • A01N 57/00 - Biocides, pest repellants or attractants, or plant growth regulators containing organic phosphorus compounds

97.

AMINO COMPOUNDS FOR TREATMENT OF IMMUNE AND INFLAMMATORY DISORDERS

      
Application Number US2016048783
Publication Number 2017/035405
Status In Force
Filing Date 2016-08-25
Publication Date 2017-03-02
Owner ACHILLION PHARMACEUTICALS, INC. (USA)
Inventor
  • Wiles, Jason, Allan
  • Phadke, Avinash, S.
  • Deshpande, Milind
  • Agarwal, Atul
  • Chen, Dawei
  • Gadhachanda, Venkat, Rao
  • Hashimoto, Akihiro
  • Pais, Godwin
  • Wang, Qiuping
  • Wang, Xiangzhu
  • Greenlee, William

Abstract

Compounds, methods of use, and processes for making inhibitors of complement Factor D are provided comprising Formula I, I" and Γ" or a pharmaceutically acceptable salt or composition thereof. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduces the excessive activation of complement.

IPC Classes  ?

  • A01N 57/00 - Biocides, pest repellants or attractants, or plant growth regulators containing organic phosphorus compounds

98.

ARYL, HETEROARYL, AND HETEROCYCLIC COMPOUNDS FOR TREATMENT OF IMMUNE AND INFLAMMATORY DISORDERS

      
Application Number US2016048788
Publication Number 2017/035409
Status In Force
Filing Date 2016-08-25
Publication Date 2017-03-02
Owner ACHILLION PHARMACEUTICALS, INC. (USA)
Inventor
  • Wiles, Jason, Allan
  • Phadke, Avinash, S.
  • Deshpande, Milind
  • Agarwal, Atul
  • Chen, Dawei
  • Gadhachanda, Venkat, Rao
  • Hashimoto, Akihiro
  • Pais, Godwin
  • Wang, Qiuping
  • Wang, Xiangzhu
  • Greenlee, William

Abstract

Compounds, methods of use, and processes for making inhibitors of complement Factor D are provided comprising Formula I, I" and I'" or a pharmaceutically acceptable salt or composition thereof. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduces the excessive activation of complement.

IPC Classes  ?

  • A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
  • A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
  • A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 471/04 - Ortho-condensed systems

99.

CARBAMATE, ESTER, AND KETONE COMPOUNDS FOR TREATMENT OF IMMUNE AND INFLAMMATORY DISORDERS

      
Application Number US2016048795
Publication Number 2017/035413
Status In Force
Filing Date 2016-08-25
Publication Date 2017-03-02
Owner ACHILLION PHARMACEUTICALS, INC. (USA)
Inventor
  • Wiles, Jason, Allan
  • Phadke, Avinash, S.
  • Deshpande, Milind
  • Agarwal, Atul
  • Chen, Dawei
  • Gadhachanda, Venkat, Rao
  • Hashimoto, Akihiro
  • Pais, Godwin
  • Wang, Qiuping
  • Wang, Xiangzhu
  • Greenlee, William

Abstract

Compounds, methods of use, and processes for making inhibitors of complement Factor D are provided comprising Formula I, I" and I'" or a pharmaceutically acceptable salt or composition thereof. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduce the excessive activation of complement.

IPC Classes  ?

  • A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
  • A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
  • A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 471/04 - Ortho-condensed systems

100.

ALKYNE COMPOUNDS FOR TREATMENT OF IMMUNE AND INFLAMMATORY DISORDERS

      
Application Number US2016048797
Publication Number 2017/035415
Status In Force
Filing Date 2016-08-25
Publication Date 2017-03-02
Owner ACHILLION PHARMACEUTICALS, INC. (USA)
Inventor
  • Wiles, Jason, Allan
  • Phadke, Avinash, S.
  • Deshpande, Milind
  • Agarwal, Atul
  • Chen, Dawei
  • Gadhachanda, Venkat, Rao
  • Hashimoto, Akihiro
  • Pais, Godwin
  • Wang, Qiuping
  • Wang, Xiangzhu
  • Greenlee, William

Abstract

Compounds, methods of use, and processes for making inhibitors of complement Factor D are provided comprising Formula I, I" and I'" or a pharmaceutically acceptable salt or composition thereof. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduce the excessive activation of complement.

IPC Classes  ?

  • A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
  • A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
  • A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
  • C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
  • C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
  • C07D 471/04 - Ortho-condensed systems
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