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Claims for Patent: 6,569,837

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Claims for Patent: 6,569,837

Title: .beta.-L-2'-deoxy pyrimidine 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)
Application Number:10/022,276
Patent Claims: 1. A method for the treatment of a hepatitis B virus infection in a human comprising administering an effective amount of a compound of the formula: ##STR20##

or pharmaceutically acceptable salt thereof, in combination or alternation with an effective amount of .beta.-L-2-hydroxymethyl-5-(cytosin-1-yl)-1,3-oxathiolane (3TC), or pharmaceutically acceptable salt thereof.

2. A method for the treatment of a hepatitis B virus infection in a human comprising administering an effective amount of a compound of the formula: ##STR21##

or pharmaceutically acceptable salt thereof, in combination or alternation with an effective amount of cis-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane (FTC), or pharmaceutically acceptable salt thereof.

3. A method for the treatment of a hepatitis B virus infection in a human comprising administering an effective amount of a compound of the formula: ##STR22##

or pharmaceutically acceptable salt thereof, in combination or alternation with an effective amount of .beta.-L-2'-fluoro-5-methyl-arabinofuranosyl-uridine (L-FMAU), or pharmaceutically acceptable salt thereof.

4. A method for the treatment of a hepatitis B virus infection in a human comprising administering an effective amount of a compound of the formula: ##STR23##

or pharmaceutically acceptable salt thereof, in combination or alternation with an effective amount of .beta.-D-2,6-diaminopurine dioxolane (DAPD), or pharmaceutically acceptable salt thereof.

5. A method for the treatment of a hepatitis B virus infection in a human comprising administering an effective amount of a compound of the formula: ##STR24##

or pharmaceutically acceptable salt thereof, in combination or alternation with an effective amount of famciclovir, or pharmaceutically acceptable salt thereof.

6. A method for the treatment of a hepatitis B virus infection in a human comprising administering an effective amount of a compound of the formula: ##STR25##

or pharmaceutically acceptable salt thereof, in combination or alternation with an effective amount of penciclovir, or pharmaceutically acceptable salt thereof.

7. A method for the treatment of a hepatitis B virus infection in a human comprising administering an effective amount of a compound of the formula: ##STR26##

or pharmaceutically acceptable salt thereof, in combination or alternation with an effective amount of 2-amino-1,9-dihydro-9-[4-hydroxy-3-(hydroxymethyl)-2-methylene-cyclopentyl ]-6H-purin-6-one (entecavir, BMS-200475), or pharmaceutically acceptable salt thereof.

8. A method for the treatment of a hepatitis B virus infection in a human comprising administering an effective amount of a compound of the formula: ##STR27##

or pharmaceutically acceptable salt thereof, in combination or alternation with an effective amount of 9-[2-(phosphono-methoxy)ethyl]adenine (PMEA, adefovir, dipivoxil), or pharmaceutically acceptable salt thereof.

9. A method for the treatment of a hepatitis B virus infection in a human comprising administering an effective amount of a compound of the formula: ##STR28##

or pharmaceutically acceptable salt thereof, in combination or alternation with an effective amount of lobucavir, or pharmaceutically acceptable salt thereof.

10. A method for the treatment of a hepatitis B virus infection in a human comprising administering an effective amount of a compound of the formula: ##STR29##

or pharmaceutically acceptable salt thereof, in combination or alternation with an effective amount of ganciclovir, or pharmaceutically acceptable salt thereof.

11. A method for the treatment of a hepatitis B virus infection in a human comprising administering an effective amount of a compound of the formula: ##STR30##

or pharmaceutically acceptable salt thereof, in combination or alternation with an effective amount of ribavirin, or pharmaceutically acceptable salt thereof.

12. A method for the treatment of a hepatitis B virus infection in a human comprising administering an effective amount of a compound of the formula: ##STR31##

or pharmaceutically acceptable salt thereof, in combination or alternation with an effective amount of .beta.-L-2-hydroxymethyl-5-(cytosin-1-yl)-1,3-oxathiolane (3TC), or pharmaceutically acceptable salt thereof.

13. A method for the treatment of a hepatitis B virus infection in a human comprising administering an effective amount of .beta.-L-2'-deoxycytidine of the formula: ##STR32##

or pharmaceutically acceptable salt thereof.

14. A method for the treatment of a hepatitis B virus infection in a human comprising administering an effective amount of .beta.-L-thymidine of the formula: ##STR33##

or pharmaceutically acceptable salt thereof.

15. A method for the treatment of a hepatitis B virus infection in a human comprising administering an effective amount of a combination of the following nucleosides: ##STR34##

or pharmaceutically acceptable salt thereof.

16. A method for the treatment of a hepatitis B virus infection in a human comprising administering an effective amount of a compound of the formula: ##STR35##

or pharmaceutically acceptable salt thereof, in combination or alternation with an effective amount of a compound 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-oxathiolane (FTC), .beta.-L-2'-fluoro-5-methyl-arabinofuranosyl-uridine (L-FMAU), .beta.-D-2,6-diaminopurine dioxolane (DAPD), famciclovir, penciclovir, 2-amino-1,9-dihydro-9-[4-hydroxy-3-(hydroxymethyl)-2-methylenecyclopentyl] -6H-purin-6-one (entecavir, BMS-200475), 9-[2-(phosphono-methoxy)ethyl]adenine (PMEA, adefovir, dipivoxil); lobucavir, ganciclovir and ribavirin.

17. A method the treatment of a hepatitis B virus infection in a human comprising administering an effective amount of a compound of the formula: ##STR36##

or pharmaceutically acceptable salt thereof, in combination or alternation with an effective amount of a compound 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-oxathiolane (FTC), .beta.-L-2'-fluoro-5-methyl-arabinofuranosyl-uridine (L-FMAU), .beta.-D-2,6-diaminopurine dioxolane (DAPD), famciclovir, penciclovir, 2-amino-1,9-dihydro-9-[4-hydroxy-3-(hydroxymethyl)-2-methylenecyclopentyl] -6H-purin-6-one (entecavir, BMS-200475), 9-[2-(phosphono-methoxy)ethyl]adenine (PMEA, adefovir, dipivoxil); lobucavir, ganciclovir and ribavirin.

18. The method of claim 13, wherein the .beta.-L-2'-deoxycytidine is at least 95% in its designated enantiomeric form.

19. The method of claim 13, wherein the .beta.-L-2'-deoxycytidine is administered in a pharmaceutically acceptable carrier.

20. The method of claim 19, wherein the pharmaceutically acceptable carrier is suitable for oral delivery.

21. The method of claim 19, wherein the pharmaceutically acceptable carrier is suitable for intravenous delivery.

22. The method of claim 19, wherein the pharmaceutically acceptable carrier is suitable for parenteral delivery.

23. The method of claim 19, wherein the pharmaceutically acceptable carrier is suitable for intradermal delivery.

24. The method of claim 19, wherein the pharmaceutically acceptable carrier is suitable for subcutaneous deliery.

25. The method of claim 19, wherein the pharmaceutically acceptable carrier is suitable for topical delivery.

26. The method of claim 19, wherein the compound is in the form of a dosage unit.

27. The method of claim 26, wherein the dosage unit contains 10 to 1500 mg of the compound.

28. The method of claim 26 or 27, wherein the dosage unit is a tablet or capsule.

29. The method of claim 14, wherein the .beta.-L-thymidine is at least 95% in its designated enantiomeric form.

30. The method of claim 14, wherein the .beta.-L-thymidine is administered in a pharmaceutically acceptable carrier.

31. The method of claim 29, wherein the pharmaceutically acceptable carrier is suitable for oral delivery.

32. The method of claim 29, wherein the pharmaceutically acceptable carrier is suitable for intravenous delivery.

33. The method of claim 29, wherein the pharmaceutically acceptable carrier is suitable for parenteral delivery.

34. The method of claim 29, wherein the pharmaceutically acceptable carrier is suitable for intradermnal delivery.

35. The method of claim 29, wherein the pharmaceutically acceptable carrier is suitable for subcutaneous delivery.

36. The method of claim 29, wherein the pharmaceutically acceptable carrier is suitable for topical delivery.

37. The method of claim 29, wherein the compound is in the form of a dosage unit.

38. The method of claim 37, wherein the dosage unit contains 10 to 1500 mg of the compound.

39. The method of claim 37 or 38, wherein the dosage unit is a tablet or capsule.

40. A method for the treatment of a heptitis B virus infection in a human compriding administering an effective amount of a compound of the formula: ##STR37##

or pharmaceutically acceptable salt thereof, in combination or alternation with an effective amount of cis-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane (FTC), or pharmaceutically acceptable salt thereof.

41. A method for the treatment of a hepatitis B virus infection in a human comprising administering an effective amount of a compound of the formula: ##STR38##

or pharmaceutically acceptable salt thereof, in combination or alternation with an effective amount of .beta.-L-2'-fluoro-5-methyl-arabinofuranosyl-uridine (L-FMAU), or pharmaceutically acceptable salt thereof.

42. A method for the treatment of a hepatitis B virus infection in a human comprising administering an effective amount of a compound of the formula: ##STR39##

or pharmaceutically acceptable salt thereof, in combination or alternation with an effective amount of .beta.-D-2,6-diaminopurine dioxolane (DAPD), or pharmaceutically acceptable salt thereof.

43. A method for the treatment of a hepatitis B virus infection in a human comprising administering an effective amount of a compound of the formula: ##STR40##

or pharmaceutically acceptable salt thereof, in combination or alternation with an effective amount of famciclovir, or pharmaceutically acceptable salt thereof.

44. A method for the treatment of a hepatitis B virus infection in a human comprising administering an effective amount of a compound of the formula: ##STR41##

or pharmaceutically acceptable salt thereof, in combination or alternation with an effective amount of penciclovir, or pharmaceutically acceptable salt thereof.

45. A method for the treatment of a hepatitis B virus infection in a human comprising administering an effective amount of a compound of the formula: ##STR42##

or pharmaceutically acceptable salt thereof, in combination or alternation with an effective amount of 2-amino-1,9-dihydro-9-[4-hydroxy-3-(hydroxymethyl)-2-methylene-cyclopentyl ]-6H-purin-6-one (entecavir, BMS-200475), or pharmaceutically acceptable salt thereof.

46. A method for the treatment of a hepatitis B virus infection in a human comprising administering an effective amount of a compound of the formula: ##STR43##

or pharmaceutically acceptable salt thereof, in combination or alternation with an effective amount of 9-[2-(phosphono-methoxy)ethyl]adenine (PMEA, adefovir, dipivoxil), or pharmaceutically acceptable salt thereof.

47. A method for the treatment of a hepatitis B virus infection in a human comprising administering an effective amount of a compound of the formula: ##STR44##

or pharmaceutically acceptable salt thereof, in combination or alternation with an effective amount of lobucavir, or pharmaceutically acceptable salt thereof.

48. A method for the treatment of a hepatitis B virus infection in a human comprising administering an effective amount of a compound of the formula: ##STR45##

or pharmaceutically acceptable salt thereof, in combination or alternation with an effective amount of ganciclovir, or pharmaceutically acceptable salt thereof.

49. A method for the treatment of a hepatitis B virus infection in a human comprising administering an effective amount of a compound of the formula: ##STR46##

or pharmaceutically acceptable salt thereof, in combination or alternation with an effective amount of ribavirin, or pharmaceutically acceptable salt thereof.
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