Auspex Pharmaceuticals, Inc.

United States of America

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        Patent 186
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        United States 59
        Canada 13
Date
2024 6
2023 7
2022 7
2021 6
2020 6
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IPC Class
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 36
A61K 9/20 - Pills, lozenges or tablets 26
A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia 26
A61K 31/473 - QuinolinesIsoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines 21
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca 20
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NICE Class
05 - Pharmaceutical, veterinary and sanitary products 5
44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services 1
Status
Pending 18
Registered / In Force 174
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1.

MULTIPARTICULATE DOSAGE FORMS COMPRISING DEUTETRABENAZINE

      
Application Number 18692074
Status Pending
Filing Date 2022-09-16
First Publication Date 2024-11-14
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Joshi, Mayank
  • Pandita, Sandeep
  • Patel, Divyang
  • Pattanayek, Soumen
  • Shah, Parag

Abstract

Provided herein are modified release multiparticulate dosage forms containing deutetrabenazine for use in the treatment of, e.g., hyperkinetic movement disorders. The dosage forms are easily administered to a subject on a once-daily or twice daily basis, and provide a safe and effective pharmacokinetic profile.

IPC Classes  ?

  • A61K 9/50 - Microcapsules
  • 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

2.

Formulations and Pharmacokinetics of Deuterated Benzoquinoline Inhibitors of Vesicular Monoamine Transporter 2

      
Application Number 18402393
Status Pending
Filing Date 2024-01-02
First Publication Date 2024-11-07
Owner Auspex Pharmaceuticals, Inc. (USA)
Inventor
  • Sommer, Andreas
  • Zhang, Chengzhi
  • Carter, John
  • Arthur, John Charles
  • Bradbury, Margaret
  • Gant, Thomas George
  • Shahbaz, Manouchehr

Abstract

The present invention relates to new pharmaceutical compositions comprising benzoquinoline compounds, and methods to inhibit vesicular monoamine transporter 2 (VMAT2) activity in a subject for the treatment of chronic hyperkinetic movement disorders.

IPC Classes  ?

  • A61K 31/473 - QuinolinesIsoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 9/16 - AgglomeratesGranulatesMicrobeadlets
  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 9/28 - DrageesCoated pills or tablets
  • A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
  • A61K 9/50 - Microcapsules
  • 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 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • C07D 455/06 - Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing quinolizine ring systems directly condensed with at least one six-membered carbocyclic ring, e.g. protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing a quinolizine ring system condensed with only one six-membered carbocyclic ring, e.g. julolidine containing benzo [a] quinolizine ring systems

3.

METHODS FOR THE TREATMENT OF ABNORMAL INVOLUNTARY MOVEMENT DISORDERS

      
Application Number 18677401
Status Pending
Filing Date 2024-05-29
First Publication Date 2024-09-26
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Stamler, David
  • Huang, Michael

Abstract

Disclosed herein are new dosage regimens for deuterium-substituted benzoquinoline compounds, and methods for the treatment of abnormal muscular activity, movement disorders, and related conditions.

IPC Classes  ?

  • A61K 31/473 - QuinolinesIsoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 31/4375 - 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 six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
  • 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 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia

4.

OSMOTIC DOSAGE FORMS COMPRISING DEUTETRABENAZINE AND METHODS OF USE THEREOF

      
Application Number 18609809
Status Pending
Filing Date 2024-03-19
First Publication Date 2024-09-19
Owner Auspex Pharmaceuticals, Inc. (USA)
Inventor
  • Shah, Parag
  • Joshi, Mayank
  • Pattanayek, Soumen
  • Patel, Divyang
  • Pandita, Sandeep

Abstract

Provided herein are osmotic dosage forms containing deutetrabenazine for use in the treatment of, e.g., hyperkinetic movement disorders. When orally administered to a subject on a once-daily basis, the dosage forms provide a favorable pharmacokinetic profile for the active agent indicating treatment efficacy over an extended period of time.

IPC Classes  ?

  • A61K 9/24 - Layered or laminated unitary dosage forms
  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 9/20 - Pills, lozenges or tablets
  • 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

5.

BENZOQUINOLINE INHIBITORS OF VESICULAR MONOAMINE TRANSPORTER 2

      
Application Number 18666076
Status Pending
Filing Date 2024-05-16
First Publication Date 2024-09-19
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor Stamler, David

Abstract

The present invention relates to new benzoquinoline inhibitors of vesicular monoamine transporter 2 (VMAT2), pharmaceutical compositions thereof, and methods of use thereof. The present invention relates to new benzoquinoline inhibitors of vesicular monoamine transporter 2 (VMAT2), pharmaceutical compositions thereof, and methods of use thereof.

IPC Classes  ?

  • A61K 31/473 - QuinolinesIsoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
  • A61K 31/13 - Amines, e.g. amantadine
  • A61K 31/198 - Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
  • A61K 31/4045 - Indole-alkylaminesAmides thereof, e.g. serotonin, melatonin
  • A61K 31/428 - Thiazoles condensed with carbocyclic 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 31/48 - Ergoline derivatives, e.g. lysergic acid, ergotamine
  • A61K 31/5513 - 1,4-Benzodiazepines, e.g. diazepam
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • C07D 455/06 - Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing quinolizine ring systems directly condensed with at least one six-membered carbocyclic ring, e.g. protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing a quinolizine ring system condensed with only one six-membered carbocyclic ring, e.g. julolidine containing benzo [a] quinolizine ring systems
  • C07D 487/04 - Ortho-condensed systems

6.

METHODS FOR THE TREATMENT OF DYSKINESIA IN CEREBRAL PALSY

      
Application Number 18343197
Status Pending
Filing Date 2023-06-28
First Publication Date 2024-03-14
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Savola, Juha-Matti
  • Gordon, Mark Forrest
  • Schneider, Frank

Abstract

The disclosure is directed to methods of treating dyskinesia in cerebral palsy in human patients using deutetrabenazine and its active metabolites.

IPC Classes  ?

  • A61K 31/4375 - 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 six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
  • A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia

7.

OSMOTIC DOSAGE FORMS COMPRISING DEUTETRABENAZINE AND METHODS OF USE THEREOF

      
Document Number 03257711
Status Pending
Filing Date 2023-06-08
Open to Public Date 2023-12-14
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Shah, Parag
  • Patel, Divyang
  • Pandita, Sandeep
  • Pattanayek, Soumen
  • Joshi, Mayank

IPC Classes  ?

  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 9/28 - DrageesCoated pills or tablets
  • A61K 31/473 - QuinolinesIsoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
  • A61K 47/10 - AlcoholsPhenolsSalts thereof, e.g. glycerolPolyethylene glycols [PEG]PoloxamersPEG/POE alkyl ethers
  • A61K 47/38 - CelluloseDerivatives thereof
  • A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
  • A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia

8.

OSMOTIC DOSAGE FORMS COMPRISING DEUTETRABENAZINE AND METHODS OF USE THEREOF

      
Application Number US2023068129
Publication Number 2023/240186
Status In Force
Filing Date 2023-06-08
Publication Date 2023-12-14
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Shah, Parag
  • Joshi, Mayank
  • Pattanayek, Soumen
  • Patel, Divyang
  • Pandita, Sandeep

Abstract

e.g.,e.g., hyperkinetic movement disorders. When orally administered to a subject on a once-daily basis, the dosage forms provide a favorable pharmacokinetic profile for the active agent indicating treatment efficacy over an extended period of time.

IPC Classes  ?

  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 9/28 - DrageesCoated pills or tablets
  • A61K 31/473 - QuinolinesIsoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
  • A61K 47/10 - AlcoholsPhenolsSalts thereof, e.g. glycerolPolyethylene glycols [PEG]PoloxamersPEG/POE alkyl ethers
  • A61K 47/38 - CelluloseDerivatives thereof
  • A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
  • A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia

9.

GASTRO RETENTIVE DOSAGE FORMS COMPRISING DEUTETRABENAZINE

      
Application Number 18246582
Status Pending
Filing Date 2021-10-12
First Publication Date 2023-12-07
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Joshi, Mayank
  • Shah, Parag
  • Pattanayek, Soumen
  • Patel, Divyang
  • Pandita, Sandeep

Abstract

Provided herein are controlled release gastro retentive dosage forms containing deutetrabenazine for use in the treatment of, e.g., hyperkinetic movement disorders. When orally administered to a subject on a once-daily basis, the dosage forms provide a favorable pharmacokinetic profile.

IPC Classes  ?

  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • 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 9/20 - Pills, lozenges or tablets
  • A61K 47/32 - Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers
  • A61K 47/38 - CelluloseDerivatives thereof

10.

MULTIPARTICULATE DOSAGE FORMS COMPRISING DEUTETRABENAZINE

      
Application Number 18245565
Status Pending
Filing Date 2021-09-17
First Publication Date 2023-11-16
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Joshi, Mayank
  • Shah, Parag
  • Pattanayek, Soumen
  • Patel, Divyang
  • Pandita, Sandeep

Abstract

Provided herein are controlled release multiparticulate dosage forms containing deutetrabenazine for use in the treatment of, e.g., hyperkinetic movement disorders. When orally administered to a subject on a once-daily basis, the dosage forms provide a favorable pharmacokinetic profile.

IPC Classes  ?

  • 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 9/14 - Particulate form, e.g. powders
  • A61K 9/16 - AgglomeratesGranulatesMicrobeadlets
  • A61K 9/50 - Microcapsules

11.

MULTIPARTICULATE DOSAGE FORMS COMPRISING DEUTETRABENAZINE

      
Document Number 03231490
Status Pending
Filing Date 2022-09-16
Open to Public Date 2023-03-23
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Joshi, Mayank
  • Pandita, Sandeep
  • Patel, Divyang
  • Pattanayek, Soumen
  • Shah, Parag

Abstract

Provided herein are modified release multiparticulate dosage forms containing deutetrabenazine for use in the treatment of, e.g., hyperkinetic movement disorders. The dosage forms are easily administered to a subject on a once-daily or twice daily basis, and provide a safe and effective pharmacokinetic profile.

IPC Classes  ?

  • A61K 9/16 - AgglomeratesGranulatesMicrobeadlets
  • A61K 9/50 - Microcapsules
  • 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

12.

MULTIPARTICULATE DOSAGE FORMS COMPRISING DEUTETRABENAZINE

      
Application Number US2022076547
Publication Number 2023/044418
Status In Force
Filing Date 2022-09-16
Publication Date 2023-03-23
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Joshi, Mayank
  • Pandita, Sandeep
  • Patel, Divyang
  • Pattanayek, Soumen
  • Shah, Parag

Abstract

Provided herein are modified release multiparticulate dosage forms containing deutetrabenazine for use in the treatment of, e.g., hyperkinetic movement disorders. The dosage forms are easily administered to a subject on a once-daily or twice daily basis, and provide a safe and effective pharmacokinetic profile.

IPC Classes  ?

  • A61K 9/16 - AgglomeratesGranulatesMicrobeadlets
  • A61K 9/50 - Microcapsules
  • 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

13.

Methods of manufacturing benzoquinoline compounds

      
Application Number 17879600
Grant Number 12077487
Status In Force
Filing Date 2022-08-02
First Publication Date 2023-03-02
Grant Date 2024-09-03
Owner Auspex Pharmaceuticals, Inc. (USA)
Inventor Zhang, Chengzhi

Abstract

The present invention relates to new methods of manufacturing benzoquinoline inhibitors of vesicular monoamine transporter 2 (VMAT2), and intermediates thereof.

IPC Classes  ?

  • C07C 231/12 - Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
  • C07B 59/00 - Introduction of isotopes of elements into organic compounds
  • C07C 221/00 - Preparation of compounds containing amino groups and doubly-bound oxygen atoms bound to the same carbon skeleton
  • C07C 231/02 - Preparation of carboxylic acid amides from carboxylic acids or from esters, anhydrides, or halides thereof by reaction with ammonia or amines
  • C07D 217/04 - Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ringAlkylene-bis-isoquinolines with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
  • C07D 455/06 - Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing quinolizine ring systems directly condensed with at least one six-membered carbocyclic ring, e.g. protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing a quinolizine ring system condensed with only one six-membered carbocyclic ring, e.g. julolidine containing benzo [a] quinolizine ring systems

14.

OSMOTIC DOSAGE FORMS COMPRISING DEUTETRABENAZINE AND METHODS OF USE THEREOF

      
Application Number 17835435
Status Pending
Filing Date 2022-06-08
First Publication Date 2022-09-22
Owner Auspex Pharmaceuticals, Inc. (USA)
Inventor
  • Shah, Parag
  • Joshi, Mayank
  • Pattanayek, Soumen
  • Patel, Divyang
  • Pandita, Sandeep

Abstract

Provided herein are osmotic dosage forms containing deutetrabenazine for use in the treatment of, e.g., hyperkinetic movement disorders. When orally administered to a subject on a once-daily basis, the dosage forms provide a favorable pharmacokinetic profile for the active agent indicating treatment efficacy over an extended period of time.

IPC Classes  ?

  • 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 9/00 - Medicinal preparations characterised by special physical form
  • A61K 9/20 - Pills, lozenges or tablets

15.

Benzoquinoline Inhibitors of Vesicular Monoamine Transporter 2

      
Application Number 17519922
Status Pending
Filing Date 2021-11-05
First Publication Date 2022-08-25
Owner Auspex Pharmaceuticals, Inc. (USA)
Inventor
  • Gant, Thomas G.
  • Shahbaz, Manouchehr

Abstract

The present invention relates to new benzoquinoline inhibitors of vesicular monoamine transporter 2 (VMAT2), pharmaceutical compositions thereof, and methods of use thereof. The present invention relates to new benzoquinoline inhibitors of vesicular monoamine transporter 2 (VMAT2), pharmaceutical compositions thereof, and methods of use thereof.

IPC Classes  ?

  • C07D 455/06 - Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing quinolizine ring systems directly condensed with at least one six-membered carbocyclic ring, e.g. protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing a quinolizine ring system condensed with only one six-membered carbocyclic ring, e.g. julolidine containing benzo [a] quinolizine ring systems
  • 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
  • C07B 59/00 - Introduction of isotopes of elements into organic compounds
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

16.

KINSTEDO

      
Serial Number 97491606
Status Pending
Filing Date 2022-07-06
Owner Auspex Pharmaceuticals, Inc. ()
NICE Classes  ? 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

Pharmaceutical preparations for the prevention and treatment of Alzheimer's disease; Pharmaceutical preparations for the prevention and treatment of depression; Pharmaceutical preparations for the prevention and treatment of psychological disorders; Pharmaceutical preparations for the prevention and treatment of diabetes and diabetic neuropathy; Pharmaceutical preparations for the prevention and treatment of cardiovascular and blood pressure disorders; Pharmaceutical preparations for the prevention and treatment of irritable bowel syndrome; Pharmaceutical preparations for the prevention and treatment of neurodegenerative diseases and disorders; Pharmaceutical preparations for the prevention and treatment of osteoporosis; Pharmaceutical preparations for the prevention and treatment of pain and neuropathic pain; Pharmaceutical preparations for the prevention and treatment of peripheral nervous system diseases and disorders; Pharmaceutical preparations for the prevention and treatment of digestive tract, gastrointestinal and dermatological diseases and disorders; Pharmaceutical preparations for the prevention and treatment of respiratory system diseases and disorders; Pharmaceutical preparations for the prevention and treatment of sexual dysfunction; Pharmaceutical preparations for the prevention and treatment of symptoms associated with uterine fibroids; Pharmaceutical preparations for the prevention and treatment of urinary incontinence and overactive bladder; Pharmaceutical preparations for the prevention and treatment of AIDS-related disorders; Pharmaceutical preparations that support, encourage and promote bone strength; Pharmaceutical preparations that support, encourage and promote bone health; Pharmaceutical preparations used in the treatment of bone disorders and bone diseases; Pharmaceutical preparations, namely, injectable contraceptives; Pharmaceutical preparations, namely, contraceptive preparations; Pharmaceutical preparations, namely, fertility enhancement preparations; Pharmaceutical preparations, namely, hormone replacement therapy preparations; Pharmaceutical preparations for the treatment of cancer; Pharmaceutical agents affecting the central nervous system; Pharmaceutical agents affecting circulatory systems; Pharmaceutical agents affecting sensory organs; Pharmaceutical agents affecting urogenital organs; Pharmaceutical agents affecting peripheral nervous system; Pharmaceutical preparations, namely, oral and injectable contraceptives, women's hormone replacement medications

17.

GASTRO RETENTIVE DOSAGE FORMS COMPRISING DEUTETRABENAZINE

      
Application Number US2021054511
Publication Number 2022/081532
Status In Force
Filing Date 2021-10-12
Publication Date 2022-04-21
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Joshi, Mayank
  • Shah, Parag
  • Pattanayek, Soumen
  • Patel, Divyang
  • Pandita, Sandeep

Abstract

e.g.,e.g., hyperkinetic movement disorders. When orally administered to a subject on a once-daily basis, the dosage forms provide a favorable pharmacokinetic profile.

IPC Classes  ?

  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 9/20 - Pills, lozenges or tablets
  • A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia

18.

MULTIPARTICULATE DOSAGE FORMS COMPRISING DEUTETRABENAZINE

      
Application Number US2021050785
Publication Number 2022/061058
Status In Force
Filing Date 2021-09-17
Publication Date 2022-03-24
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Joshi, Mayank
  • Shah, Parag
  • Pattanayek, Soumen
  • Patel, Divyang
  • Pandita, Sandeep

Abstract

Provided herein are controlled release multiparticulate dosage forms containing deutetrabenazine for use in the treatment of, e.g., hyperkinetic movement disorders. When orally administered to a subject on a once-daily basis, the dosage forms provide a favorable pharmacokinetic profile.

IPC Classes  ?

  • A61K 9/16 - AgglomeratesGranulatesMicrobeadlets
  • A61K 9/50 - Microcapsules
  • 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
  • A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia

19.

ANALOGS OF DEUTETRABENAZINE, THEIR PREPARATION AND USE

      
Application Number 17507037
Status Pending
Filing Date 2021-10-21
First Publication Date 2022-02-10
Owner Auspex Pharmaceuticals, Inc. (USA)
Inventor
  • Zhang, Chengzhi
  • Kerr, James

Abstract

The disclosure is directed to deutetrabenazine analogs, compositions comprising same and methods of detecting same in compositions comprising deutetrabenazine.

IPC Classes  ?

  • 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
  • A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
  • A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
  • C07D 471/04 - Ortho-condensed systems
  • A61K 31/473 - QuinolinesIsoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines

20.

AUSTEDO XR

      
Serial Number 97261591
Status Registered
Filing Date 2022-02-10
Registration Date 2024-06-11
Owner Auspex Pharmaceuticals, Inc. ()
NICE Classes  ? 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

Pharmaceutical preparations for the treatment of central nervous system diseases, namely, neurodegeneration, psychiatric conditions, pain, movement disorders

21.

OSMOTIC DOSAGE FORMS COMPRISING DEUTETRABENAZINE AND METHODS OF USE THEREOF

      
Application Number US2021036778
Publication Number 2021/252741
Status In Force
Filing Date 2021-06-10
Publication Date 2021-12-16
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Shah, Parag
  • Joshi, Mayank
  • Pattanayek, Soumen
  • Patel, Divyang
  • Pandita, Sandeep

Abstract

e.g.e.g., hyperkinetic movement disorders. When orally administered to a subject on a once- daily basis, the dosage forms provide a favorable pharmacokinetic profile for the active agent indicating treatment efficacy over an extended period of time.

IPC Classes  ?

  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 9/28 - DrageesCoated pills or tablets
  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 47/10 - AlcoholsPhenolsSalts thereof, e.g. glycerolPolyethylene glycols [PEG]PoloxamersPEG/POE alkyl ethers
  • A61K 47/38 - CelluloseDerivatives thereof
  • A61K 31/473 - QuinolinesIsoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
  • A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
  • A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia

22.

OSMOTIC DOSAGE FORMS COMPRISING DEUTETRABENAZINE AND METHODS OF USE THEREOF

      
Document Number 03186425
Status Pending
Filing Date 2021-06-10
Open to Public Date 2021-12-16
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Shah, Parag
  • Joshi, Mayank
  • Pattanayek, Soumen
  • Patel, Divyang
  • Pandita, Sandeep

Abstract

Provided herein are osmotic dosage forms containing deutetrabenazine for use in the treatment of, e.g., hyperkinetic movement disorders. When orally administered to a subject on a once- daily basis, the dosage forms provide a favorable pharmacokinetic profile for the active agent indicating treatment efficacy over an extended period of time.

IPC Classes  ?

  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 9/28 - DrageesCoated pills or tablets
  • A61K 31/473 - QuinolinesIsoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
  • A61K 47/10 - AlcoholsPhenolsSalts thereof, e.g. glycerolPolyethylene glycols [PEG]PoloxamersPEG/POE alkyl ethers
  • A61K 47/38 - CelluloseDerivatives thereof
  • A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
  • A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia

23.

Osmotic dosage forms comprising deutetrabenazine and methods of use thereof

      
Application Number 17344271
Grant Number 11311488
Status In Force
Filing Date 2021-06-10
First Publication Date 2021-12-16
Grant Date 2022-04-26
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Shah, Parag
  • Joshi, Mayank
  • Pattanayek, Soumen
  • Patel, Divyang
  • Pandita, Sandeep

Abstract

Provided herein are osmotic dosage forms containing deutetrabenazine for use in the treatment of, e.g., hyperkinetic movement disorders. When orally administered to a subject on a once-daily basis, the dosage forms provide a favorable pharmacokinetic profile for the active agent indicating treatment efficacy over an extended period of time.

IPC Classes  ?

  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 9/24 - Layered or laminated unitary dosage forms
  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • 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

24.

Methods for the treatment of abnormal involuntary movement disorders

      
Application Number 17400194
Grant Number 12016858
Status In Force
Filing Date 2021-08-12
First Publication Date 2021-12-09
Grant Date 2024-06-25
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Stamler, David
  • Huang, Michael

Abstract

Disclosed herein are new dosage regimens for deuterium-substituted benzoquinoline compounds, and methods for the treatment of abnormal muscular activity, movement disorders, and related conditions.

IPC Classes  ?

  • A61K 31/473 - QuinolinesIsoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 31/4375 - 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 six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
  • 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 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia

25.

Methods for the treatment of abnormal involuntary movement disorders

      
Application Number 17212205
Grant Number 11446291
Status In Force
Filing Date 2021-03-25
First Publication Date 2021-09-09
Grant Date 2022-09-20
Owner Auspex Pharmaceuticals, Inc. (USA)
Inventor
  • Stamler, David
  • Huang, Michael Fangching

Abstract

Disclosed herein are new dosage regimens for deuterium-substituted benzoquinoline compounds, and methods for the treatment of abnormal muscular activity, movement disorders, and related conditions.

IPC Classes  ?

  • A61K 31/473 - QuinolinesIsoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
  • A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
  • A61K 31/4375 - 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 six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
  • 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 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61K 9/20 - Pills, lozenges or tablets

26.

Methods for the treatment of abnormal involuntary movement disorders

      
Application Number 17154312
Grant Number 11357772
Status In Force
Filing Date 2021-01-21
First Publication Date 2021-05-20
Grant Date 2022-06-14
Owner
  • AUXPEX PHARMACEUTICALS, INC. (USA)
  • AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Stamler, David
  • Huang, Michael

Abstract

Disclosed herein are new dosage regimens for deuterium-substituted benzoquinoline compounds, and methods for the treatment of abnormal muscular activity, movement disorders, and related conditions.

IPC Classes  ?

  • A61K 31/473 - QuinolinesIsoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • 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 31/4375 - 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 six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
  • A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia

27.

Formulations and pharmacokinetics of deuterated benzoquinoline inhibitors of vesicular monoamine transporter 2

      
Application Number 16682041
Grant Number 11033540
Status In Force
Filing Date 2019-11-13
First Publication Date 2020-09-17
Grant Date 2021-06-15
Owner Auspex Pharmaceuticals, Inc. (USA)
Inventor
  • Sommer, Andreas
  • Zhang, Chengzhi
  • Carter, John
  • Arthur, John Charles
  • Bradbury, Margaret
  • Gant, Thomas George
  • Shahbaz, Manouchehr

Abstract

The present invention relates to new pharmaceutical compositions comprising benzoquinoline compounds, and methods to inhibit vesicular monoamine transporter 2 (VMAT2) activity in a subject for the treatment of chronic hyperkinetic movement disorders.

IPC Classes  ?

  • 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 31/473 - QuinolinesIsoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
  • A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
  • A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia
  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 9/16 - AgglomeratesGranulatesMicrobeadlets
  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 9/28 - DrageesCoated pills or tablets
  • A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
  • A61K 9/50 - Microcapsules
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • C07D 455/06 - Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing quinolizine ring systems directly condensed with at least one six-membered carbocyclic ring, e.g. protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing a quinolizine ring system condensed with only one six-membered carbocyclic ring, e.g. julolidine containing benzo [a] quinolizine ring systems

28.

Formulations and pharmacokinetics of deuterated benzoquinoline inhibitors of vesicular monoamine transporter 2

      
Application Number 16859514
Grant Number 11666566
Status In Force
Filing Date 2020-04-27
First Publication Date 2020-08-13
Grant Date 2023-06-06
Owner Auspex Pharmaceuticals, Inc. (USA)
Inventor
  • Sommer, Andreas
  • Zhang, Chengzhi
  • Carter, John
  • Arthur, John Charles
  • Bradbury, Margaret
  • Gant, Thomas George
  • Shahbaz, Manouchehr

Abstract

The present invention relates to new pharmaceutical compositions comprising benzoquinoline compounds, and methods to inhibit vesicular monoamine transporter 2 (VMAT2) activity in a subject for the treatment of chronic hyperkinetic movement disorders.

IPC Classes  ?

  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 9/28 - DrageesCoated pills or tablets
  • A61K 47/38 - CelluloseDerivatives thereof
  • A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
  • A61K 31/473 - QuinolinesIsoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 9/16 - AgglomeratesGranulatesMicrobeadlets
  • A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
  • A61K 9/50 - Microcapsules
  • 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 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • C07D 455/06 - Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing quinolizine ring systems directly condensed with at least one six-membered carbocyclic ring, e.g. protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing a quinolizine ring system condensed with only one six-membered carbocyclic ring, e.g. julolidine containing benzo [a] quinolizine ring systems

29.

DEUTETRABENAZINE FOR THE TREATMENT OF DYSKINESIA IN CEREBRAL PALSY

      
Document Number 03123393
Status Pending
Filing Date 2019-12-13
Open to Public Date 2020-06-18
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Savola, Juha-Matti
  • Gordon, Mark Forrest
  • Schneider, Frank

Abstract

The disclosure is directed to methods of treating dyskinesia in cerebral palsy in human patients using deutetrabenazine and its active metabolites.

IPC Classes  ?

  • 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
  • A61P 25/02 - Drugs for disorders of the nervous system for peripheral neuropathies

30.

Methods for the treatment of dyskinesia in cerebral palsy

      
Application Number 16713917
Grant Number 11324732
Status In Force
Filing Date 2019-12-13
First Publication Date 2020-06-18
Grant Date 2022-05-10
Owner Auspex Pharmaceuticals, Inc. (USA)
Inventor
  • Savola, Juha-Matti
  • Gordon, Mark Forrest
  • Schneider, Frank

Abstract

The disclosure is directed to methods of treating dyskinesia in cerebral palsy in human patients using deutetrabenazine and its active metabolites.

IPC Classes  ?

  • A61K 31/4375 - 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 six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
  • A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia

31.

DEUTETRABENAZINE FOR THE TREATMENT OF DYSKINESIA IN CEREBRAL PALSY

      
Application Number US2019066150
Publication Number 2020/123900
Status In Force
Filing Date 2019-12-13
Publication Date 2020-06-18
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Savola, Juha-Matti
  • Gordon, Mark Forrest
  • Schneider, Frank

Abstract

The disclosure is directed to methods of treating dyskinesia in cerebral palsy in human patients using deutetrabenazine and its active metabolites.

IPC Classes  ?

  • 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
  • A61P 25/02 - Drugs for disorders of the nervous system for peripheral neuropathies

32.

Analogs of deutetrabenazine, their preparation and use

      
Application Number 16582362
Grant Number 11179386
Status In Force
Filing Date 2019-09-25
First Publication Date 2020-01-16
Grant Date 2021-11-23
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Zhang, Chengzhi
  • Kerr, James

Abstract

The disclosure is directed to deutetrabenazine analogs, compositions comprising same and methods of detecting same in compositions comprising deutetrabenazine.

IPC Classes  ?

  • 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
  • A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
  • A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
  • C07D 471/04 - Ortho-condensed systems
  • A61K 31/473 - QuinolinesIsoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines

33.

Cyclopropane carboxamide modulators of cystic fibrosis transmembrane conductance regulator

      
Application Number 16225098
Grant Number 10689370
Status In Force
Filing Date 2018-12-19
First Publication Date 2019-12-05
Grant Date 2020-06-23
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Zhang, Chengzhi
  • Chakma, Justin

Abstract

The present invention relates to new cyclopropanecarboxamide modulators of cystic fibrosis transmembrane conductance regulator proteins, pharmaceutical compositions thereof, and methods of use thereof.

IPC Classes  ?

  • 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
  • A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
  • A61P 11/00 - Drugs for disorders of the respiratory system

34.

Pharmaceutical formulations

      
Application Number 16510246
Grant Number 10966922
Status In Force
Filing Date 2019-07-12
First Publication Date 2019-10-31
Grant Date 2021-04-06
Owner Auspex Pharmaceuticals, Inc. (USA)
Inventor
  • Sommer, Andreas
  • Zhang, Chengzhi
  • Carter, John
  • Arthur, John
  • Bradbury, Margaret

Abstract

The present invention relates to new extended release pharmaceutical compositions and methods of use thereof for the treatment of disorders.

IPC Classes  ?

  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 31/133 - Amines, e.g. amantadine having hydroxy groups, e.g. sphingosine
  • A61K 31/135 - Amines, e.g. amantadine having aromatic rings, e.g. methadone
  • A61K 31/137 - Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine
  • 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 31/19 - Carboxylic acids, e.g. valproic acid
  • 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 31/4745 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
  • A61K 31/522 - Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
  • A61K 9/28 - DrageesCoated pills or tablets
  • A61K 31/00 - Medicinal preparations containing organic active ingredients

35.

NOW IT'S YOUR MOVE

      
Serial Number 88663758
Status Registered
Filing Date 2019-10-22
Registration Date 2020-05-19
Owner Auspex Pharmaceuticals, Inc. ()
NICE Classes  ? 44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services

Goods & Services

Providing medical information relating to neurological diseases

36.

Methods for the treatment of abnormal involuntary movement disorders

      
Application Number 16040012
Grant Number 10959996
Status In Force
Filing Date 2018-07-19
First Publication Date 2018-11-08
Grant Date 2021-03-30
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Stamler, David
  • Huang, Michael Fangching

Abstract

Disclosed herein are new dosage regimens for deuterium-substituted benzoquinoline compounds, and methods for the treatment of abnormal muscular activity, movement disorders, and related conditions.

IPC Classes  ?

  • A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 31/4375 - 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 six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
  • 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 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61K 31/473 - QuinolinesIsoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines

37.

Cyclopropanecarboxamide modulators of cystic fibrosis transmembrane conductance regulator

      
Application Number 15539169
Grant Number 10167278
Status In Force
Filing Date 2015-12-27
First Publication Date 2018-09-20
Grant Date 2019-01-01
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Zhang, Chengzhi
  • Chakma, Justin

Abstract

The present invention relates to new cyclopropanecarboxamide modulators of cystic fibrosis transmembrane conductance regulator proteins, pharmaceutical compositions thereof, and methods of use thereof.

IPC Classes  ?

  • 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
  • A61P 11/00 - Drugs for disorders of the respiratory system

38.

ANALOGS OF DEUTETRABENAZINE, THEIR PREPARATION AND USE

      
Document Number 03056612
Status Pending
Filing Date 2018-03-15
Open to Public Date 2018-09-20
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Zhang, Chengzi
  • Kerr, Jim

Abstract

The disclosure is directed to deutetrabenazine analogs, compositions comprising same and methods of detecting same in compositions comprising deutetrabenazine.

IPC Classes  ?

  • A61K 31/4375 - 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 six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
  • A61P 25/00 - Drugs for disorders of the nervous system
  • C07D 471/04 - Ortho-condensed systems

39.

Analogs of deutetrabenazine, their preparation and use

      
Application Number 15922329
Grant Number 11813232
Status In Force
Filing Date 2018-03-15
First Publication Date 2018-09-20
Grant Date 2023-11-14
Owner Auspex Pharmaceuticals, Inc. (USA)
Inventor
  • Zhang, Chengzhi
  • Kerr, James

Abstract

The disclosure is directed to deutetrabenazine analogs, compositions comprising same and methods of detecting same in compositions comprising deutetrabenazine.

IPC Classes  ?

  • 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
  • A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
  • A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
  • C07D 471/04 - Ortho-condensed systems
  • A61K 31/473 - QuinolinesIsoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines

40.

DEUTERATED AMINOPYRIDINE COMPOUNDS

      
Application Number US2017064992
Publication Number 2018/106850
Status In Force
Filing Date 2017-12-07
Publication Date 2018-06-14
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Zhang, Chengzhi
  • Laufer, Ralph

Abstract

The present disclosure is directed to Compound I and Compound II as well as pharmaceutical compositions including Compound I or Compound II, or mixtures thereof. The disclosure is additionally directed to methods of making the aforementioned compounds and pharmaceutical compositions as well as their methods of use.

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
  • A61P 35/02 - Antineoplastic agents specific for leukemia
  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings

41.

DEUTERIUM-SUBSTITUTED PYRIDIN- AND PYRIMIDIN-2-YL-METHYLAMINE COMPOUNDS

      
Application Number US2017052426
Publication Number 2018/057576
Status In Force
Filing Date 2017-09-20
Publication Date 2018-03-29
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor Zhang, Chengzhi

Abstract

Described are deuterium-substituted pyridin- and pyrimidin-2-yl-methylamine compounds of structural Formula I, which are agonists of 5-hydroxytryptamine receptors. Also described are pharmaceutical compositions comprising the deuterium-substituted pyridin- and pyrimidin-2-yl-methyiamine compounds, and methods of use thereof. Formula (I) In formula (I) X is N or C-R21; R1-R21 a re- independently, hydrogen or deuterium; at least one of R1-R21is deuterium; and at least one of R1-R21 has deuterium enrichment of at least about 1%.

IPC Classes  ?

  • 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 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
  • A61P 43/00 - Drugs for specific purposes, not provided for in groups
  • A61P 25/00 - Drugs for disorders of the nervous system

42.

Deuterium-substituted pyridin- and pyrimidin-2-yl-methylamine compounds

      
Application Number 15709828
Grant Number 10626105
Status In Force
Filing Date 2017-09-20
First Publication Date 2018-03-22
Grant Date 2020-04-21
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor Zhang, Chengzhi

Abstract

Described are deuterium-substituted pyridin- and pyrimidin-2-yl-methylamine compounds of structural Formula (I), which are agonists of 5-hydroxytryptamine receptors. Also described are pharmaceutical compositions comprising the deuterium-substituted pyridin- and pyrimidin-2-yl-methylamine compounds, and methods of use thereof.

IPC Classes  ?

  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic 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

43.

DEUTERIUM-SUBSTITUTED OXAZEPIN COMPOUNDS

      
Application Number US2017050395
Publication Number 2018/048977
Status In Force
Filing Date 2017-09-07
Publication Date 2018-03-15
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Fisher, Richard
  • Zhang, Chengzhi

Abstract

Described are deuterium-substituted oxazepin compounds of structural Formula I, which are inhibitors/blockers of the late sodium current. Also described are pharmaceutical compositions comprising the deuterium-substituted oxazepin compounds, and methods of use thereof. (I)

IPC Classes  ?

  • 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
  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61P 9/00 - Drugs for disorders of the cardiovascular system

44.

Methods for the treatment of abnormal involuntary movement disorders

      
Application Number 15722208
Grant Number 11564917
Status In Force
Filing Date 2017-10-02
First Publication Date 2018-03-08
Grant Date 2023-01-31
Owner Auspex Pharmaceuticals, Inc. (USA)
Inventor
  • Stamler, David
  • Huang, Michael Fangching

Abstract

Disclosed herein are new dosage regimens for deuterium-substituted benzoquinoline compounds, and methods for the treatment of abnormal muscular activity, movement disorders, and related conditions.

IPC Classes  ?

  • A61K 31/473 - QuinolinesIsoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
  • A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61K 31/4375 - 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 six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
  • 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

45.

Dimethoxyphenyl inhibitors of vesicular monoamine transporter 2

      
Application Number 15550152
Grant Number 10722479
Status In Force
Filing Date 2016-02-17
First Publication Date 2018-02-08
Grant Date 2020-07-28
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor Zhang, Chengzhi

Abstract

Described are dimethoxyphenyl inhibitors of VMAT2, pharmaceutical compositions thereof, and methods of use thereof.

IPC Classes  ?

  • A61K 31/137 - Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine
  • A61K 31/138 - Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
  • A61K 31/4375 - 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 six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
  • C07C 217/60 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains not further substituted by singly-bound oxygen atoms linked by carbon chains having two carbon atoms between the amino groups and the six-membered aromatic ring or the condensed ring system containing that ring
  • C07B 59/00 - Introduction of isotopes of elements into organic compounds

46.

Methods for the treatment of abnormal involuntary movement disorders

      
Application Number 15667483
Grant Number 11648244
Status In Force
Filing Date 2017-08-02
First Publication Date 2017-11-16
Grant Date 2023-05-16
Owner Auspex Pharmaceuticals, Inc. (USA)
Inventor
  • Stamler, David
  • Huang, Michael Fangching

Abstract

Disclosed herein are new dosage regimens for deuterium-substituted benzoquinoline compounds, and methods for the treatment of abnormal muscular activity, movement disorders, and related conditions.

IPC Classes  ?

  • A61K 31/473 - QuinolinesIsoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61K 31/4375 - 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 six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
  • A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
  • 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

47.

Methods of manufacturing benzoquinoline compounds

      
Application Number 15472779
Grant Number 10513488
Status In Force
Filing Date 2017-03-29
First Publication Date 2017-07-13
Grant Date 2019-12-24
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor Zhang, Chengzhi

Abstract

The present invention relates to new methods of manufacturing benzoquinoline inhibitors of vesicular monoamine transporter 2 (VMAT2), and intermediates thereof.

IPC Classes  ?

  • C07D 217/04 - Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ringAlkylene-bis-isoquinolines with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
  • C07D 455/06 - Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing quinolizine ring systems directly condensed with at least one six-membered carbocyclic ring, e.g. protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing a quinolizine ring system condensed with only one six-membered carbocyclic ring, e.g. julolidine containing benzo [a] quinolizine ring systems
  • C07C 231/12 - Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
  • C07C 231/02 - Preparation of carboxylic acid amides from carboxylic acids or from esters, anhydrides, or halides thereof by reaction with ammonia or amines
  • C07C 221/00 - Preparation of compounds containing amino groups and doubly-bound oxygen atoms bound to the same carbon skeleton
  • C07B 59/00 - Introduction of isotopes of elements into organic compounds

48.

AZETIDINE MODULATORS OF THE SPHINGOSINE 1-PHOSPHATE RECEPTOR

      
Application Number US2017012009
Publication Number 2017/120124
Status In Force
Filing Date 2017-01-03
Publication Date 2017-07-13
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Zhang, Chengzhi
  • Chakma, Justin

Abstract

Described are deuterium-substituted azetidine compounds of Formula (I), which are modulators of sphingosine 1 -phosphate receptor. Also described are pharmaceutical compositions comprising the deuterium-substituted azetidine compounds, and methods of use thereof.

IPC Classes  ?

  • C07D 205/04 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members

49.

TETRAHYDROCARBAZOLE INHIBITORS OF SIRT1 RECEPTORS

      
Application Number US2017012442
Publication Number 2017/120409
Status In Force
Filing Date 2017-01-06
Publication Date 2017-07-13
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Zhang, Chengzhi
  • Laufer, Ralph

Abstract

Described are deuterium-substituted tetrahydrocarbazole compounds of Formulae (I), (II), or (III), which are inhibitors of sirtuin 1 (SIRT1). Also described are pharmaceutical compositions comprising the deuterium-substituted tetrahydrocarbazole compounds, and methods of use thereof.

IPC Classes  ?

  • C07D 209/56 - Ring systems containing three or more rings
  • A61K 31/403 - 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 carbocyclic rings, e.g. carbazole
  • A61P 25/00 - Drugs for disorders of the nervous system

50.

Tetrahydrocarbazole inhibitors of SIRT1 receptors

      
Application Number 15400144
Grant Number 09884819
Status In Force
Filing Date 2017-01-06
First Publication Date 2017-07-06
Grant Date 2018-02-06
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Zhang, Chengzhi
  • Laufer, Ralph

Abstract

Described are deuterium-substituted tetrahydrocarbazole compounds of Formulae I, II, or III which are inhibitors of sirtuin 1 (SIRT1). Also described are pharmaceutical compositions comprising the deuterium-substituted tetrahydrocarbazole compounds, and methods of use thereof.

IPC Classes  ?

  • C07D 209/86 - CarbazolesHydrogenated carbazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the ring system
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61K 31/403 - 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 carbocyclic rings, e.g. carbazole
  • A61K 31/4704 - 2-Quinolinones, e.g. carbostyril

51.

DEUTERATED CHLOROKYNURENINES FOR THE TREATMENT OF NEUROPSYCHIATRIC DISORDERS

      
Application Number US2016050667
Publication Number 2017/065899
Status In Force
Filing Date 2016-09-08
Publication Date 2017-04-20
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Ott, Gregory, R.
  • Zhang, Chengzhi
  • Laufer, Ralph

Abstract

Described are deuterated chlorokynurenines and compositions, and their application as pharmaceuticals for the treatment of disease. Methods of modulating N-methyl-D-aspartate (NMDA) receptor activity, methods of treating disorders, including neuropsychiatric disorders such as depression, epilepsy, schizophrenia, and Huntington's Disease, and use of said deuterated chlorokynurenines are also described.

IPC Classes  ?

  • C07B 59/00 - Introduction of isotopes of elements into organic compounds
  • C07C 229/36 - 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 containing six-membered aromatic rings with at least one amino group and one carboxyl group bound to the same carbon atom of the carbon skeleton

52.

Pharmaceutical formulations

      
Application Number 15116970
Grant Number 10166183
Status In Force
Filing Date 2015-02-05
First Publication Date 2016-12-01
Grant Date 2019-01-01
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Sommer, Andreas
  • Zhang, Chengzhi
  • Carter, John
  • Arthur, John
  • Bradbury, Margaret

Abstract

The present invention relates to new extended release pharmaceutical compositions and methods of use thereof for the treatment of disorders. In certain embodiments, disclosed herein is an extended-release pharmaceutical formulation comprising, in a solid dosage form for oral delivery of between about 100 mg and about 1 g total weight: between about 2 and about 18% of an active ingredient; between about 70% and about 96% of one or more diluents; between about 1% and about 10% of a water-soluble binder and between about 0.5 and about 2% of a surfactant.

IPC Classes  ?

  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 31/522 - Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
  • A61K 31/19 - Carboxylic acids, e.g. valproic acid
  • 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 31/437 - 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 9/20 - Pills, lozenges or tablets
  • A61K 31/00 - Medicinal preparations containing organic active ingredients
  • A61K 9/28 - DrageesCoated pills or tablets

53.

Piperidine inhibitors of Janus kinase 3

      
Application Number 15229267
Grant Number 09856261
Status In Force
Filing Date 2016-08-05
First Publication Date 2016-11-24
Grant Date 2018-01-02
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Rao, Tadimeti
  • Zhang, Chengzhi

Abstract

The present invention relates to new piperidine inhibitors of Janus kinase 3 activity, pharmaceutical compositions thereof, and methods of use thereof.

IPC Classes  ?

  • A01N 43/90 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having two or more relevant hetero rings, condensed among themselves or with a common carbocyclic ring system
  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • C07D 487/00 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups
  • C07D 487/04 - Ortho-condensed systems

54.

DEUTERIUM-SUBSTITUTED OXADIAZOLES

      
Application Number US2016024143
Publication Number 2016/164180
Status In Force
Filing Date 2016-03-25
Publication Date 2016-10-13
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Zhang, Chengzhi
  • Chakma, Justin

Abstract

Described are deuterated modulators of S1P1 receptors, pharmaceutical compositions thereof, and methods of use thereof.

IPC Classes  ?

55.

METHODS FOR THE TREATMENT OF ABNORMAL INVOLUNTARY MOVEMENT DISORDERS

      
Document Number 02978006
Status In Force
Filing Date 2016-03-07
Open to Public Date 2016-09-15
Grant Date 2024-06-25
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Stamler, David
  • Huang, Michael Fangching

Abstract

Disclosed herein are new dosage regimens for deuterium-substituted benzoquinoline compounds, and methods for the treatment of abnormal muscular activity, movement disorders, and related conditions.

IPC Classes  ?

  • A61K 31/4375 - 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 six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
  • A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia

56.

METHODS FOR THE TREATMENT OF ABNORMAL INVOLUNTARY MOVEMENT DISORDERS

      
Document Number 03236214
Status Pending
Filing Date 2016-03-07
Open to Public Date 2016-09-15
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Stamler, David
  • Huang, Michael Fangching

Abstract

Disclosed herein are new dosage regimens for deuterium-substituted benzoquinoline compounds, and methods for the treatment of abnormal muscular activity, movement disorders, and related conditions.

IPC Classes  ?

  • 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
  • A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia

57.

METHODS FOR THE TREATMENT OF ABNORMAL INVOLUNTARY MOVEMENT DISORDERS

      
Application Number US2016021238
Publication Number 2016/144901
Status In Force
Filing Date 2016-03-07
Publication Date 2016-09-15
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Stamler, David
  • Huang, Michael, Fangching

Abstract

Disclosed herein are new dosage regimens for deuterium-substituted benzoquinoline compounds, and methods for the treatment of abnormal muscular activity, movement disorders, and related conditions.

IPC Classes  ?

  • A61K 31/4375 - 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 six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
  • A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia

58.

DIMETHOXYPHENYL INHIBITORS OF VESICULAR MONOAMINE TRANSPORTER 2

      
Application Number US2016018222
Publication Number 2016/133989
Status In Force
Filing Date 2016-02-17
Publication Date 2016-08-25
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor Zhang, Chengzhi

Abstract

Described are dimethoxyphenyl inhibitors of VMAT2, pharmaceutical compositions thereof, and methods of use thereof.

IPC Classes  ?

  • A61K 31/137 - Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine
  • A61K 31/138 - Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
  • C07C 215/20 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated the carbon skeleton being saturated and containing rings

59.

Formulations and pharmacokinetics of deuterated benzoquinoline inhibitors of vesicular monoamine transporter 2

      
Application Number 15044655
Grant Number 09814708
Status In Force
Filing Date 2016-02-16
First Publication Date 2016-08-18
Grant Date 2017-11-14
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Sommer, Andreas
  • Zhang, Chengzhi
  • Carter, John
  • Arthur, John
  • Bradbury, Margaret
  • Gant, Thomas
  • Shahbaz, Manouchehr

Abstract

The present invention relates to new pharmaceutical compositions comprising benzoquinoline compounds, and methods to inhibit vesicular monoamine transporter 2 (VMAT2) activity in a subject for the treatment of chronic hyperkinetic movement disorders.

IPC Classes  ?

  • C07D 455/06 - Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing quinolizine ring systems directly condensed with at least one six-membered carbocyclic ring, e.g. protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing a quinolizine ring system condensed with only one six-membered carbocyclic ring, e.g. julolidine containing benzo [a] quinolizine ring systems
  • C07D 471/04 - Ortho-condensed systems
  • 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 31/473 - QuinolinesIsoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 9/16 - AgglomeratesGranulatesMicrobeadlets
  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 9/28 - DrageesCoated pills or tablets
  • A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
  • A61K 9/50 - Microcapsules
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

60.

Formulations pharmacokinetics of deuterated benzoquinoline inhibitors of vesicular monoamine transporter 2

      
Application Number 15071797
Grant Number 09550780
Status In Force
Filing Date 2016-03-16
First Publication Date 2016-08-04
Grant Date 2017-01-24
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Sommer, Andreas
  • Zhang, Chengzhi
  • Carter, John
  • Arthur, John
  • Bradbury, Margaret
  • Gant, Thomas
  • Shahbaz, Manouchehr

Abstract

The present invention relates to new pharmaceutical compositions comprising benzoquinoline compounds, and methods to inhibit vesicular monoamine transporter 2 (VMAT2) activity in a subject for the treatment of chronic hyperkinetic movement disorders.

IPC Classes  ?

  • A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
  • A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia
  • A61P 25/24 - Antidepressants
  • A61P 25/00 - Drugs for disorders of the nervous system
  • A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
  • A61K 31/5415 - 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 ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
  • C07D 455/06 - Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing quinolizine ring systems directly condensed with at least one six-membered carbocyclic ring, e.g. protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing a quinolizine ring system condensed with only one six-membered carbocyclic ring, e.g. julolidine containing benzo [a] quinolizine ring systems
  • C07D 471/04 - Ortho-condensed systems
  • C07B 59/00 - Introduction of isotopes of elements into organic compounds

61.

3-FLUORO-BENZONITRILE INHIBITORS OF 11-BETA-HYDROXYLASE

      
Application Number US2015067543
Publication Number 2016/109361
Status In Force
Filing Date 2015-12-27
Publication Date 2016-07-07
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Zhang, Chengzhi
  • Chakma, Justin

Abstract

The present invention relates to new 3-fluoro-benzonitrile modulators of 11-β- hydroxylase, pharmaceutical compositions thereof, and methods of use thereof.

IPC Classes  ?

  • A61K 31/4188 - 1,3-Diazoles condensed with heterocyclic ring systems, e.g. biotin, sorbinil
  • C07D 487/04 - Ortho-condensed systems

62.

CYCLOPROPANECARBOXAMIDE MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR

      
Application Number US2015067544
Publication Number 2016/109362
Status In Force
Filing Date 2015-12-27
Publication Date 2016-07-07
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Zhang, Chengzhi
  • Chakma, Justin

Abstract

The present invention relates to new cyclopropanecarboxamide modulators of cystic fibrosis transmembrane conductance regulator proteins, pharmaceutical compositions thereof, and methods of use thereof.

IPC Classes  ?

  • A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings

63.

CYCLOPROPYL DIHYDROBENZOFURAN MODULATORS OF MELATONIN RECEPTORS

      
Application Number US2015067541
Publication Number 2016/109359
Status In Force
Filing Date 2015-12-27
Publication Date 2016-07-07
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Zhang, Chengzhi
  • Chakma, Justin
  • Laufer, Ralph

Abstract

The present invention relates to new cyclopropyl dihydrobenzofuran modulators of melatonin receptors, pharmaceutical compositions thereof, and methods of use thereof.

IPC Classes  ?

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

64.

DIHYDROQUINAZOLINE INHIBITORS OF VIRAL TERMINASE

      
Application Number US2015067542
Publication Number 2016/109360
Status In Force
Filing Date 2015-12-27
Publication Date 2016-07-07
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Zhang, Chengzhi
  • Chakma, Justin

Abstract

The present invention relates to new dihydroquinazoline modulators of viral infection, pharmaceutical compositions thereof, and methods of use thereof.

IPC Classes  ?

  • A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
  • C07D 239/84 - Nitrogen atoms

65.

N-ARYL PYRIDINONES MODULATORS OF FIBROSIS AND/OR COLLAGEN INFILTRATION

      
Application Number US2015027765
Publication Number 2015/171345
Status In Force
Filing Date 2015-04-27
Publication Date 2015-11-12
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor Zhang, Chengzhi

Abstract

The present invention relates to new N-Aryi pyridinones modulators of fibrosis and/or collagen infiltration, pharmaceutical compositions thereof, and methods of use thereof. Disclosed herein are new N-aryl pyridinones compounds and compositions and their application as pharmaceuticals for the treatment of disorders. Methods of modulation of fibrosis and/or collagen infiltration in a subject are also provided for the treatment of disorders.

IPC Classes  ?

  • A61K 31/4412 - Non-condensed pyridinesHydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring

66.

Piperidine inhibitors of Janus kinase 3

      
Application Number 14596784
Grant Number 09493469
Status In Force
Filing Date 2015-01-14
First Publication Date 2015-11-12
Grant Date 2016-11-15
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Rao, Tadimeti
  • Zhang, Chengzhi

Abstract

The present invention relates to new piperidine inhibitors of Janus kinase 3 activity, pharmaceutical compositions thereof, and methods of use thereof.

IPC Classes  ?

  • C07D 487/00 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups
  • C07D 487/04 - Ortho-condensed systems

67.

OXINDOLE INHIBITORS OF TYROSINE KINASE

      
Application Number US2015024074
Publication Number 2015/153877
Status In Force
Filing Date 2015-04-02
Publication Date 2015-10-08
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Rao, Tadimeti
  • Zhang, Chengzhi

Abstract

The present invention relates to new oxindole inhibitors of tyrosine kinase, pharmaceutical compositions thereof, and methods of use thereof. Formula (I).

IPC Classes  ?

  • C07D 209/34 - Oxygen atoms in position 2
  • 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 209/30 - 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

68.

AUSTEDO

      
Serial Number 86752573
Status Registered
Filing Date 2015-09-10
Registration Date 2018-02-06
Owner Auspex Pharmaceuticals, Inc. ()
NICE Classes  ? 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

Pharmaceutical preparations for the treatment of central nervous system diseases, namely, neurodegeneration, psychiatric conditions, pain, movement disorders

69.

NOVEL PHARMACEUTICAL FORMULATIONS

      
Application Number US2015014545
Publication Number 2015/120110
Status In Force
Filing Date 2015-02-05
Publication Date 2015-08-13
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Sommer, Andreas
  • Zhang, Chengzhi
  • Carter, John
  • Arthur, John
  • Bradbury, Margaret

Abstract

The present invention relates to new extended release pharmaceutical compositions and methods of use thereof for the treatment of disorders. In certain embodiments, disclosed herein is an extended-release pharmaceutical formulation comprising, in a solid dosage form for oral delivery of between about 100 mg and about 1 g total weight: between about 2 and about 18% of an active ingredient; between about 70% and about 96% of one or more diluents; between about 1% and about 10% of a water-soluble binder and between about 0.5 and about 2% of a surfactant.

IPC Classes  ?

  • C07D 455/06 - Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing quinolizine ring systems directly condensed with at least one six-membered carbocyclic ring, e.g. protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing a quinolizine ring system condensed with only one six-membered carbocyclic ring, e.g. julolidine containing benzo [a] quinolizine ring systems

70.

SUBSTITUTED N-ARYL PYRIDINONES

      
Application Number US2015012438
Publication Number 2015/112701
Status In Force
Filing Date 2015-01-22
Publication Date 2015-07-30
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Shah, Pratik
  • Saks, Samuel

Abstract

Disclosed herein are substituted N-Aryl pyridinone fibrotic inhibitors and/or collagen infiltration modulators of Formula (I), process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.

IPC Classes  ?

  • A61K 31/44 - Non-condensed pyridinesHydrogenated derivatives thereof
  • A61K 38/39 - Connective tissue peptides, e.g. collagen, elastin, laminin, fibronectin, vitronectin, cold insoluble globulin [CIG]
  • C07K 14/75 - Fibrinogen

71.

BENZOQUINOLINE INHIBITORS OF VESICULAR MONOAMINE TRANSPORTER 2

      
Application Number US2015012445
Publication Number 2015/112707
Status In Force
Filing Date 2015-01-22
Publication Date 2015-07-30
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor Stamler, David

Abstract

The present invention relates to new benzoquinoline inhibitors of vesicular monoamine transporter 2 (VMAT2), pharmaceutical compositions thereof, and methods of use thereof. (Formula (I))

IPC Classes  ?

  • A61K 31/4353 - 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
  • C07D 221/06 - Ring systems of three rings

72.

METHODS OF MANUFACTURING BENZOQUINOLINE COMPOUNDS

      
Application Number US2014067117
Publication Number 2015/084622
Status In Force
Filing Date 2014-11-24
Publication Date 2015-06-11
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor Zhang, Chengzhi

Abstract

The present invention relates to new methods of manufacturing benzoquinoline inhibitors of vesicular monoamine transporter 2 (VMAT2), and intermediates thereof. Novel methods of manufacturing benzoquinoline compounds of formula (I), including tetrabenazine and deuterated tetrabenazine analogs such as d6-tetrabenazine are disclosed herein. Tetrabenazine is a vesicular monoamine transporter 2 (VMAT2) inhibitor and is commonly prescribed for the treatment of Huntington's disease. d6-Tetrabenazine is a deuterated analog of tetrabenazine which has improved pharmacokinetic properties when compared to the non-deuterated drug and is currently under clinical development.

IPC Classes  ?

  • A61K 31/473 - QuinolinesIsoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines

73.

METHODS OF TREATING ABNORMAL MUSCULAR ACTIVITY

      
Application Number US2014066740
Publication Number 2015/077520
Status In Force
Filing Date 2014-11-21
Publication Date 2015-05-28
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor Shah, Pratik

Abstract

Methods for treating abnormal muscular activity are disclosed. The methods may be performed remotely and permit monitoring of a subject outside a healthcare provider's office.

IPC Classes  ?

  • C07D 455/06 - Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing quinolizine ring systems directly condensed with at least one six-membered carbocyclic ring, e.g. protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing a quinolizine ring system condensed with only one six-membered carbocyclic ring, e.g. julolidine containing benzo [a] quinolizine ring systems
  • C07C 69/96 - Esters of carbonic or haloformic acids

74.

BENZOQUINOLINE INHIBITORS OF VESICULAR MONOAMINE TRANSPORTER 2

      
Application Number US2014066741
Publication Number 2015/077521
Status In Force
Filing Date 2014-11-21
Publication Date 2015-05-28
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Shah, Pratik
  • Saks, Samuel

Abstract

The present invention relates to new benzoquinoline inhibitors of vesicular monoamine transporter 2 (VMAT2), pharmaceutical compositions thereof, and methods of use thereof. (I)

IPC Classes  ?

  • C07D 455/06 - Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing quinolizine ring systems directly condensed with at least one six-membered carbocyclic ring, e.g. protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing a quinolizine ring system condensed with only one six-membered carbocyclic ring, e.g. julolidine containing benzo [a] quinolizine ring systems
  • C07C 69/96 - Esters of carbonic or haloformic acids

75.

Quinolone inhibitors of lipoprotein-associated phospholipase A2

      
Application Number 14043624
Grant Number 09512104
Status In Force
Filing Date 2013-10-01
First Publication Date 2015-04-02
Grant Date 2016-12-06
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Rao, Tadimeti
  • Zhang, Chengzhi

Abstract

The present invention relates to new quinolone inhibitors of lipoprotein-associated phospholipase A2 activity, pharmaceutical compositions thereof, and methods of use thereof.

IPC Classes  ?

  • A61K 31/4375 - 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 six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
  • C07D 215/233 - Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 4
  • 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

76.

BENZOQUINOLONE INHIBITORS OF VMAT2

      
Application Number US2014057587
Publication Number 2015/048370
Status In Force
Filing Date 2014-09-26
Publication Date 2015-04-02
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor Zhang, Chengzhi

Abstract

The present invention relates to new benzoquinolone inhibitors of VMAT2, pharmaceutical compositions thereof, and methods of use thereof represented by structural Formula I.

IPC Classes  ?

  • A61K 31/5513 - 1,4-Benzodiazepines, e.g. diazepam
  • A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
  • C07D 455/06 - Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing quinolizine ring systems directly condensed with at least one six-membered carbocyclic ring, e.g. protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing a quinolizine ring system condensed with only one six-membered carbocyclic ring, e.g. julolidine containing benzo [a] quinolizine ring systems

77.

DIHYDROXYPHENYL NEUROTRANSMITTER COMPOUNDS, COMPOSITIONS AND METHODS

      
Document Number 02917159
Status In Force
Filing Date 2014-07-08
Open to Public Date 2015-01-15
Grant Date 2022-08-23
Owner
  • AUSPEX PHARMACEUTICALS, INC. (USA)
  • THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES (USA)
Inventor
  • Goldstein, David S.
  • Holmes, Courtney
  • Alken, Rudolf-Giesbert
  • Schneider, Frank
  • Zhang, Chengzhi

Abstract

The present invention relates to new dihydoxyphenyl modulators of neurotransmitter levels, pharmaceutical compositions thereof, and methods of use thereof

IPC Classes  ?

  • A61K 31/198 - Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
  • A61P 25/00 - Drugs for disorders of the nervous system
  • C07B 59/00 - Introduction of isotopes of elements into organic compounds
  • C07C 229/36 - 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 containing six-membered aromatic rings with at least one amino group and one carboxyl group bound to the same carbon atom of the carbon skeleton

78.

DIHYDROXYPHENYL NEUROTRANSMITTER COMPOUNDS, COMPOSITIONS AND METHODS

      
Application Number US2014045731
Publication Number 2015/006315
Status In Force
Filing Date 2014-07-08
Publication Date 2015-01-15
Owner
  • AUSPEX PHARMACEUTICALS, INC. (USA)
  • THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPT. OF HEALTH & HUMAN SERVICES (USA)
Inventor
  • Goldstein, David, S.
  • Holmes, Courtney
  • Alken, Rudolf-Giesbert
  • Schneider, Frank
  • Zhang, Chengzhi

Abstract

The present invention relates to new dihydoxyphenyl modulators of neurotransmitter levels, pharmaceutical compositions thereof, and methods of use thereof.

IPC Classes  ?

  • C07C 229/08 - 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 the nitrogen atom of the amino group being further bound to hydrogen atoms
  • C07C 229/22 - 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 the carbon skeleton being further substituted by oxygen atoms
  • A61K 31/223 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of alpha-amino acids
  • A61P 25/00 - Drugs for disorders of the nervous system

79.

Formulations and pharmacokinetics of deuterated benzoquinoline inhibitors of vesicular monoamine transporter 2

      
Application Number 14479823
Grant Number 09233959
Status In Force
Filing Date 2014-09-08
First Publication Date 2015-01-01
Grant Date 2016-01-12
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Sommer, Andreas
  • Zhang, Chengzhi
  • Carter, John
  • Arthur, John
  • Bradbury, Margaret
  • Gant, Thomas
  • Shahbaz, Manouchehr

Abstract

The present invention relates to new pharmaceutical compositions comprising benzoquinoline compounds, and methods to inhibit vesicular monoamine transporter 2 (VMAT2) activity in a subject for the treatment of chronic hyperkinetic movement disorders.

IPC Classes  ?

  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
  • C07D 455/06 - Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing quinolizine ring systems directly condensed with at least one six-membered carbocyclic ring, e.g. protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing a quinolizine ring system condensed with only one six-membered carbocyclic ring, e.g. julolidine containing benzo [a] quinolizine ring systems
  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • A61K 9/16 - AgglomeratesGranulatesMicrobeadlets
  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 9/28 - DrageesCoated pills or tablets
  • A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
  • A61K 9/50 - Microcapsules
  • A61K 31/473 - QuinolinesIsoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
  • 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

80.

AUSTEDO

      
Serial Number 86492763
Status Registered
Filing Date 2014-12-30
Registration Date 2017-06-13
Owner Auspex Pharmaceuticals, Inc. ()
NICE Classes  ? 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

Pharmaceutical preparations for the treatment of central nervous system diseases, namely, neurodegeneration, psychiatric conditions, pain, movement disorders

81.

AUSTEDO

      
Serial Number 86492765
Status Registered
Filing Date 2014-12-30
Registration Date 2017-06-13
Owner Auspex Pharmaceuticals, Inc. ()
NICE Classes  ? 05 - Pharmaceutical, veterinary and sanitary products

Goods & Services

Pharmaceutical preparations for the treatment of central nervous system diseases, namely, neurodegeneration, psychiatric conditions, pain, movement disorders

82.

Formulations and pharmacokinetics of deuterated benzoquinoline inhibitors of vesicular monoamine transporter 2

      
Application Number 14245024
Grant Number 09296739
Status In Force
Filing Date 2014-04-04
First Publication Date 2014-11-20
Grant Date 2016-03-29
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Sommer, Andreas
  • Zhang, Chengzhi
  • Carter, John
  • Arthur, John
  • Bradbury, Margaret
  • Gant, Thomas
  • Shahbaz, Manouchehr

Abstract

The present invention relates to new pharmaceutical compositions comprising benzoquinoline compounds, and methods to inhibit vesicular monoamine transporter 2 (VMAT2) activity in a subject for the treatment of chronic hyperkinetic movement disorders.

IPC Classes  ?

  • C07D 471/04 - 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
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
  • C07D 455/06 - Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing quinolizine ring systems directly condensed with at least one six-membered carbocyclic ring, e.g. protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing a quinolizine ring system condensed with only one six-membered carbocyclic ring, e.g. julolidine containing benzo [a] quinolizine ring systems
  • 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 9/00 - Medicinal preparations characterised by special physical form
  • A61K 9/16 - AgglomeratesGranulatesMicrobeadlets
  • A61K 9/20 - Pills, lozenges or tablets
  • A61K 9/28 - DrageesCoated pills or tablets
  • A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
  • A61K 9/50 - Microcapsules
  • A61K 31/473 - QuinolinesIsoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines

83.

Aminopyrimidine inhibitors of tyrosine kinase

      
Application Number 14257347
Grant Number 10568965
Status In Force
Filing Date 2014-04-21
First Publication Date 2014-08-14
Grant Date 2020-02-25
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor Zhang, Chengzhi

Abstract

The present invention relates to new aminopyrimidine inhibitors of tyrosine kinase activity, pharmaceutical compositions thereof, and methods of use thereof.

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
  • 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

84.

BENZOQUINOLONE INHIBITORS OF VMAT2

      
Application Number US2014013327
Publication Number 2014/120654
Status In Force
Filing Date 2014-01-28
Publication Date 2014-08-07
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Sommer, Andreas
  • Zhang, Chengzhi

Abstract

The present invention relates to new benzoquinolone inhibitors of VMAT2, pharmaceutical compositions thereof, and methods of use thereof.

IPC Classes  ?

  • C07D 471/04 - Ortho-condensed systems
  • A61K 31/4375 - 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 six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
  • A61P 21/00 - Drugs for disorders of the muscular or neuromuscular system
  • A61P 25/00 - Drugs for disorders of the nervous system
  • A61P 35/00 - Antineoplastic agents

85.

Pyrimidinone inhibitors of lipoprotein-associated phospholipase A2

      
Application Number 14107953
Grant Number 09585884
Status In Force
Filing Date 2013-12-16
First Publication Date 2014-04-17
Grant Date 2017-03-07
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Rao, Tadimeti
  • Zhang, Chengzhi

Abstract

The present invention relates to new pyrimidinone inhibitors of lipoprotein-associated phospholipase A2 activity, pharmaceutical compositions thereof, and methods of use thereof.

IPC Classes  ?

  • A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
  • 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 9/04 - Inotropic agents, i.e. stimulants of cardiac contractionDrugs for heart failure
  • C07D 239/70 - Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

86.

FORMULATIONS PHARMACOKINETICS OF DEUTERATED BENZOQUINOLINE INHIBITORS OF VESICULAR MONOAMINE TRANSPORTER 2

      
Document Number 02883641
Status In Force
Filing Date 2013-09-18
Open to Public Date 2014-03-27
Grant Date 2021-09-14
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Sommer, Andreas
  • Zhang, Chengzhi
  • Carter, John
  • Arthur, John
  • Bradbury, Margaret
  • Gant, Thomas
  • Shahbaz, Manouchehr

Abstract

The present invention relates to new pharmaceutical compositions comprising benzoquinoline compounds, and methods to inhibit vesicular monoamine transporter 2 (VMAT2) activity in a subject for the treatment of chronic hyperkinetic movement disorders.

IPC Classes  ?

  • A61K 9/00 - Medicinal preparations characterised by special physical form
  • 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 47/38 - CelluloseDerivatives thereof

87.

FORMULATIONS PHARMACOKINETICS OF DEUTERATED BENZOQUINOLINE INHIBITORS OF VESICULAR MONOAMINE TRANSPORTER 2

      
Application Number US2013060387
Publication Number 2014/047167
Status In Force
Filing Date 2013-09-18
Publication Date 2014-03-27
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Sommer, Andreas
  • Zhang, Chengzhi
  • Carter, John
  • Arthur, John
  • Bradbury, Margaret
  • Gant, Thomas
  • Shahbaz, Manouchehr

Abstract

The present invention relates to new pharmaceutical compositions comprising benzoquinoline compounds, and methods to inhibit vesicular monoamine transporter 2 (VMAT2) activity in a subject for the treatment of chronic hyperkinetic movement disorders.

IPC Classes  ?

  • A61K 31/4375 - 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 six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
  • 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 9/20 - Pills, lozenges or tablets

88.

FORMULATIONS PHARMACOKINETICS OF DEUTERATED BENZOQUINOLINE INHIBITORS OF VESICULAR MONOAMINE TRANSPORTER 2

      
Document Number 03124804
Status In Force
Filing Date 2013-09-18
Open to Public Date 2014-03-27
Grant Date 2023-08-22
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Sommer, Andreas
  • Zhang, Chengzhi
  • Carter, John
  • Arthur, John
  • Bradbury, Margaret
  • Gant, Thomas
  • Shahbaz, Manouchehr

Abstract

The present invention relates to new pharmaceutical compositions comprising benzoquinoline compounds, and methods to inhibit vesicular monoamine transporter 2 (VMAT2) activity in a subject for the treatment of chronic hyperkinetic movement disorders. The present invention relates to new pharmaceutical compositions comprising benzoquinoline compounds, and methods to inhibit vesicular monoamine transporter 2 (VMAT2) activity in a subject for the treatment of chronic hyperkinetic movement disorders.

IPC Classes  ?

  • 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
  • A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia

89.

Aminothiazole modulators of beta-3-adrenoreceptor

      
Application Number 13921723
Grant Number 09029407
Status In Force
Filing Date 2013-06-19
First Publication Date 2013-10-24
Grant Date 2015-05-12
Owner Auspex Pharmaceuticals, Inc. (USA)
Inventor
  • Rao, Tadimeti
  • Zhang, Chengzhi

Abstract

The present invention relates to new aminothiazole modulators of beta-3-adrenoreceptor activity, pharmaceutical compositions thereof, and methods of use thereof.

IPC Classes  ?

  • A61K 31/425 - Thiazoles
  • C07D 277/40 - Unsubstituted amino or imino radicals
  • C07D 277/22 - Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
  • A61K 31/426 - 1,3-Thiazoles
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

90.

Piperidine inhibitors of janus kinase 3

      
Application Number 13627747
Grant Number 08962638
Status In Force
Filing Date 2012-09-26
First Publication Date 2013-02-14
Grant Date 2015-02-24
Owner Auspex Pharmaceuticals, Inc. (USA)
Inventor
  • Rao, Tadimeti
  • Zhang, Chengzhi

Abstract

The present invention relates to new piperidine inhibitors of Janus kinase 3 activity, pharmaceutical compositions thereof, and methods of use thereof.

IPC Classes  ?

  • A01N 43/90 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having two or more relevant hetero rings, condensed among themselves or with a common carbocyclic ring system
  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • C07D 487/00 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups
  • C07D 487/04 - Ortho-condensed systems

91.

SUBSTITUTED N-ARYL PYRIDINONES

      
Application Number US2012027872
Publication Number 2012/122165
Status In Force
Filing Date 2012-03-06
Publication Date 2012-09-13
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Zhang, Chengzhi
  • Sommers, Andreas

Abstract

Disclosed herein are methods of administering deuterated pirfenidone and kits thereof.

IPC Classes  ?

  • A61K 31/4412 - Non-condensed pyridinesHydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
  • A61K 31/4418 - Non-condensed pyridinesHydrogenated derivatives thereof having a carbocyclic ring directly attached to the heterocyclic ring, e.g. cyproheptadine
  • C07D 213/64 - One oxygen atom attached in position 2 or 6
  • A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
  • A61P 19/00 - Drugs for skeletal disorders

92.

Pyrimidinone inhibitors of lipoprotein-associated phospholipase A2

      
Application Number 12840725
Grant Number 08637524
Status In Force
Filing Date 2010-07-21
First Publication Date 2011-12-15
Grant Date 2014-01-28
Owner Auspex Pharmaceuticals, Inc (USA)
Inventor
  • Rao, Tadimeti
  • Zhang, Chengzhi

Abstract

The present invention relates to new pyrimidinone inhibitors of lipoprotein-associated phospholipase A2 activity, pharmaceutical compositions thereof, and methods of use thereof

IPC Classes  ?

  • C07D 239/78 - QuinazolinesHydrogenated quinazolines with hetero atoms directly attached in position 2
  • A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
  • A61P 11/06 - Antiasthmatics
  • 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

93.

BENZOQUINOLONE INHIBITORS OF VMAT2

      
Application Number US2011038592
Publication Number 2011/153157
Status In Force
Filing Date 2011-05-31
Publication Date 2011-12-08
Owner AUSPEX PHARMACEUTICAL, INC. (USA)
Inventor
  • Gant, Thomas, G.
  • Zhang, Chengzhi
  • Shahbaz, Manouchehr

Abstract

The present invention relates to new benzoquinolone inhibitors of VMAT2, pharmaceutical compositions thereof, and methods of use thereof.Formula (I)

IPC Classes  ?

  • C07D 471/04 - Ortho-condensed systems
  • A61K 31/4375 - 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 six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
  • A61P 25/00 - Drugs for disorders of the nervous system
  • A61P 35/00 - Antineoplastic agents

94.

MACROLIDE INHIBITORS OF MTOR

      
Application Number US2011030507
Publication Number 2011/123524
Status In Force
Filing Date 2011-03-30
Publication Date 2011-10-06
Owner AUSPEX PHARMACEUTICAL, INC. (USA)
Inventor Zhang, Chengzhi

Abstract

The present invention relates to new macrolide inhibitors of mTOR, pharmaceutical compositions thereof, and methods of use thereof (Formula I).

IPC Classes  ?

  • C07D 498/14 - Ortho-condensed systems
  • C07D 498/16 - Peri-condensed systems
  • A61K 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
  • A61K 31/33 - Heterocyclic compounds
  • A61P 35/00 - Antineoplastic agents

95.

TRIMETHOXYPHENYL INHIBITORS OF TYROSINE KINASE

      
Application Number US2011025368
Publication Number 2011/106248
Status In Force
Filing Date 2011-02-18
Publication Date 2011-09-01
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Zhang, Chengzhi
  • Sommers, Andreas

Abstract

The present invention relates to new trimethoxyphenyl inhibitors of tyrosine kinase, pharmaceutical compositions thereof, and methods of use thereof. (I)

IPC Classes  ?

  • C07D 498/04 - Ortho-condensed systems
  • A61K 31/5383 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
  • A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
  • A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
  • A61P 35/00 - Antineoplastic agents

96.

4,6-diaminopyrimidine stimulators of soluble guanylate cyclase

      
Application Number 12911268
Grant Number 09260424
Status In Force
Filing Date 2010-10-25
First Publication Date 2011-08-18
Grant Date 2016-02-16
Owner Auspex Pharmaceuticals, Inc. (USA)
Inventor
  • Rao, Tadimeti
  • Zhang, Chengzhi

Abstract

The present invention relates to new 4,6-diaminopyrimidine stimulators of soluble guanylate cyclase, pharmaceutical compositions thereof, and methods of use thereof

IPC Classes  ?

  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic 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
  • A61P 11/00 - Drugs for disorders of the respiratory system
  • A61P 19/10 - Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
  • 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 9/12 - Antihypertensives
  • A61P 25/06 - Antimigraine agents
  • A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
  • A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
  • C07D 471/04 - Ortho-condensed 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 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

97.

Quinolone inhibitors of lipoprotein-associated phospholipase A2

      
Application Number 12845384
Grant Number 08575348
Status In Force
Filing Date 2010-07-28
First Publication Date 2011-06-09
Grant Date 2013-11-05
Owner Auspex Pharmaceuticals, Inc (USA)
Inventor
  • Rao, Tadimeti
  • Zhang, Chengzhi

Abstract

The present invention relates to new quinolone inhibitors of lipoprotein-associated phospholipase A2 activity, pharmaceutical compositions thereof, and methods of use thereof.

IPC Classes  ?

98.

CYCLOHEXYL UREA MODULATORS OF D2 RECEPTORS AND/OR D3 RECEPTORS

      
Application Number US2010056714
Publication Number 2011/060363
Status In Force
Filing Date 2010-11-15
Publication Date 2011-05-19
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Newbold, Ronald
  • Zhang, Chengzhi

Abstract

The present invention relates to new cyclohexyl urea modulators of D2 receptors and/or modulators of D3 receptors, pharmaceutical compositions thereof, and methods of use thereof.

IPC Classes  ?

  • C07D 295/033 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms containing only hydrogen and carbon atoms in addition to the ring hetero elements containing only one hetero ring with the ring nitrogen atoms directly attached to carbocyclic rings
  • 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
  • A61P 25/00 - Drugs for disorders of the nervous system

99.

4,6-DIAMINOPYRIMIDINE STIMULATORS OF SOLUBLE GUANYLATE CYCLASE

      
Application Number US2010053969
Publication Number 2011/056511
Status In Force
Filing Date 2010-10-25
Publication Date 2011-05-12
Owner AUSPEX PHARMACEUTICALS, INC. (USA)
Inventor
  • Rao, Tadimeti
  • Zhang, Chengzhi

Abstract

The present invention relates to new 4,6-diaminopyrimidine stimulators of soluble guanylate cyclase, pharmaceutical compositions thereof, and methods of use thereof.

IPC Classes  ?

  • C07D 471/04 - Ortho-condensed systems
  • 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 31/437 - 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 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • A61P 9/12 - Antihypertensives
  • A61P 11/06 - Antiasthmatics
  • 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 19/10 - Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis

100.

Aminothiazole modulators of beta-3-adrenoreceptor

      
Application Number 12796781
Grant Number 08586760
Status In Force
Filing Date 2010-06-09
First Publication Date 2011-04-07
Grant Date 2013-11-19
Owner Auspex Pharmaceuticals, Inc. (USA)
Inventor
  • Rao, Tadimeti
  • Zhang, Chengzhi

Abstract

The present invention relates to new aminothiazole modulators of beta-3-adrenoreceptor activity, pharmaceutical compositions thereof, and methods of use thereof.

IPC Classes  ?

  • C07D 277/20 - Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
  • A61K 31/425 - Thiazoles
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