Janssen Biopharma, Inc.

United States of America

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IPC Class
C07H 19/16 - Purine radicals 14
C07H 19/06 - Pyrimidine radicals 13
C07H 19/20 - Purine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids 13
C07H 19/10 - Pyrimidine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids 12
A61P 31/16 - Antivirals for RNA viruses for influenza or rhinoviruses 9
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Found results for  patents

1.

Modified Nucleoside Phosphoramidites

      
Application Number 18672651
Status Pending
Filing Date 2024-05-23
First Publication Date 2024-09-19
Owner Janssen BioPharma, Inc. (USA)
Inventor
  • Gryaznov, Sergei
  • Hong, Jin
  • Rajwanshi, Vivek Kumar
  • Beigelman, Leonid

Abstract

The present disclosure relates to compounds and compositions containing 5′-phosphoramidite nucleoside monomers, and methods of making and use.

IPC Classes  ?

  • C07H 19/10 - Pyrimidine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids
  • C07H 1/00 - Processes for the preparation of sugar derivatives
  • C07H 19/20 - Purine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids

2.

SYNTHESIS OF OLIGONUCLEOTIDES AND RELATED COMPOUNDS

      
Application Number 17916064
Status Pending
Filing Date 2021-03-30
First Publication Date 2024-03-21
Owner JANSSEN BIOPHARMA, INC. (USA)
Inventor
  • Zhong, Minghong
  • Jin, Yi
  • Gala, Dinesh
  • Prhavc, Marija

Abstract

Methods of synthesizing oligonucleotides via new intermediates on a cleavable support having an azidomethyl moiety are disclosed. The method comprises multiple reaction cycles, each of which comprises sequential coupling a nucleoside or oligonucleotide subunit on a cleavable support having an azidomethyl moiety and a nucleoside phosphoramidite or an oligonucleotide phosphoramidite, capping, oxidation/thiolation and deblocking; followed by orthogonal cleavage of the azidomethyl support while keeping all other protecting groups intact. The method can be used in combination with a support moiety for either solid phase or liquid phase oligo synthesis. The soluble support facilitates homogeneous reactions and efficient separations by simple precipitation. The methods also provide novel intermediates useful in the synthesis of oligonucleotide conjugates.

IPC Classes  ?

  • C07H 21/02 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with ribosyl as saccharide radical
  • C07H 19/067 - Pyrimidine radicals with ribosyl as the saccharide radical
  • C07H 19/167 - Purine radicals with ribosyl as the saccharide radical

3.

SYNTHESIS OF 3'N NUCLEOSIDES THROUGH OXIME INTERMEDIATES AND RELATED COMPOUNDS

      
Application Number 17912418
Status Pending
Filing Date 2021-03-15
First Publication Date 2023-06-29
Owner JANSSEN BIOPHARMA, INC. (USA)
Inventor
  • Gryaznov, Sergei
  • Rajwanshi, Vivek Kumar
  • Houpis, Ioannis N.

Abstract

Provided herein are novel synthetic routes to amines through an oxime intermediate, e.g., 3′-N nucleosides and novel and intermediate compounds produced during these synthetic procedures.

IPC Classes  ?

  • C07H 1/00 - Processes for the preparation of sugar derivatives
  • C07H 19/06 - Pyrimidine radicals
  • C07H 19/16 - Purine radicals
  • C12N 15/11 - DNA or RNA fragmentsModified forms thereof
  • C07H 19/10 - Pyrimidine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids
  • C07H 19/20 - Purine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids

4.

COMPOUNDS FOR THE TREATMENT OF PARAMYXOVIRUS VIRAL INFECTIONS

      
Application Number 17228573
Status Pending
Filing Date 2021-04-12
First Publication Date 2022-12-15
Owner Janssen BioPharma, Inc. (USA)
Inventor
  • Wang, Guangyi
  • Beigelman, Leonid
  • Truong, Anh
  • Napolitano, Carmela
  • Andreotti, Daniele
  • He, Haiying

Abstract

Disclosed herein are new antiviral compounds, together with pharmaceutical compositions that include one or more antiviral compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus viral infection with one or more small molecule compounds. Examples of paramyxovirus infection include an infection caused by human respiratory syncytial virus (RSV).

IPC Classes  ?

  • C07D 495/04 - Ortho-condensed systems
  • A61K 31/352 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. cannabinols, methantheline
  • A61K 31/4196 - 1,2,4-Triazoles
  • A61K 31/4365 - 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 having sulfur as a ring hetero atom, e.g. ticlopidine
  • C07C 255/66 - Carboxylic acid nitriles containing cyano groups and nitrogen atoms further bound to other hetero atoms, other than oxygen atoms of nitro or nitroso groups, bound to the same carbon skeleton with the nitrogen atoms further bound to nitrogen atoms having cyano groups and nitrogen atoms being part of hydrazine or hydrazone groups bound to the same carbon skeleton
  • C07D 233/88 - Nitrogen atoms, e.g. allantoin
  • C07D 261/20 - Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings condensed with carbocyclic rings or ring systems
  • C07D 307/40 - Radicals substituted by oxygen atoms
  • C07D 307/52 - Radicals substituted by nitrogen atoms not forming part of a nitro radical
  • C07D 333/20 - Radicals substituted by singly bound hetero atoms other than halogen by nitrogen atoms
  • C07D 333/58 - Radicals substituted by nitrogen atoms
  • A61K 31/4025 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
  • A61K 31/404 - Indoles, e.g. pindolol
  • A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
  • 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 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
  • C07D 213/50 - Ketonic radicals
  • C07D 233/64 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
  • C07D 333/68 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
  • C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 409/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • A61K 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
  • A61K 31/382 - Heterocyclic compounds having sulfur as a ring hetero atom having six-membered rings, e.g. thioxanthenes
  • A61K 31/426 - 1,3-Thiazoles
  • A61K 31/4418 - Non-condensed pyridinesHydrogenated derivatives thereof having a carbocyclic ring directly attached to the heterocyclic ring, e.g. cyproheptadine
  • 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
  • C07C 251/84 - Hydrazones having doubly-bound carbon atoms of hydrazone groups being part of rings other than six-membered aromatic rings
  • C07D 207/335 - Radicals substituted by nitrogen atoms not forming part of a nitro radical
  • C07D 215/12 - Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
  • C07D 215/42 - Nitrogen atoms attached in position 4
  • C07D 233/61 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms not forming part of a nitro radical, attached to ring nitrogen atoms
  • C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
  • A61K 31/277 - NitrilesIsonitriles having a ring, e.g. verapamil
  • A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
  • A61K 31/423 - Oxazoles condensed with carbocyclic rings
  • A61K 31/4436 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
  • 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 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
  • A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • C07C 243/34 - Hydrazines having nitrogen atoms of hydrazine groups acylated by carboxylic acids with acylating carboxyl groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of a carbon skeleton further substituted by nitrogen atoms
  • C07D 209/20 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals substituted additionally by nitrogen atoms, e.g. tryptophane
  • C07D 209/86 - CarbazolesHydrogenated carbazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the ring system
  • C07D 233/38 - One oxygen atom with acyl radicals or hetero atoms directly attached to ring nitrogen atoms
  • C07D 233/60 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms with hydrocarbon radicals, substituted by oxygen or sulfur atoms, attached to ring nitrogen atoms
  • C07D 277/64 - Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2
  • C07D 307/81 - Radicals substituted by nitrogen atoms not forming part of a nitro radical
  • C07D 405/10 - 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 carbon chain containing aromatic rings
  • C07D 417/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
  • A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
  • A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
  • C07C 243/18 - Hydrazines having nitrogen atoms of hydrazine groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing rings
  • C07D 277/56 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
  • C07D 333/66 - Nitrogen atoms not forming part of a nitro radical
  • C07D 413/04 - 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 directly linked by a ring-member-to-ring- member bond
  • C07D 471/04 - Ortho-condensed systems
  • C07D 495/14 - Ortho-condensed systems
  • A61K 31/4427 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems
  • A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
  • C07D 213/42 - Radicals substituted by singly-bound nitrogen atoms having hetero atoms attached to the substituent nitrogen atom
  • C07D 213/68 - One oxygen atom attached in position 4
  • C07D 215/38 - Nitrogen atoms
  • C07D 217/24 - Oxygen atoms
  • C07D 307/91 - DibenzofuransHydrogenated dibenzofurans
  • C07D 311/68 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulfur atoms in position 2 or 4 with nitrogen atoms directly attached in position 4
  • C07D 333/16 - Radicals substituted by singly bound hetero atoms other than halogen by oxygen atoms
  • C07D 333/62 - Benzo [b] thiophenesHydrogenated benzo [b] thiophenes with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
  • C07D 401/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
  • C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
  • A61K 31/341 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
  • A61K 31/4164 - 1,3-Diazoles
  • A61K 31/428 - Thiazoles condensed with carbocyclic rings
  • A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
  • A61K 31/4704 - 2-Quinolinones, e.g. carbostyril
  • A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • C07C 255/34 - Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring with cyano groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by unsaturated carbon chains
  • C07D 209/08 - IndolesHydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
  • C07D 215/14 - Radicals substituted by oxygen atoms
  • C07D 333/54 - Benzo [b] thiophenesHydrogenated benzo [b] thiophenes with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
  • C07D 335/06 - BenzothiopyransHydrogenated benzothiopyrans
  • C07D 405/04 - 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 directly linked by a ring-member-to-ring- member bond
  • C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 409/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
  • A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
  • A61K 31/4155 - 1,2-Diazoles not condensed and containing further heterocyclic rings
  • A61K 31/47 - QuinolinesIsoquinolines
  • A61K 31/538 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
  • C07C 251/80 - Hydrazones having doubly-bound carbon atoms of hydrazone groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of an unsaturated carbon skeleton the carbon skeleton containing rings
  • C07D 209/14 - Radicals substituted by nitrogen atoms, not forming part of a nitro radical
  • C07D 213/65 - One oxygen atom attached in position 3 or 5
  • C07D 333/50 - Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
  • C07D 333/76 - Dibenzothiophenes

5.

Modified nucleoside phosphoramidites

      
Application Number 17514168
Grant Number 12030907
Status In Force
Filing Date 2021-10-29
First Publication Date 2022-02-17
Grant Date 2024-07-09
Owner Janssen BioPharma, Inc. (USA)
Inventor
  • Gryaznov, Sergei
  • Hong, Jin
  • Rajwanshi, Vivek Kumar
  • Beigelman, Leonid

Abstract

A method of making a compound represented by Formula (I): 4 is independently in each instance H or F; a is 1 or 2; and b is 1, 2, or 3.

IPC Classes  ?

  • C07H 19/10 - Pyrimidine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids
  • C07H 1/00 - Processes for the preparation of sugar derivatives
  • C07H 19/20 - Purine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids

6.

POLYNUCLEOTIDE CONSTRUCTS AND USES THEREOF

      
Application Number IB2021057497
Publication Number 2022/034555
Status In Force
Filing Date 2021-08-13
Publication Date 2022-02-17
Owner JANSSEN BIOPHARMA, INC. (USA)
Inventor
  • Ushach, Irina
  • Yun, Theodore

Abstract

Oligodeoxynucleotide-based immunostimulatory Toll-Like Receptor 9 (TLR9) agonists are described. Also described are compositions comprising the TLR9 agonists, methods of making the TLR9 agonists, and methods of using the TLR9 agonists to treat immune diseases, disorders or conditions.

IPC Classes  ?

  • C12N 15/117 - Nucleic acids having immunomodulatory properties, e.g. containing CpG-motifs

7.

SYNTHESIS OF OLIGONUCLEOTIDES AND RELATED COMPOUNDS

      
Document Number 03178892
Status Pending
Filing Date 2021-03-30
Open to Public Date 2021-10-07
Owner JANSSEN BIOPHARMA, INC. (USA)
Inventor
  • Zhong, Minghong
  • Jin, Yi
  • Gala, Dinesh
  • Prhavc, Marija

Abstract

Methods of synthesizing oligonucleotides via new intermediates on a cleavable support having an azidomethyl moiety are disclosed. The method comprises multiple reaction cycles, each of which comprises sequential coupling a nucleoside or oligonucleotide subunit on a cleavable support having an azidomethyl moiety and a nucleoside phosphoramidite or an oligonucleotide phosphoramidite, capping, oxidation/thiolation and deblocking; followed by orthogonal cleavage of the azidomethyl support while keeping all other protecting groups intact. The method can be used in combination with a support moiety for either solid phase or liquid phase oligo synthesis. The soluble support facilitates homogeneous reactions and efficient separations by simple precipitation. The methods also provide novel intermediates useful in the synthesis of oligonucleotide conjugates.

IPC Classes  ?

  • C07H 1/00 - Processes for the preparation of sugar derivatives
  • C07H 19/067 - Pyrimidine radicals with ribosyl as the saccharide radical
  • C07H 19/167 - Purine radicals with ribosyl as the saccharide radical
  • C07H 21/02 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with ribosyl as saccharide radical

8.

ANTIVIRAL COMPOUNDS AND USES THEREOF

      
Application Number IB2021052750
Publication Number 2021/198981
Status In Force
Filing Date 2021-04-01
Publication Date 2021-10-07
Owner JANSSEN BIOPHARMA, INC. (USA)
Inventor
  • Beigelman, Leonid
  • Grosse, Sandrine Celine
  • Matcha, Kiran
  • Mc Gowan, David Craig
  • Stein, Karin Ann
  • Truong, Anh Pham
  • Wang, Guangyi

Abstract

Compounds for inhibiting replication of a respiratory syncytial virus (RSV) are provided. The compounds may find use as therapeutic agents for treating or preventing an RSV infection.

IPC Classes  ?

9.

SYNTHESIS OF OLIGONUCLEOTIDES AND RELATED COMPOUNDS

      
Application Number IB2021052595
Publication Number 2021/198883
Status In Force
Filing Date 2021-03-30
Publication Date 2021-10-07
Owner JANSSEN BIOPHARMA, INC. (USA)
Inventor
  • Zhong, Minghong
  • Jin, Yi
  • Gala, Dinesh
  • Prhavc, Marija

Abstract

Methods of synthesizing oligonucleotides via new intermediates on a cleavable support having an azidomethyl moiety are disclosed. The method comprises multiple reaction cycles, each of which comprises sequential coupling a nucleoside or oligonucleotide subunit on a cleavable support having an azidomethyl moiety and a nucleoside phosphoramidite or an oligonucleotide phosphoramidite, capping, oxidation/thiolation and deblocking; followed by orthogonal cleavage of the azidomethyl support while keeping all other protecting groups intact. The method can be used in combination with a support moiety for either solid phase or liquid phase oligo synthesis. The soluble support facilitates homogeneous reactions and efficient separations by simple precipitation. The methods also provide novel intermediates useful in the synthesis of oligonucleotide conjugates.

IPC Classes  ?

  • C07H 1/00 - Processes for the preparation of sugar derivatives
  • C07H 19/067 - Pyrimidine radicals with ribosyl as the saccharide radical
  • C07H 19/167 - Purine radicals with ribosyl as the saccharide radical
  • C07H 21/02 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with ribosyl as saccharide radical

10.

NUCLEIC ACID POLYMERS

      
Application Number IB2021052704
Publication Number 2021/198958
Status In Force
Filing Date 2021-03-31
Publication Date 2021-10-07
Owner JANSSEN BIOPHARMA, INC. (USA)
Inventor
  • Gryaznov, Sergei
  • Pandarinathan, Lakshmipathi

Abstract

A nucleic acid polymer comprising 8 to 50 nucleoside subunits linked by intersubunit linkages, wherein the nucleic acid polymer comprises (A) one or more 3'-5' thiophosphoramidate intersubunit linkage and the remaining intersubunit linkages are 3'-5' thiophosphate intersubunit linkages and/or (B) at least 40% of the nucleoside subunits contain a 2'-MOE substituent. Those nucleic acid polymers are useful in the treatment of a viral infection, more specifically Hepatitis B virus and/or Hepatitis D virus.

IPC Classes  ?

  • C07H 21/00 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
  • C07H 1/00 - Processes for the preparation of sugar derivatives
  • C07H 19/06 - Pyrimidine radicals
  • C07H 19/16 - Purine radicals
  • A61P 31/14 - Antivirals for RNA viruses

11.

HETEROARYL-SUBSTITUTED MACROCYCLIC FLU ENDONUCLEASE INHIBITORS

      
Application Number IB2021052544
Publication Number 2021/191872
Status In Force
Filing Date 2021-03-26
Publication Date 2021-09-30
Owner JANSSEN BIOPHARMA, INC. (USA)
Inventor
  • Hendricks, Robert Than
  • Stoycheva, Antitsa Dimitrova
  • Bonfanti, Jean-François
  • Raboisson, Pierre Jean-Marie Bernard
  • Fortin, Jèrôme Michel Claude
  • Mercey, Guillaume Jean Maurice

Abstract

OrthomyxoviridaeOrthomyxoviridaeOrthomyxoviridae family.

IPC Classes  ?

  • C07D 498/18 - Bridged systems
  • A61P 31/16 - Antivirals for RNA viruses for influenza or rhinoviruses
  • A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine

12.

SYNTHESIS OF 3'N NUCLEOSIDES THROUGH OXIME INTERMEDIATES AND RELATED COMPOUNDS

      
Document Number 03176112
Status Pending
Filing Date 2021-03-15
Open to Public Date 2021-09-23
Owner JANSSEN BIOPHARMA, INC. (USA)
Inventor
  • Gryaznov, Sergei
  • Rajwanshi, Vivek Kumar
  • Houpis, Ioannis N.

Abstract

Provided herein are novel synthetic routes to amines through an oxime intermediate, e.g., 3'-N nucleosides and novel and intermediate compounds produced during these synthetic procedures.

IPC Classes  ?

  • C07H 1/00 - Processes for the preparation of sugar derivatives
  • C07H 19/00 - Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radicalNucleosidesMononucleotidesAnhydro derivatives thereof
  • C07H 19/067 - Pyrimidine radicals with ribosyl as the saccharide radical
  • C07H 19/167 - Purine radicals with ribosyl as the saccharide radical
  • C07H 21/00 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids

13.

SYNTHESIS OF 3'N NUCLEOSIDES THROUGH OXIME INTERMEDIATES AND RELATED COMPOUNDS

      
Application Number IB2021052141
Publication Number 2021/186328
Status In Force
Filing Date 2021-03-15
Publication Date 2021-09-23
Owner JANSSEN BIOPHARMA, INC. (USA)
Inventor
  • Gryaznov, Sergei
  • Rajwanshi, Vivek Kumar
  • Houpis, Ioannis N.

Abstract

Provided herein are novel synthetic routes to amines through an oxime intermediate, e.g., 3'-N nucleosides and novel and intermediate compounds produced during these synthetic procedures.

IPC Classes  ?

  • C07H 1/00 - Processes for the preparation of sugar derivatives
  • C07H 19/00 - Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radicalNucleosidesMononucleotidesAnhydro derivatives thereof
  • C07H 19/067 - Pyrimidine radicals with ribosyl as the saccharide radical
  • C07H 19/167 - Purine radicals with ribosyl as the saccharide radical
  • C07H 21/00 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids

14.

METHOD FOR SYNTHESIS OF 2'-ALKYL- OR 2'-ALKENYL- OR 2'-ALKYNYL-4'-FLUORO-ADENOSINE DERIVATIVES AND INTERMEDIATES THEREOF

      
Application Number IB2021050106
Publication Number 2021/140471
Status In Force
Filing Date 2021-01-07
Publication Date 2021-07-15
Owner JANSSEN BIOPHARMA, INC. (USA)
Inventor
  • Zhang, Hai-Ren
  • Serebryany, Vladimir

Abstract

A method of making nucleoside 1, which has a 3-hydrocarbyl-5-fluoro-5-(hydroxy-methyl)tetrahydrofuran-3,4-diol ring system, where hydrocarbyl group R1 is lower alkyl, lower alkenyl, or lower alkynyl and R2 may be an adenine moiety having an exocyclic amino group protected as an imidodicarbonate or as a carbamate. Nucleoside 1 is prepared from an intermediate 4 by adding iodine fluoride across the exocyclic double bond to produce a 5-fluoro-5-iodomethyl derivative 5. The iodine atom is displaced with a carboxylic acid nucleophile in the presence of an oxidizing agent to produce a 5-fluoro-5-(acyloxy)methyl ester derivative 7, where R3 is an acyl group. Ester 7 may be converted into compound 1 by cleavage of the ester.

IPC Classes  ?

  • C07H 1/00 - Processes for the preparation of sugar derivatives
  • C07H 19/167 - Purine radicals with ribosyl as the saccharide radical

15.

TOLL-LIKE RECEPTOR 7 AND/OR 8 AGONISTS AND USES THEREOF

      
Application Number IB2020059178
Publication Number 2021/064614
Status In Force
Filing Date 2020-09-30
Publication Date 2021-04-08
Owner JANSSEN BIOPHARMA, INC. (USA)
Inventor
  • Gryaznov, Sergei
  • Yun, Theodore
  • Beigelman, Leonid

Abstract

RNA oligonucleotide-based immunostimulatory Toll-Like Receptor 7 (TLR7) and/or TLR8 agonists are described. Also described are compositions comprising the TLR7 and/or TLR8 agonists, methods of making the TLR7 and/or TLR8 agonists, and methods of using the TLR7 and/or TLR8 agonists to treat immune diseases, disorders or conditions, such as viral infections or cancer.

IPC Classes  ?

  • A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
  • A61K 47/22 - Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
  • A61K 47/28 - Steroids, e.g. cholesterol, bile acids or glycyrrhetinic acid
  • A61P 35/00 - Antineoplastic agents

16.

Substituted nucleosides, nucleotides and analogs thereof

      
Application Number 16130971
Grant Number RE048171
Status In Force
Filing Date 2014-09-18
First Publication Date 2020-08-25
Grant Date 2020-08-25
Owner Janssen BioPharma, Inc. (USA)
Inventor
  • Wang, Guangyi
  • Smith, David Bernard
  • Beigelman, Leonid
  • Deval, Jerome
  • Prhavc, Marija

Abstract

Disclosed herein are nucleosides, nucleotides and analogs thereof, pharmaceutical compositions that include one or more of nucleosides, nucleotides and analogs thereof, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a disease and/or a condition, including an infection from a paramyxovirus and/or an orthomyxovirus, with a nucleoside, a nucleotide and an analog thereof.

IPC Classes  ?

  • C07H 19/06 - Pyrimidine radicals
  • A61K 31/708 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid having oxo groups directly attached to the purine ring system, e.g. guanosine, guanylic acid
  • A61K 31/706 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
  • C07H 19/20 - Purine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids
  • A61K 31/7076 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
  • C07H 19/12 - Triazine radicals
  • C07H 19/207 - Purine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids the phosphoric or polyphosphoric acids being esterified by a further hydroxylic compound, e.g. flavine-adenine dinucleotide or nicotinamide-adenine dinucleotide
  • A61K 31/7068 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
  • C07H 19/16 - Purine radicals
  • A61K 31/7072 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
  • C07H 19/10 - Pyrimidine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids

17.

ANTIVIRAL NUCLEOSIDES AND DERIVATIVES THEREOF

      
Application Number IB2020050747
Publication Number 2020/157694
Status In Force
Filing Date 2020-01-30
Publication Date 2020-08-06
Owner JANSSEN BIOPHARMA, INC. (USA)
Inventor
  • Beigelman, Leonid
  • Wang, Guangyi
  • Dyatkina, Natalia

Abstract

Disclosed herein are nucleoside compounds and derivatives thereof, pharmaceutical compositions containing same, and their methods of synthesis. The compounds are useful in treating orthomyxovirus infections, such as influenza infections.

IPC Classes  ?

  • C07D 417/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • C07F 9/117 - Esters of phosphoric acids with cycloaliphatic alcohols
  • A61P 31/16 - Antivirals for RNA viruses for influenza or rhinoviruses
  • A61K 31/661 - Phosphorus acids or esters thereof not having P—C bonds, e.g. fosfosal, dichlorvos, malathion
  • A61K 31/6615 - Compounds having two or more esterified phosphorus acid groups, e.g. inositol triphosphate, phytic acid

18.

ANTIVIRAL NUCLEOSIDES AND DERIVATIVES THEREOF

      
Document Number 03128455
Status Pending
Filing Date 2020-01-30
Open to Public Date 2020-08-06
Owner JANSSEN BIOPHARMA, INC. (USA)
Inventor
  • Beigelman, Leonid
  • Wang, Guangyi
  • Dyatkina, Natalia

Abstract

Disclosed herein are nucleoside compounds and derivatives thereof, pharmaceutical compositions containing same, and their methods of synthesis. The compounds are useful in treating orthomyxovirus infections, such as influenza infections.

IPC Classes  ?

  • C07D 417/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • A61K 31/661 - Phosphorus acids or esters thereof not having P—C bonds, e.g. fosfosal, dichlorvos, malathion
  • A61K 31/6615 - Compounds having two or more esterified phosphorus acid groups, e.g. inositol triphosphate, phytic acid
  • A61P 31/16 - Antivirals for RNA viruses for influenza or rhinoviruses
  • C07F 9/117 - Esters of phosphoric acids with cycloaliphatic alcohols

19.

CYCLOBUTYL NUCLEOSIDE ANALOGS AS ANTI-VIRALS

      
Document Number 03122470
Status Pending
Filing Date 2019-12-04
Open to Public Date 2020-06-18
Owner JANSSEN BIOPHARMA, INC. (USA)
Inventor
  • Zhong, Minghong
  • Wang, Guangyi

Abstract

Described herein are cyclobutyl nucleoside analogs of Formula (I), pharmaceutical compositions that include one or more cyclobutyl nucleoside analogs and methods of using the same to treat HBV, HDV and/or HIV.

IPC Classes  ?

  • C07D 239/47 - One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
  • A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
  • A61K 31/52 - Purines, e.g. adenine
  • A61K 31/522 - Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
  • A61K 31/6615 - Compounds having two or more esterified phosphorus acid groups, e.g. inositol triphosphate, phytic acid
  • A61K 31/664 - Amides of phosphorus acids
  • A61K 31/685 - Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols one of the hydroxy compounds having nitrogen atoms, e.g. phosphatidylserine, lecithin
  • A61P 31/12 - Antivirals
  • A61P 31/20 - Antivirals for DNA viruses
  • C07D 239/54 - Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
  • C07D 473/18 - Heterocyclic compounds containing purine ring systems with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6 one oxygen and one nitrogen atom, e.g. guanine
  • C07D 473/34 - Nitrogen atom attached in position 6, e.g. adenine
  • C07D 487/04 - Ortho-condensed systems
  • C07F 9/09 - Esters of phosphoric acids
  • C07F 9/24 - Esteramides

20.

CYCLOBUTYL NUCLEOSIDE ANALOGS AS ANTI-VIRALS

      
Application Number IB2019060430
Publication Number 2020/121122
Status In Force
Filing Date 2019-12-04
Publication Date 2020-06-18
Owner JANSSEN BIOPHARMA, INC. (USA)
Inventor
  • Zhong, Minghong
  • Wang, Guangyi

Abstract

Described herein are cyclobutyl nucleoside analogs of Formula (I), pharmaceutical compositions that include one or more cyclobutyl nucleoside analogs and methods of using the same to treat HBV, HDV and/or HIV.

IPC Classes  ?

  • C07D 239/47 - One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
  • C07D 239/54 - Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
  • C07D 473/18 - Heterocyclic compounds containing purine ring systems with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6 one oxygen and one nitrogen atom, e.g. guanine
  • C07D 473/34 - Nitrogen atom attached in position 6, e.g. adenine
  • C07D 487/04 - Ortho-condensed systems
  • C07F 9/09 - Esters of phosphoric acids
  • C07F 9/24 - Esteramides
  • A61P 31/12 - Antivirals
  • A61P 31/20 - Antivirals for DNA viruses
  • A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
  • A61K 31/52 - Purines, e.g. adenine
  • A61K 31/522 - Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
  • A61K 31/6615 - Compounds having two or more esterified phosphorus acid groups, e.g. inositol triphosphate, phytic acid
  • A61K 31/664 - Amides of phosphorus acids
  • A61K 31/685 - Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols one of the hydroxy compounds having nitrogen atoms, e.g. phosphatidylserine, lecithin

21.

CYCLOPENTYL NUCLEOSIDE ANALOGS AS ANTI-VIRALS

      
Application Number IB2019060431
Publication Number 2020/121123
Status In Force
Filing Date 2019-12-04
Publication Date 2020-06-18
Owner JANSSEN BIOPHARMA, INC. (USA)
Inventor
  • Zhong, Minghong
  • Wang, Guangyi

Abstract

Described herein are cyclopentyl nucleoside analogs of Formula (I), pharmaceutical compositions that include one or more cyclopentyl nucleoside analogs and methods of using the same to treat HBV, HDV and/or HIV. (I)

IPC Classes  ?

  • C07D 239/47 - One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
  • C07D 239/54 - Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
  • C07D 473/18 - Heterocyclic compounds containing purine ring systems with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6 one oxygen and one nitrogen atom, e.g. guanine
  • C07D 473/34 - Nitrogen atom attached in position 6, e.g. adenine
  • C07D 487/04 - Ortho-condensed systems
  • C07F 9/09 - Esters of phosphoric acids
  • C07F 9/24 - Esteramides
  • A61P 31/12 - Antivirals
  • A61P 31/20 - Antivirals for DNA viruses
  • A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • A61K 31/52 - Purines, e.g. adenine
  • A61K 31/6615 - Compounds having two or more esterified phosphorus acid groups, e.g. inositol triphosphate, phytic acid
  • A61K 31/664 - Amides of phosphorus acids
  • A61K 31/685 - Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols one of the hydroxy compounds having nitrogen atoms, e.g. phosphatidylserine, lecithin

22.

CYCLOPENTYL NUCLEOSIDE ANALOGS AS ANTI-VIRALS

      
Document Number 03122410
Status Pending
Filing Date 2019-12-04
Open to Public Date 2020-06-18
Owner JANSSEN BIOPHARMA, INC. (USA)
Inventor
  • Zhong, Minghong
  • Wang, Guangyi

Abstract

Described herein are cyclopentyl nucleoside analogs of Formula (I), pharmaceutical compositions that include one or more cyclopentyl nucleoside analogs and methods of using the same to treat HBV, HDV and/or HIV. (I)

IPC Classes  ?

  • C07D 239/47 - One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
  • A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
  • A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
  • A61K 31/52 - Purines, e.g. adenine
  • A61K 31/6615 - Compounds having two or more esterified phosphorus acid groups, e.g. inositol triphosphate, phytic acid
  • A61K 31/664 - Amides of phosphorus acids
  • A61K 31/685 - Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols one of the hydroxy compounds having nitrogen atoms, e.g. phosphatidylserine, lecithin
  • A61P 31/12 - Antivirals
  • A61P 31/20 - Antivirals for DNA viruses
  • C07D 239/54 - Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
  • C07D 473/18 - Heterocyclic compounds containing purine ring systems with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6 one oxygen and one nitrogen atom, e.g. guanine
  • C07D 473/34 - Nitrogen atom attached in position 6, e.g. adenine
  • C07D 487/04 - Ortho-condensed systems
  • C07F 9/09 - Esters of phosphoric acids
  • C07F 9/24 - Esteramides

23.

MACROCYCLIC FLU ENDONUCLEASE INHIBITORS

      
Application Number IB2019058591
Publication Number 2020/075080
Status In Force
Filing Date 2019-10-09
Publication Date 2020-04-16
Owner JANSSEN BIOPHARMA, INC. (USA)
Inventor
  • Hendricks, Robert Than
  • Stoycheva, Antitsa Dimitrova
  • Bonfanti, Jean-François
  • Raboisson, Pierre Jean-Marie Bernard
  • Fortin, Jérôme, Michel, Claude
  • Mercey, Guillaume, Jean, Maurice

Abstract

OrthomyxoviridaeOrthomyxoviridaeOrthomyxoviridae family.

IPC Classes  ?

  • C07D 498/14 - Ortho-condensed systems
  • A61P 31/16 - Antivirals for RNA viruses for influenza or rhinoviruses
  • A61K 31/5395 - 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 oxygen as the ring hetero atoms, e.g. 1,2-oxazines having two or more nitrogen atoms in the same ring, e.g. oxadiazines
  • A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine

24.

MACROCYCLIC FLU ENDONUCLEASE INHIBITORS

      
Document Number 03115792
Status Pending
Filing Date 2019-10-09
Open to Public Date 2020-04-16
Owner JANSSEN BIOPHARMA, INC. (USA)
Inventor
  • Hendricks, Robert Than
  • Stoycheva, Antitsa Dimitrova
  • Bonfanti, Jean-Francois
  • Raboisson, Pierre Jean-Marie Bernard
  • Fortin, Jerome Michel Claude
  • Mercey, Guillaume Jean Maurice

Abstract

The present invention relates to macrocyclic pyridotriazine derivatives of formula (I) and the pharmaceutically acceptable salts, solvates or or polymorph thereof, and the use of such compounds as a medicament, in particular in the prevention and/or treatment of viral infections caused by viruses belonging to the Orthomyxoviridae famiIy. The present invention furthermore relates to pharmaceutical compositions or combination preparations of the compounds, and to the compositions or preparations for use as a medicament, more preferably for the prevention or treatment of viral infections caused by viruses belonging to the Orthomyxoviridae family.

IPC Classes  ?

  • C07D 498/14 - Ortho-condensed systems
  • A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
  • A61K 31/5395 - 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 oxygen as the ring hetero atoms, e.g. 1,2-oxazines having two or more nitrogen atoms in the same ring, e.g. oxadiazines
  • A61P 31/16 - Antivirals for RNA viruses for influenza or rhinoviruses

25.

Substituted nucleosides, nucleotides and analogs thereof

      
Application Number 16692858
Grant Number 10793591
Status In Force
Filing Date 2019-11-22
First Publication Date 2020-03-12
Grant Date 2020-10-06
Owner Janssen BioPharma, Inc. (USA)
Inventor
  • Beigelman, Leonid
  • Wang, Guangyi
  • Smith, David Bernard

Abstract

Disclosed herein are nucleotide analogs, methods of synthesizing nucleotide analogs and methods of treating diseases and/or conditions such as a HCV infection with one or more nucleotide analogs.

IPC Classes  ?

  • C07H 19/073 - Pyrimidine radicals with 2-deoxyribosyl as the saccharide radical
  • C07H 19/173 - Purine radicals with 2-deoxyribosyl as the saccharide radical
  • C07H 19/20 - Purine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids
  • C07H 19/207 - Purine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids the phosphoric or polyphosphoric acids being esterified by a further hydroxylic compound, e.g. flavine-adenine dinucleotide or nicotinamide-adenine dinucleotide
  • C07H 19/10 - Pyrimidine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids
  • C07H 19/06 - Pyrimidine radicals
  • C07H 19/213 - Purine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids containing cyclic phosphate
  • A61P 31/14 - Antivirals for RNA viruses
  • C07H 19/16 - Purine radicals

26.

Aza-pyridone compounds and uses thereof

      
Application Number 16537396
Grant Number 10980805
Status In Force
Filing Date 2019-08-09
First Publication Date 2020-01-30
Grant Date 2021-04-20
Owner Janssen BioPharma, Inc. (USA)
Inventor
  • Hendricks, Robert Than
  • Beigelman, Leonid
  • Smith, David Bernard
  • Stoycheva, Antitsa Dimitrova

Abstract

Disclosed herein are aza-pyridone compounds, pharmaceutical compositions that include one or more aza-pyridone compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a disease and/or a condition, including an orthomyxovirus infection, with an aza-pyridone compounds. Examples of an orthomyxovirus viral infection include an influenza infection.

IPC Classes  ?

  • A61K 31/5025 - PyridazinesHydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
  • C07D 487/04 - Ortho-condensed systems
  • A61K 31/13 - Amines, e.g. amantadine
  • A61K 31/196 - Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
  • A61K 31/215 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
  • A61K 31/351 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
  • A61K 31/4965 - Non-condensed pyrazines
  • A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
  • A61K 31/7056 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
  • A61K 38/21 - Interferons
  • C07B 59/00 - Introduction of isotopes of elements into organic compounds

27.

Substituted nucleosides, nucleotides and analogs thereof

      
Application Number 16528414
Grant Number 11021509
Status In Force
Filing Date 2019-07-31
First Publication Date 2020-01-23
Grant Date 2021-06-01
Owner Janssen BioPharma, Inc. (USA)
Inventor
  • Beigelman, Leonid
  • Wang, Guangyi
  • Smith, David Bernard
  • Deval, Jerome
  • Prhavc, Marija

Abstract

Disclosed herein are nucleosides, nucleotides and analogs thereof, pharmaceutical compositions that include one or more of nucleosides, nucleotides and analogs thereof, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a disease and/or a condition, including an infection from a paramyxovirus and/or an orthomyxovirus, with a nucleoside, a nucleotide and an analog thereof.

IPC Classes  ?

  • C07H 19/06 - Pyrimidine radicals
  • C07H 19/207 - Purine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids the phosphoric or polyphosphoric acids being esterified by a further hydroxylic compound, e.g. flavine-adenine dinucleotide or nicotinamide-adenine dinucleotide
  • C07H 19/16 - Purine radicals
  • A61P 31/16 - Antivirals for RNA viruses for influenza or rhinoviruses
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • C07D 405/04 - 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 directly linked by a ring-member-to-ring- member bond
  • C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
  • C07D 473/18 - Heterocyclic compounds containing purine ring systems with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6 one oxygen and one nitrogen atom, e.g. guanine
  • C07D 473/34 - Nitrogen atom attached in position 6, e.g. adenine
  • C07D 487/04 - Ortho-condensed systems
  • C07D 493/04 - Ortho-condensed systems
  • C07H 19/00 - Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radicalNucleosidesMononucleotidesAnhydro derivatives thereof
  • C07H 19/14 - Pyrrolo-pyrimidine radicals
  • C12N 9/12 - Transferases (2.) transferring phosphorus containing groups, e.g. kinases (2.7)
  • C07H 19/10 - Pyrimidine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids
  • C07H 19/12 - Triazine radicals
  • C07H 19/20 - Purine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids

28.

AZA-pyridone compounds and uses thereof

      
Application Number 16290690
Grant Number 10702523
Status In Force
Filing Date 2019-03-01
First Publication Date 2019-10-17
Grant Date 2020-07-07
Owner Janssen BioPharma, Inc. (USA)
Inventor
  • Hendricks, Robert Than
  • Beigelman, Leonid
  • Smith, David Bernard
  • Stoycheva, Antitsa Dimitrova

Abstract

Disclosed herein are aza-pyridone compounds, pharmaceutical compositions that include one or more aza-pyridone compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a disease and/or a condition, including an orthomyxovirus infection, with an aza-pyridone compounds. Examples of an orthomyxovirus viral infection include an influenza infection.

IPC Classes  ?

  • A61K 31/5025 - PyridazinesHydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
  • A61K 31/196 - Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
  • A61K 38/21 - Interferons
  • A61K 31/4965 - Non-condensed pyrazines
  • A61K 31/13 - Amines, e.g. amantadine
  • A61K 31/215 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
  • A61K 31/351 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
  • A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
  • A61K 31/7056 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
  • C07B 59/00 - Introduction of isotopes of elements into organic compounds
  • C07D 487/04 - Ortho-condensed systems

29.

MODIFIED OLIGONUCLEOTIDES AND METHODS OF USE

      
Document Number 03094508
Status Pending
Filing Date 2019-03-21
Open to Public Date 2019-09-26
Owner JANSSEN BIOPHARMA, INC. (USA)
Inventor
  • Jekle, Christian Andreas
  • Ozes, Ali

Abstract

Methods and compositions for reducing drug resistance are described. Agents for decreasing m6A RNA methylation are described. Also described are compositions comprising the agents, methods of making the agents, and methods of using the agents to reduce drug resistance in a subject in need thereof, or to stimulate an immune response.

IPC Classes  ?

  • C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
  • A61K 31/215 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
  • A61K 31/351 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
  • A61K 31/712 - Nucleic acids or oligonucleotides having modified sugars, i.e. other than ribose or 2'-deoxyribose
  • A61P 31/16 - Antivirals for RNA viruses for influenza or rhinoviruses

30.

OLIGONUCLEOTIDE CONSTRUCTS AND USES THEREOF

      
Document Number 03079157
Status Pending
Filing Date 2018-11-02
Open to Public Date 2019-05-09
Owner JANSSEN BIOPHARMA, INC. (USA)
Inventor
  • Gryaznov, Sergei
  • Beigelman, Leonid
  • Yun, Theodore

Abstract

Oligodeoxynucleotide-based immunostimulatory Toll-Like Receptor 9 (TLR9) agonists are described. Also described are compositions comprising the TLR9 agonists, methods of making the TLR9 agonists, and methods of using the TLR9 agonists to treat immune diseases, disorders or conditions, such as viral infections or cancer.

IPC Classes  ?

  • C12N 15/117 - Nucleic acids having immunomodulatory properties, e.g. containing CpG-motifs
  • A61K 39/00 - Medicinal preparations containing antigens or antibodies
  • A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
  • A61K 47/22 - Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
  • A61K 47/26 - Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharidesDerivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
  • C07H 21/00 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
  • C12N 15/11 - DNA or RNA fragmentsModified forms thereof

31.

GALNAC DERIVATIVES

      
Document Number 03075598
Status Pending
Filing Date 2018-09-14
Open to Public Date 2019-03-21
Owner JANSSEN BIOPHARMA, INC. (USA)
Inventor
  • Gryaznov, Sergei
  • Hong, Jin
  • Pandey, Rajendra K.
  • Rajwanshi, Vivek Kumar
  • Beigelman, Leonid

Abstract

Modified oligonucleotides comprising a GalNAc moiety of the present disclosure along with methods of making and use, e.g., against HBV are disclosed.

IPC Classes  ?

  • C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
  • A61K 47/26 - Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharidesDerivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
  • A61P 31/14 - Antivirals for RNA viruses
  • C07H 21/02 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with ribosyl as saccharide radical

32.

SUBSTITUTED NUCLEOSIDES, NUCLEOTIDES AND ANALOGS THEREOF

      
Document Number 03075950
Status Pending
Filing Date 2018-09-18
Open to Public Date 2019-03-21
Owner JANSSEN BIOPHARMA, INC. (USA)
Inventor
  • Beigelman, Leonid
  • Deval, Jerome
  • Prhavc, Marija

Abstract

Disclosed herein are compounds of the Formula (I) and pharmaceutically acceptable salts thereof: (I) where the variables in Formula (I) are described herein. Methods of synthesizing such compounds and methods of using them to treat diseases and/or conditions such as a Picornaviridae, Flaviviridae, Filoviridae, Pneumoviridae and/or Coronaviridae viral infections are also disclosed.

IPC Classes  ?

  • C07H 11/00 - Compounds containing saccharide radicals esterified by inorganic acidsMetal salts thereof
  • A61K 31/706 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
  • A61P 31/12 - Antivirals

33.

MODIFIED NUCLEOSIDE PHOSPHORAMIDITES

      
Document Number 03075718
Status Pending
Filing Date 2018-09-14
Open to Public Date 2019-03-21
Owner JANSSEN BIOPHARMA, INC. (USA)
Inventor
  • Gryaznov, Sergei
  • Hong, Jin
  • Rajwanshi, Vivek Kumar
  • Beigelman, Leonid

Abstract

The present disclosure relates to compounds and compositions containing 5'-phosphoramidite nucleoside monomers of formulae (I) and (II), and methods of making and use, wherein the substituents are as defined in the appended claims.

IPC Classes  ?

  • C07H 1/00 - Processes for the preparation of sugar derivatives
  • C07H 19/06 - Pyrimidine radicals
  • C07H 19/067 - Pyrimidine radicals with ribosyl as the saccharide radical
  • C07H 19/16 - Purine radicals
  • C07H 19/167 - Purine radicals with ribosyl as the saccharide radical
  • C07H 19/24 - Heterocyclic radicals containing oxygen or sulfur as ring hetero atom
  • C07H 21/00 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids

34.

Substituted nucleosides, nucleotides and analogs thereof

      
Application Number 16203409
Grant Number 10683320
Status In Force
Filing Date 2018-11-28
First Publication Date 2019-03-21
Grant Date 2020-06-16
Owner Janssen BioPharma, Inc. (USA)
Inventor
  • Beigelman, Leonid
  • Wang, Guangyi
  • Smith, David Bernard

Abstract

Disclosed herein are nucleotide analogs, methods of synthesizing nucleotide analogs and methods of treating diseases and/or conditions such as a HCV infection with one or more nucleotide analogs.

IPC Classes  ?

  • C07H 19/207 - Purine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids the phosphoric or polyphosphoric acids being esterified by a further hydroxylic compound, e.g. flavine-adenine dinucleotide or nicotinamide-adenine dinucleotide
  • C07H 19/10 - Pyrimidine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids
  • C07H 19/06 - Pyrimidine radicals
  • C07H 19/20 - Purine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids
  • C07H 19/173 - Purine radicals with 2-deoxyribosyl as the saccharide radical
  • C07H 19/213 - Purine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids containing cyclic phosphate
  • A61P 31/14 - Antivirals for RNA viruses
  • C07H 19/16 - Purine radicals

35.

Substituted nucleosides, nucleotides and analogs thereof

      
Application Number 16161705
Grant Number 10487104
Status In Force
Filing Date 2018-10-16
First Publication Date 2019-01-31
Grant Date 2019-11-26
Owner Janssen BioPharma, Inc. (USA)
Inventor
  • Beigelman, Leonid
  • Wang, Guangyi
  • Smith, David Bernard

Abstract

Disclosed herein are nucleotide analogs, methods of synthesizing nucleotide analogs and methods of treating diseases and/or conditions such as a HCV infection with one or more nucleotide analogs.

IPC Classes  ?

  • C07H 19/173 - Purine radicals with 2-deoxyribosyl as the saccharide radical
  • C07H 19/20 - Purine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids
  • C07H 19/207 - Purine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids the phosphoric or polyphosphoric acids being esterified by a further hydroxylic compound, e.g. flavine-adenine dinucleotide or nicotinamide-adenine dinucleotide
  • C07H 19/213 - Purine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids containing cyclic phosphate
  • C07H 19/10 - Pyrimidine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids
  • C07H 19/06 - Pyrimidine radicals
  • C07H 19/16 - Purine radicals
  • A61P 31/14 - Antivirals for RNA viruses

36.

MODIFIED OLIGONUCLEOTIDES AND METHODS OF USE

      
Document Number 03037042
Status Pending
Filing Date 2017-09-14
Open to Public Date 2018-03-22
Owner JANSSEN BIOPHARMA, INC. (USA)
Inventor
  • Gryaznov, Sergei
  • Beigelman, Leonid
  • Hong, Jin
  • Rajwanshi, Vivek
  • Martinez Montero, Saul

Abstract

Modified oligonucleotides comprising modifications at the 2' and/or 3' positions(s) along with methods of making and use, e.g., against HBV are disclosed.

IPC Classes  ?

  • C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
  • A61K 31/712 - Nucleic acids or oligonucleotides having modified sugars, i.e. other than ribose or 2'-deoxyribose
  • A61K 31/7125 - Nucleic acids or oligonucleotides having modified internucleoside linkage, i.e. other than 3'-5' phosphodiesters
  • C07H 21/02 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with ribosyl as saccharide radical

37.

Substituted nucleosides, nucleotides and analogs thereof

      
Application Number 15790764
Grant Number 10370401
Status In Force
Filing Date 2017-10-23
First Publication Date 2018-02-15
Grant Date 2019-08-06
Owner Janssen BioPharma, Inc. (USA)
Inventor
  • Beigelman, Leonid
  • Wang, Guangyi
  • Smith, David Bernard
  • Prhavc, Marija
  • Jekle, Christian Andreas
  • Deval, Jerome

Abstract

Disclosed herein are nucleosides, nucleotides and nucleotide analogs, methods of synthesizing the same and methods of treating diseases and/or conditions such as a Picornavirus and/or Flaviviridae infection with one or more nucleosides, nucleotides and nucleotide analogs.

IPC Classes  ?

  • A61K 31/7076 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
  • A61K 31/708 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid having oxo groups directly attached to the purine ring system, e.g. guanosine, guanylic acid
  • C07H 19/20 - Purine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids
  • C07H 19/06 - Pyrimidine radicals
  • C07H 19/16 - Purine radicals
  • C07H 19/10 - Pyrimidine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids
  • A61K 31/7064 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
  • A61K 31/7052 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
  • A61K 31/7072 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
  • C07H 19/11 - Pyrimidine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids containing cyclic phosphate
  • C07H 19/207 - Purine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids the phosphoric or polyphosphoric acids being esterified by a further hydroxylic compound, e.g. flavine-adenine dinucleotide or nicotinamide-adenine dinucleotide
  • C07H 19/213 - Purine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids containing cyclic phosphate

38.

SUBSTITUTED NUCLEOSIDES, NUCLEOTIDES AND ANALOGS THEREOF

      
Application Number US2017046366
Publication Number 2018/031818
Status In Force
Filing Date 2017-08-10
Publication Date 2018-02-15
Owner JANSSEN BIOPHARMA, INC. (USA)
Inventor
  • Wang, Guangyi
  • Beigelman, Leonid
  • Deval, Jerome
  • Jekle, Christian Andreas

Abstract

Disclosed herein are nucleotide analogs, methods of synthesizing nucleotide analogs and methods of treating diseases and/or conditions such as a Picornaviridae and/or Flaviviridae viral infections with one or more nucleotide analogs.

IPC Classes  ?

  • C07H 19/16 - Purine radicals
  • C07H 19/14 - Pyrrolo-pyrimidine radicals
  • C07H 19/167 - Purine radicals with ribosyl as the saccharide radical
  • C07H 19/20 - Purine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids
  • C07H 19/23 - Heterocyclic radicals containing two or more heterocyclic rings condensed among themselves or condensed with a common carbocyclic ring system, not provided for in groups
  • A61K 31/7076 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
  • A61K 31/7064 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
  • A61K 31/706 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
  • A61K 31/708 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid having oxo groups directly attached to the purine ring system, e.g. guanosine, guanylic acid
  • A61P 31/12 - Antivirals
  • A61P 31/14 - Antivirals for RNA viruses
  • A61P 31/16 - Antivirals for RNA viruses for influenza or rhinoviruses

39.

Compounds for the treatment of paramyxovirus viral infections

      
Application Number 15627757
Grant Number 11014935
Status In Force
Filing Date 2017-06-20
First Publication Date 2017-10-05
Grant Date 2021-05-25
Owner Janssen BioPharma, Inc. (USA)
Inventor
  • Wang, Guangyi
  • Beigelman, Leonid
  • Truong, Anh
  • Napolitano, Carmela
  • Andreotti, Daniele
  • He, Haiying

Abstract

Disclosed herein are new antiviral compounds, together with pharmaceutical compositions that include one or more antiviral compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus viral infection with one or more small molecule compounds. Examples of paramyxovirus infection include an infection caused by human respiratory syncytial virus (RSV).

IPC Classes  ?

  • C07D 409/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • C07D 495/04 - Ortho-condensed systems
  • C07D 333/58 - Radicals substituted by nitrogen atoms
  • C07D 215/12 - Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
  • C07D 215/14 - Radicals substituted by oxygen atoms
  • C07D 311/68 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulfur atoms in position 2 or 4 with nitrogen atoms directly attached in position 4
  • C07D 215/42 - Nitrogen atoms attached in position 4
  • C07D 217/24 - Oxygen atoms
  • C07D 333/16 - Radicals substituted by singly bound hetero atoms other than halogen by oxygen atoms
  • C07D 333/20 - Radicals substituted by singly bound hetero atoms other than halogen by nitrogen atoms
  • C07D 233/38 - One oxygen atom with acyl radicals or hetero atoms directly attached to ring nitrogen atoms
  • C07D 333/50 - Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
  • C07D 333/54 - Benzo [b] thiophenesHydrogenated benzo [b] thiophenes with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
  • C07D 233/61 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms not forming part of a nitro radical, attached to ring nitrogen atoms
  • C07D 333/62 - Benzo [b] thiophenesHydrogenated benzo [b] thiophenes with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
  • C07D 333/66 - Nitrogen atoms not forming part of a nitro radical
  • C07D 333/68 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
  • C07D 335/06 - BenzothiopyransHydrogenated benzothiopyrans
  • C07D 233/88 - Nitrogen atoms, e.g. allantoin
  • C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • C07D 401/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
  • C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 405/04 - 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 directly linked by a ring-member-to-ring- member bond
  • C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 413/04 - 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 directly linked by a ring-member-to-ring- member bond
  • C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 417/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 471/04 - Ortho-condensed systems
  • C07D 261/20 - Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings condensed with carbocyclic rings or ring systems
  • C07D 207/335 - Radicals substituted by nitrogen atoms not forming part of a nitro radical
  • C07D 209/08 - IndolesHydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
  • C07D 209/14 - Radicals substituted by nitrogen atoms, not forming part of a nitro radical
  • C07D 277/64 - Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2
  • C07D 209/86 - CarbazolesHydrogenated carbazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the ring system
  • C07D 213/42 - Radicals substituted by singly-bound nitrogen atoms having hetero atoms attached to the substituent nitrogen atom
  • C07D 213/50 - Ketonic radicals
  • C07D 213/65 - One oxygen atom attached in position 3 or 5
  • C07D 213/68 - One oxygen atom attached in position 4
  • C07D 307/52 - Radicals substituted by nitrogen atoms not forming part of a nitro radical
  • C07D 307/81 - Radicals substituted by nitrogen atoms not forming part of a nitro radical
  • C07D 233/60 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms with hydrocarbon radicals, substituted by oxygen or sulfur atoms, attached to ring nitrogen atoms
  • C07D 495/14 - Ortho-condensed systems
  • C07C 251/84 - Hydrazones having doubly-bound carbon atoms of hydrazone groups being part of rings other than six-membered aromatic rings
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
  • A61K 31/404 - Indoles, e.g. pindolol
  • A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
  • A61K 31/4155 - 1,2-Diazoles not condensed and containing further heterocyclic rings
  • A61K 31/4418 - Non-condensed pyridinesHydrogenated derivatives thereof having a carbocyclic ring directly attached to the heterocyclic ring, e.g. cyproheptadine
  • A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
  • A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
  • A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
  • C07C 243/34 - Hydrazines having nitrogen atoms of hydrazine groups acylated by carboxylic acids with acylating carboxyl groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of a carbon skeleton further substituted by nitrogen atoms
  • C07C 251/80 - Hydrazones having doubly-bound carbon atoms of hydrazone groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of an unsaturated carbon skeleton the carbon skeleton containing rings
  • C07C 255/34 - Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring with cyano groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by unsaturated carbon chains
  • A61K 31/4164 - 1,3-Diazoles
  • A61K 31/426 - 1,3-Thiazoles
  • A61K 31/4436 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
  • A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
  • A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
  • A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
  • A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
  • C07D 209/20 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals substituted additionally by nitrogen atoms, e.g. tryptophane
  • C07D 233/64 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
  • C07D 277/56 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
  • C07D 409/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
  • A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
  • A61K 31/277 - NitrilesIsonitriles having a ring, e.g. verapamil
  • A61K 31/341 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
  • A61K 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
  • A61K 31/352 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. cannabinols, methantheline
  • A61K 31/382 - Heterocyclic compounds having sulfur as a ring hetero atom having six-membered rings, e.g. thioxanthenes
  • A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
  • A61K 31/4025 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
  • A61K 31/4196 - 1,2,4-Triazoles
  • A61K 31/423 - Oxazoles condensed with carbocyclic rings
  • A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
  • A61K 31/428 - Thiazoles condensed with carbocyclic rings
  • A61K 31/4365 - 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 having sulfur as a ring hetero atom, e.g. ticlopidine
  • 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 31/4427 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems
  • 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
  • A61K 31/47 - QuinolinesIsoquinolines
  • A61K 31/4704 - 2-Quinolinones, e.g. carbostyril
  • A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
  • A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
  • A61K 31/538 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
  • C07C 243/18 - Hydrazines having nitrogen atoms of hydrazine groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing rings
  • C07C 255/66 - Carboxylic acid nitriles containing cyano groups and nitrogen atoms further bound to other hetero atoms, other than oxygen atoms of nitro or nitroso groups, bound to the same carbon skeleton with the nitrogen atoms further bound to nitrogen atoms having cyano groups and nitrogen atoms being part of hydrazine or hydrazone groups bound to the same carbon skeleton
  • C07D 215/38 - Nitrogen atoms
  • C07D 307/40 - Radicals substituted by oxygen atoms
  • C07D 307/91 - DibenzofuransHydrogenated dibenzofurans
  • C07D 333/76 - Dibenzothiophenes
  • C07D 405/10 - 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 carbon chain containing aromatic rings
  • C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

40.

Substituted nucleosides, nucleotides and analogs thereof

      
Application Number 15423270
Grant Number 10307439
Status In Force
Filing Date 2017-02-02
First Publication Date 2017-05-25
Grant Date 2019-06-04
Owner JANSSEN BIOPHARMA, INC. (USA)
Inventor
  • Blatt, Lawrence M.
  • Beigelman, Leonid
  • Symons, Julian Alexander
  • Smith, David Bernard

Abstract

Disclosed herein are nucleosides, nucleotides and nucleotide analogs, methods of synthesizing the same and methods of treating diseases and/or conditions such as a Coronaviridae virus, a Togaviridae virus, a Hepeviridae virus and/or a Bunyaviridae virus infection with one or more nucleosides, nucleotides and nucleotide analogs.

IPC Classes  ?

  • A01N 43/04 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atom with one hetero atom
  • A61K 31/70 - CarbohydratesSugarsDerivatives thereof
  • A61K 31/708 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid having oxo groups directly attached to the purine ring system, e.g. guanosine, guanylic acid
  • A61K 31/7068 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
  • A61K 31/7072 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
  • A61K 31/7076 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
  • C07F 9/6574 - Esters of oxyacids of phosphorus

41.

Substituted nucleosides, nucleotides and analogs thereof

      
Application Number 15256337
Grant Number 10112966
Status In Force
Filing Date 2016-09-02
First Publication Date 2017-02-09
Grant Date 2018-10-30
Owner JANSSEN BIOPHARMA, INC. (USA)
Inventor
  • Beigelman, Leonid
  • Wang, Guangyi
  • Smith, David Bernard

Abstract

Disclosed herein are nucleotide analogs, methods of synthesizing nucleotide analogs and methods of treating diseases and/or conditions such as a HCV infection with one or more nucleotide analogs.

IPC Classes  ?

  • C07H 19/10 - Pyrimidine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids
  • C07H 19/06 - Pyrimidine radicals
  • C07H 19/16 - Purine radicals
  • C07H 19/213 - Purine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids containing cyclic phosphate
  • C07H 19/20 - Purine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids
  • C07H 19/207 - Purine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids the phosphoric or polyphosphoric acids being esterified by a further hydroxylic compound, e.g. flavine-adenine dinucleotide or nicotinamide-adenine dinucleotide
  • C07H 19/173 - Purine radicals with 2-deoxyribosyl as the saccharide radical

42.

Substituted nucleosides, nucleotides and analogs thereof

      
Application Number 15256345
Grant Number 10144755
Status In Force
Filing Date 2016-09-02
First Publication Date 2017-02-09
Grant Date 2018-12-04
Owner JANSSEN BIOPHARMA, INC. (USA)
Inventor
  • Beigelman, Leonid
  • Wang, Guangyi
  • Smith, David Bernard

Abstract

Disclosed herein are nucleotide analogs, methods of synthesizing nucleotide analogs and methods of treating diseases and/or conditions such as a HCV infection with one or more nucleotide analogs.

IPC Classes  ?

  • C07H 19/10 - Pyrimidine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids
  • C07H 19/06 - Pyrimidine radicals
  • C07H 19/20 - Purine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids
  • C07H 19/173 - Purine radicals with 2-deoxyribosyl as the saccharide radical
  • C07H 19/16 - Purine radicals
  • C07H 19/207 - Purine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids the phosphoric or polyphosphoric acids being esterified by a further hydroxylic compound, e.g. flavine-adenine dinucleotide or nicotinamide-adenine dinucleotide
  • C07H 19/213 - Purine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids containing cyclic phosphate

43.

AZA-PYRIDONE COMPOUNDS AND USES THEREOF

      
Document Number 02979216
Status Pending
Filing Date 2016-03-09
Open to Public Date 2016-09-15
Owner JANSSEN BIOPHARMA, INC. (USA)
Inventor
  • Hendricks, Robert Than
  • Beigelman, Leonid
  • Smith, David Bernard
  • Stoycheva, Antitsa Dimitrova

Abstract

Disclosed herein are aza-pyridone compounds, pharmaceutical compositions that include one or more aza-pyridone compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a disease and/or a condition, including an orthomyxovirus infection, with an aza-pyridone compound. Examples of an orthomyxovirus viral infection include an influenza infection.

IPC Classes  ?

  • C07D 487/04 - Ortho-condensed systems
  • A61K 31/5025 - PyridazinesHydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
  • A61P 31/16 - Antivirals for RNA viruses for influenza or rhinoviruses
  • C07D 471/04 - Ortho-condensed systems

44.

ANTIVIRAL COMPOUNDS

      
Document Number 02977150
Status Pending
Filing Date 2016-02-24
Open to Public Date 2016-09-01
Owner JANSSEN BIOPHARMA, INC. (USA)
Inventor
  • Wang, Guangyi
  • Beigelman, Leonid
  • Truong, Anh
  • Stein, Karin Ann

Abstract

Disclosed herein are new antiviral compounds, together with pharmaceutical compositions that include one or more antiviral compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus viral infection with one or more small molecule compounds. Examples of paramyxovirus infection include an infection caused by human respiratory syncytial virus (RSV).

IPC Classes  ?

  • C07D 491/048 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
  • 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 31/4355 - 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 oxygen as a ring hetero atom
  • A61K 31/436 - 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 oxygen as a ring hetero atom, e.g. rapamycin
  • 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 31/4375 - 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 31/44 - Non-condensed pyridinesHydrogenated derivatives thereof
  • A61K 31/4427 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems
  • A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
  • A61K 31/47 - QuinolinesIsoquinolines
  • A61K 31/4704 - 2-Quinolinones, e.g. carbostyril
  • A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
  • A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
  • A61K 31/536 - 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 oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with carbocyclic ring systems
  • A61K 31/538 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
  • A61P 31/14 - Antivirals for RNA viruses
  • C07D 213/36 - Radicals substituted by singly-bound nitrogen atoms
  • C07D 213/68 - One oxygen atom attached in position 4
  • C07D 221/04 - Ortho- or peri-condensed ring systems
  • C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • C07D 413/04 - 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 directly linked by a ring-member-to-ring- member bond
  • C07D 471/04 - Ortho-condensed systems
  • C07D 491/052 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
  • C07D 491/20 - Spiro-condensed systems
  • C07D 498/04 - Ortho-condensed systems

45.

ANTIVIRAL COMPOUNDS

      
Document Number 02921294
Status In Force
Filing Date 2014-08-19
Open to Public Date 2015-02-26
Grant Date 2023-05-16
Owner JANSSEN BIOPHARMA, INC. (USA)
Inventor
  • Wang, Guangyi
  • Beigelman, Leonid
  • Truong, Anh
  • Napolitano, Carmela
  • Andreotti, Daniele
  • He, Haiying
  • Stein, Karin Ann

Abstract

Disclosed herein are new antiviral compounds, together with pharmaceutical compositions that include one or more antiviral compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus viral infection with one or more small molecule compounds. Examples of paramyxovirus infection include an infection caused by human respiratory syncytial virus (RSV).

IPC Classes  ?

  • C07D 207/267 - 2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to the ring nitrogen atom
  • A61K 31/14 - Quaternary ammonium compounds, e.g. edrophonium, choline
  • A61K 31/33 - Heterocyclic compounds
  • C07D 213/40 - Acylated substituent nitrogen atom
  • C07D 233/58 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring nitrogen atoms
  • C07D 239/34 - One oxygen atom
  • C07D 277/28 - Radicals substituted by nitrogen atoms
  • C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 409/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
  • C07D 413/04 - 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 directly linked by a ring-member-to-ring- member bond
  • C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 417/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • C07D 417/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 471/04 - Ortho-condensed systems
  • C07D 487/04 - Ortho-condensed systems
  • C07D 491/048 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
  • C07D 491/052 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
  • C07D 491/20 - Spiro-condensed systems
  • C07D 495/14 - Ortho-condensed systems

46.

Substituted nucleosides, nucleotides and analogs thereof

      
Application Number 14386294
Grant Number 09441007
Status In Force
Filing Date 2013-03-19
First Publication Date 2015-02-19
Grant Date 2016-09-13
Owner JANSSEN BIOPHARMA, INC. (USA)
Inventor
  • Wang, Guangyi
  • Smith, David Bernard
  • Beigelman, Leonid
  • Deval, Jerome
  • Prhavc, Marija

Abstract

Disclosed herein are nucleosides, nucleotides and analogs thereof, pharmaceutical compositions that include one or more of nucleosides, nucleotides and analogs thereof, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a disease and/or a condition, including an infection from a paramyxovirus and/or an orthomyxovirus, with a nucleoside, a nucleotide and an analog thereof.

IPC Classes  ?

  • C07H 19/06 - Pyrimidine radicals
  • C07H 19/16 - Purine radicals
  • C07H 19/20 - Purine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids
  • C07H 19/10 - Pyrimidine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids
  • C07H 19/12 - Triazine radicals
  • C07H 19/207 - Purine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids the phosphoric or polyphosphoric acids being esterified by a further hydroxylic compound, e.g. flavine-adenine dinucleotide or nicotinamide-adenine dinucleotide
  • A61K 31/7068 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
  • A61K 31/7072 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
  • A61K 31/7076 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
  • A61K 31/708 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid having oxo groups directly attached to the purine ring system, e.g. guanosine, guanylic acid
  • A61K 31/706 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom

47.

COMPOUNDS FOR THE TREATMENT OF PARAMOXYVIRUS VIRAL INFECTIONS

      
Document Number 02882088
Status In Force
Filing Date 2013-08-21
Open to Public Date 2014-02-27
Grant Date 2021-11-23
Owner JANSSEN BIOPHARMA, INC. (USA)
Inventor
  • Wang, Guangyi
  • Beigelman, Leonid
  • Truong, Anh
  • Napolitano, Carmela
  • Andreotti, Daniele
  • He, Haiying

Abstract

Disclosed herein are new antiviral compounds, together with pharmaceutical compositions that include one or more antiviral compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus viral infection with one or more small molecule compounds. Examples of paramyxovirus infection include an infection caused by human respiratory syncytial virus (RSV).

IPC Classes  ?

  • C07D 333/52 - Benzo [b] thiophenesHydrogenated benzo [b] thiophenes
  • A61K 31/14 - Quaternary ammonium compounds, e.g. edrophonium, choline
  • A61K 31/16 - Amides, e.g. hydroxamic acids
  • A61K 31/33 - Heterocyclic compounds
  • C07C 251/84 - Hydrazones having doubly-bound carbon atoms of hydrazone groups being part of rings other than six-membered aromatic rings
  • C07C 251/86 - Hydrazones having doubly-bound carbon atoms of hydrazone groups bound to carbon atoms of six-membered aromatic rings
  • C07D 207/00 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
  • C07D 209/04 - IndolesHydrogenated indoles
  • C07D 213/00 - Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
  • C07D 215/00 - Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
  • C07D 217/00 - Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
  • C07D 233/60 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms with hydrocarbon radicals, substituted by oxygen or sulfur atoms, attached to ring nitrogen atoms
  • C07D 235/02 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
  • C07D 249/04 - 1,2,3-TriazolesHydrogenated 1,2,3-triazoles
  • C07D 249/18 - Benzotriazoles
  • C07D 261/02 - Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
  • C07D 265/00 - Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
  • C07D 307/02 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
  • C07D 307/78 - Benzo [b] furansHydrogenated benzo [b] furans
  • C07D 311/02 - Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
  • C07D 333/02 - Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
  • C07D 335/04 - Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
  • C07D 401/00 - 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
  • C07D 403/00 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group
  • C07D 407/00 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group
  • C07D 409/00 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
  • C07D 413/00 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
  • C07D 417/00 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group
  • C07D 417/02 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings
  • C07D 495/02 - Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
  • C07D 495/14 - Ortho-condensed systems

48.

SUBSTITUTED NUCLEOSIDES, NUCLEOTIDES AND ANALOGS THEREOF

      
Document Number 02866901
Status In Force
Filing Date 2013-03-19
Open to Public Date 2013-09-26
Grant Date 2020-09-22
Owner JANSSEN BIOPHARMA, INC. (USA)
Inventor
  • Wang, Guangyi
  • Smith, David Bernard
  • Beigelman, Leonid
  • Deval, Jerome
  • Prhavc, Marija

Abstract

Disclosed herein are nucleosides, nucleotides and analogs thereof, pharmaceutical compositions that include one or more of nucleosides, nucleotides and analogs thereof, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a disease and/or a condition, including an infection from a paramyxovirus and/or an orthomyxovirus, with a nucleoside, a nucleotide and an analog thereof.

IPC Classes  ?

  • A61K 31/7068 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
  • A61K 31/7072 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
  • A61K 31/7076 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
  • A61K 31/708 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid having oxo groups directly attached to the purine ring system, e.g. guanosine, guanylic acid

49.

SUBSTITUTED NUCLEOSIDES, NUCLEOTIDES AND ANALOGS THEREOF AND THEIR USE IN AMELIORATING OR TREATING A DISEASE OR CONDITION ASSOCIATED WITH VIRAL INFECTIONS

      
Document Number 02860289
Status In Force
Filing Date 2012-12-20
Open to Public Date 2013-06-27
Grant Date 2021-03-16
Owner JANSSEN BIOPHARMA, INC. (USA)
Inventor
  • Beigelman, Leonid
  • Wang, Guangyi
  • Smith, David Bernard
  • Deval, Jerome
  • Prhavc, Marija

Abstract

Disclosed herein are nucleosides, nucleotides and analogs thereof, pharmaceutical compositions that include one or more of nucleosides, nucleotides and analogs thereof, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a disease and/or a condition, including an infection from a paramyxovirus and/or an orthomyxovirus, with a nucleoside, a nucleotide and an analog thereof.

IPC Classes  ?

  • C07H 19/00 - Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radicalNucleosidesMononucleotidesAnhydro derivatives thereof
  • A61K 31/7068 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
  • A61K 31/7072 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
  • A61K 31/7076 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
  • A61K 31/708 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid having oxo groups directly attached to the purine ring system, e.g. guanosine, guanylic acid
  • A61P 31/12 - Antivirals
  • C07H 19/06 - Pyrimidine radicals
  • C07H 19/14 - Pyrrolo-pyrimidine radicals
  • C07H 19/16 - Purine radicals
  • C12N 9/99 - Enzyme inactivation by chemical treatment