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Details for Patent: 6,946,450

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Details for Patent: 6,946,450

Title: .beta.-L-2'-deoxy-nucleosides for the treatment of hepatitis B
Abstract:This invention is directed to a method for treating a host infected with hepatitis B comprising administering an effective amount of an anti-HBV biologically active 2'-deoxy-.beta.-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof, wherein the 2'-deoxy-.beta.-L-erythro-pentofuranonucleoside has the formula: ##STR1## wherein R is selected from the group consisting of H, straight chained, branched or cyclic alkyl, CO-alkyl, CO-aryl, CO-alkoxyalkyl, CO-aryloxyalkyl, CO-substituted aryl, alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, amino acid residue, mono, di, or triphosphate, or a phosphate derivative; and BASE is a purine or pyrimidine base which may be optionally substituted. The 2'-deoxy-.beta.-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof may be administered either alone or in combination with another 2'-deoxy-.beta.-L-erythro-pentofuranonucleoside or in combination with another anti-hepatitis B agent.
Inventor(s): Gosselin; Gilles (Montpellier, FR), Imbach; Jean-Louis (Montpellier, FR), Bryant; Martin L. (Carlisle, MA)
Assignee: Idenix Pharmaceuticals, Inc. (Cambridge, MA) Centre National de la Recherche Scientifique (Paris, FR) L'Universite Montpellier II (Montpellier, FR)
Filing Date:May 13, 2003
Application Number:10/437,802
Claims:1. A method for treating a human infected with hepatitis B virus comprising administering an effective amount of the .beta.-L-nucleoside: ##STR19## or a pharmaceutically acceptable salt thereof, wherein R is selected from the group consisting of H, mono, di or tri phosphate, an amino acid acyl residue, acyl, alkyl, and a stabilized phosphate prodrug.

2. The method according to claim 1, wherein the compound is ##STR20## or a phannaceutically acceptable salt thereof.

3. The method of claim 1, wherein the R is a monophosphate.

4. The method of claim 1, wherein the R is a diphosphate.

5. The method of claim 1, wherein the R is a triphosphate.

6. The method of claim 1, wherein the R is an amino acid acyl residue.

7. The method of claim 1, wherein the R is acyl.

8. The method of claim 1, wherein the R is alkyl.

9. The method of claim 1, wherein the R is a stabilized phosphate prodrug.

10. The method according to claim 1, wherein the compound is administered in a pharmaceutically acceptable carrier.

11. The method according to claim 1, wherein the pharmaceutically acceptable carrier is suitable for oral delivery.

12. The method according to claim 1, wherein the pharmaceutically acceptable carrier is suitable for intravenous delivery.

13. The method according to claim 1, wherein the pharmaceutically acceptable carrier is suitable for parenteral delivery.

14. The method according to claim 1, wherein the pharmaceutically acceptable carrier is suitable for intradermal delivery.

15. The method according to claim 1, wherein the pharmaceutically acceptable carrier is suitabie for subcutaneous delivery.

16. The method according to claim 1, wherein the pharmaceutically acceptable carrier is suitable for topical delivery.

17. The method according to claim 1, wherein the compound is in the form of a dosage unit.

18. The method according to claim 17, wherein the dosage unit contains 10 to 1500 mg of the compound.

19. The method according to claim 17 or 18, wherein the dosage unit is a tablet or capsule.

20. A method for treating a human infected with hepatitis B virus comprising administering an effective amount of the .beta.-L-nucleoside: ##STR21## or a pharmaceutically acceptable salt or thereof, in alternation or combination with one or more other anti-hepatitis agents, wherein R is selected from the group consisting of H, mono, di or tri phosphate, an amino acid acyl residue, acyl, ailcyl, and a stabilized phosphate prodrug.

21. The method according to claim 20, wherein the anti-hepatitis agent is selected from the group consisting of .beta.-L-2-hydroxymethyl-5-(cytosin-1-yl)-1,3-oxathiolane (3TC), cis-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxatbiolane (FTC), .beta.L-2"-fluoro-5-methyl-arabinofuranosyluridine (L-FMAU), .beta.-D-2,6-diaminopurine dioxolane (DAPD), famciclovir, penciclovir, 2-amino-1,9-dihydro-9-[4-hydroxy-3-(hydroxymethyl)-2-methylenecyclo-pentyl ]-6H-purin-6-one (entecavir, BMS-200475), 9-[2-(phosphono-methoxy)ethyl]-adenine (PMEA, adefovir, dipivoxil); 9-((1R,2R,3S)-2,3-bis(hydroxyinethyl)cyclo-butyl)guanine (lobucavir), ganciclovir, and ribavirin.

22. The method according to claim 20, wherein the anti-hepatitis agent is .beta.-L-2-hydroxymethyl-5-(cytosin-1-yl)-1,3-oxathiolane (3TC).

23. The method according to claim 20, wherein the anti-hepatitis agent is cis-2-hydroxymcthyl-5-(5-fluorocytosin-1-yl)-1,3-oxatbiolane (FTC).

24. The method according to claim 20, wherein the anti-hepatitis agent is L-2'-fluoro-5-methyl-arabinofuranosyluridine (L-FMAU).

25. The method according to claim 20, wherein the anti-hepatitis agent is .beta.-D-2,6-diaminopurine dioxolane (DAPD).

26. The method according to claim 20, wherein the anti-hepatitis agent is famicilovir.

27. The method according to claim 20, wherein the anti-hepatitis agent is penciclovir.

28. The method according to claim 20, wherein the anti-hepatitis agent is 2-amino-1,9-dihydro-9-[4-hydroxy-3-(hydroxymethyl)-2-methylenecyclo-pentyl ]-6H-purin-6-one (entecavir, BMS-200475).

29. The method according to claim 20, wherein the anti-hepatitis agent is 9-[2-(phosphono-methoxy)ethyl]-adenine (PMEA, adefovir, dipivoxil).

30. The method according to claim 20, wherein the anti-hepatitis agent is 9-((1R,2R,3S)-2,3-bis(hydroxymethyl)cyclo-butyl)guanine (lobucavir).

31. The method according to claim 20, wherein the anti-hepatitis agent is ganciclovir.

32. The method according to claim 20, wherein the anti-hepatitis agent is ribavirin.

33. The method according to claim 20, wherein the compound is administered in a pharmaceutically acceptable carrier.

34. The method according to claim 20, wherein the pharmaceutically acceptable carrier is suitable for oral delivery.

35. The method according to claim 20, wherein the pharmaceutically acceptable carrier is suitable for intravenous delivery.

36. The method according to claim 20, wherein the pharmaceutically acceptable carrier is suitable for parentcral delivery.

37. The method according to claim 20, wherein the pharmaceutically acceptable carrier is suitable for intradermal delivery.

38. The method according to claim 20, wherein the pharmaceutically acceptable carrier is suitable for subcutaneous delivery.

39. The method according to claim 20, wherein the pharmaceutically acceptable carrier is suitable for topical delivery.

40. The method according to claim 20, wherein the compound is in the form of a dosage unit.

41. The method according to claim 40, wherein the dosage unit contains 10 to 1500 mg of the compound.

42. The method according to claim 40 and 41, wherein the dosage unit is a tablet or capsule.

43. A pharmaceutical composition for treating a human infected with hepatitis B virus comprising an effective amount of the B-L-nucleoside: ##STR22## or a pharmaceutically acceptable salt or thereof, wherein R is selected from the group consisting of H, mono, di or tri phosphate, an amino acid acyl residue, acyl, alkyl, and a stabilized phosphate prodrug; with one or more other anti-hepatitis agents; optionally in a pharmaceutically acceptable carrier.

44. The pharmaceutical composition of claim 43, wherein the .beta.-L-nucleoside is ##STR23## or a pharmaceutically acceptable salt thereof.

45. The pharmaceutical composition according claim 43, wherein the compound is the form of a dosage unit.

46. The pharmaceutical composition according to claim 45, wherein the dosage unit contains 10 to 1500 mg of the compound.

47. The pharmaceutical composition according claim 43, wherein the composition is administered in a pharmaceutically acceptable carrier.

48. The pharmaceutical composition according claim 43, wherein the pharmaceutically acceptable carrier is suitable for oral delivery.

49. The pharmaceutical composition according claim 43, wherein the pharmaceutically acceptable carrier is suitable for intravenous delivery.

50. The pharmaceutical composition according claim 43, wherein the pharmaceutically acceptable carrier is suitable for parenteral delivery.

51. The pharmaceutical composition according claim 43, wherein the pharmaceutically acceptable carrier is suitable for intradermal delivery.

52. The pharmaceutical composition according claim 43, wherein the pharmaceutically acceptable carrier is suitable for subcutaneous delivery.

53. The pharmaceutical composition according claim 43, wherein the pharmaceutically acceptable carder is suitable for topical delivery.

54. The method according to claim 20, wherein the R is a monophosphate.

55. The method according to claim 20, wherein the R is a diphospbate.

56. The method according to claim 20, wherein the R is a triphosphate.

57. The method according to claim 20, wherein the R is an amino acid acyl residue.

58. The method according to claim 20, wherein the R is acyl.

59. The method according to claim 20, wherein the R is alkyl.

60. The method according to claim 20, wherein the R is a stabilized phosphate prodrug.

61. The pharmaceutical composition according to claim 43, wherein the R is a monophosphate.

62. The pharmaceutical composition according to claim 43, wherein the R is a diphosphate.

63. The pharmaceutical composition according to claim 43, wherein the R is a triphosphate.

64. The pharmaceutical composition according to claim 43, wherein the R is an amino acid acyl residue.

65. The pharmaceutical composition according to claim 43, wherein the R is acyl.

66. The pharmaceutical composition according to ciaim 43, wherein the R is alkyl.

67. The pharmaceutical composition according to claim 43, wherein the R is a stabilized phosphate prodrug.

68. The pharmaceutical composition according to claim 45 or 46, wherein the dosage unit is a tablet or capsule.

69. The pharmaceutical composition according to claim 43, wherein the anti-hepatitis agent is selected from the group consisting of .beta.-L-2-hydroxymcthyl-5-(cytosin-1-yl)-1,3-oxathiolane (3TC), cis-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane (FTC), .beta.-L-2'-fluoro-5-methyl-arabinofuranosyluridine (L-FMAU), .beta.-D-2,6-diaminopurine dioxolane (DAPD), famciclovir, penciclovir, 2-amino-1,9-dihydro-9-[4-hydroxy-3-(hydroxymethyl)-2-methylenecyclo-pentyl ]-6H-purin-6-one (entecavir, BMS-200475), 9-[2-(phosphono-methoxy)ethyl]-adenine (PMEA, adefovir, dipivoxil); 9-((1R,2R,3S)-2,3-bis(hydroxymethyl)cyclo-butyl)guanine (lobucavir), ganciclovir, and ribavirin.

70. The phannaceutical composition according to claim 43, wherein the anti-hepatitis agent is .beta.-L-2-hydroxymethyl-5-(cytosin-1-yl)-1,3-oxathiolane (3TC).

71. The pharmaceutical composition according to claim 43, wherein the anti-hepatitis agent is cis-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane (FTC).

72. The pharmaceutical composition according to claim 43, wherein the anti-hepatitis agent is L-2'-fluoro-5-methyl-arabinofuranosyluridine (L-FMAU).

73. The pharmaceutical composition according to claim 43, wherein the anti-hepatitis agent is .beta.-D-2,6-diaminopurine dioxolane (DAPD).

74. The pharmaceutical composition according to claim 43, wherein the anti-hepatitis agent is famicilovir.

75. The pharmaceutical composition according to claim 43, wherein the anti-hepatitis agent is penciclovir.

76. The pharmaceutical composition according to claim 43, wherein the anti-hepatitis agent is 2-amino-1,9dihydro-9-[4-hydroxy-3-(hydroxymethyl)-2-methylene-cyclopentyl] -6H-purin-6-one (entecavir, BMS-200475).

77. The pharmaceutical composition according to claim 43, wherein the anti-hepatitis agent is 9-[2-(phosphono-methoxy)ethy]-adenine (PMEA, adefovir, dipivoxil).

78. The pharmaceutical composition according to claim 43, wherein the anti-hepatitis agent is 9-((1R,2R,3S)-2,3-bis(hydroxymethyl)cyclo-butyl)guanine (lobucavir).

79. The pharmaceutical composition according to claim 43, wherein the anti-hepatitis agent is ganciclovir.

80. The pharmaceutical composition according to claim 43, wherein the anti-hepatitis agent is ribavirin.

81. The method of claim 20, wherein the .beta.-L-nucleoside is ##STR24## or a pharmaceutically acceptable salt thereof.
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