D-AMINO ACID COMPOUNDS FOR LIVER DISEASE

• US 20160002281A1
• Filed: 09/16/2015
• Published: 01/07/2016
• Est. Priority Date: 05/22/2012
• Status: Abandoned Application

• Current Assignee: Idenix Pharmaceuticals (Merck & Co., Inc.)
• Original Assignee: Idenix Pharmaceuticals (Merck & Co., Inc.)
• Inventors: MAYES, Benjamin Alexander, MOUSSA, Adel M., STEWART, Alistair James, GOSSELIN, Gilles, PARSY, Christophe Claude, DOUSSON, Cyril B., PIERRA, Claire, RAHALI, Houcine, ALEXANDRE, Franois-Ren, GRIFFON, Jean-Franois, SURLERAUX, Dominique
• Application Number:
  US14/856,462
• Publication Number:
  US 20160002281A1
• Time in Patent Office: Days
• US Class Current: 1/1
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/403 condensed with carbocyclic rings, e.g. carbazole
• CPC Class Codes: A61K 31/4709 Non-condensed quinolines and containing further heterocyclic rings
• CPC Class Codes: A61K 31/497 containing further heterocyclic rings
• CPC Class Codes: A61K 31/7056 containing five-membered rings with nitrogen as a ring hetero atom
• CPC Class Codes: A61K 31/7072 having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
• CPC Class Codes: A61K 31/7076 containing purines, e.g. adenosine, adenylic acid
• CPC Class Codes: A61K 31/708 having oxo groups directly attached to the purine ring system, e.g. guanosine, guanylic acid
• CPC Class Codes: A61K 38/21 Interferons [IFN]
• CPC Class Codes: A61K 38/55 Protease inhibitors
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61P 1/16 for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
• CPC Class Codes: A61P 31/12 Antivirals
• CPC Class Codes: A61P 31/14 for RNA viruses
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: C07H 19/10 with the saccharide radical esterified by phosphoric or polyphosphoric acids
• CPC Class Codes: C07H 19/16 Purine radicals
• CPC Class Codes: C07H 19/20 with the saccharide radical esterified by phosphoric or polyphosphoric acids

Abstract

Provided herein are compounds, compositions and methods for the treatment of liver disease and conditions, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents.

Claims

1-2. -2. (canceled)

3. A compound according to formula (II) or a pharmaceutically acceptable salt, solvate, tautomeric form or polymorphic form thereof:

29. The compound of claim 3, wherein said compound is according to the structure:

30. The compound of claim 3, wherein said compound is:

31. The compound of claim 3, wherein said compound is:

32. The compound of claim 3, wherein said compound is according to the structure:

33. The compound according to claim 32, wherein said compound is:

34. The compound according to claim 32, wherein said compound is:

35. The compound according to claim 3, wherein said compound is according to the structure:

36. The compound according to claim 35, wherein said compound is according to the structure:

37. The compound according to claim 35, wherein said compound is

38. The compound according to claim 37, wherein said compound is

4-28. -28. (canceled)

39. A compound having the structure:

40. A compound having the structure:

41. A nucleoside composition comprising a compound according to Formula IIa or IIb:

42. The composition according to claim 41, wherein said compound is:

43. The composition according to claim 41, wherein said compound is:

44. The composition according to claim 43, wherein said compound is:

45. A pharmaceutical composition comprising a compound according to formula (II) or a pharmaceutically acceptable salt, solvate, tautomeric form or polymorphic form thereof:

46. The pharmaceutical composition of claim 45, wherein said composition provides a therapeutically effective amount of said compound for treating a human infected with HCV.

47. The pharmaceutical composition of claim 46, wherein said compound is according to the structure:

48. The pharmaceutical composition of claim 47, wherein said compound is according to the structure:

49. The pharmaceutical composition of claim 46, wherein said compound is:

50. The pharmaceutical composition of claim 49, wherein said compound is:

51. The pharmaceutical composition of claim 46, wherein said compound is:

52. The pharmaceutical composition of claim 51, wherein said compound is:

53. The pharmaceutical composition of claim 51, wherein said compound is a designated enantiomer, and said composition is substantially free of other stereoisomers of said compound.

54. The pharmaceutical composition of claim 52, wherein said compound is a designated enantiomer, and said composition is substantially free of other stereoisomers of said compound.

55. A method for the treatment of a human infected with a hepatitis C virus, comprising the administration to said human an effective amount of a compound according to formula (II) or a pharmaceutically acceptable salt, solvate, tautomeric form or polymorphic form thereof:

56. The method of claim 55, wherein said compound is according to the structure:

57. The method of claim 56, wherein said compound is according to the structure:

58. The method of claim 55, wherein said compound is:

59. The method of claim 58, wherein said compound is:

60. The method of claim 55, wherein said compound is:

61. The method of claim 60, wherein said compound is:

62. A method for the treatment of a human infected with a hepatitis C virus, comprising the administration to said human an effective amount of a pharmaceutical composition comprising a compound according to Formula IIa or IIb, or a pharmaceutically acceptable salt, solvate, tautomeric form or polymorphic form thereof:

63. The method of claim 62, wherein said compound is:

64. The method of claim 63, wherein said compound is:

65. The method of claim 62, wherein said compound is:

66. The method of claim 65, wherein said compound is: