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Claims for Patent: 6,180,639

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Claims for Patent: 6,180,639

Title: 1,3-oxathiolane nucleoside analogues
Abstract:(-)-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one, its pharmaceutically acceptable derivatives, pharmaceutical formulation thereof, methods for its preparation and its uses as an antiviral agent are described.
Inventor(s): Coates; Jonathan Allan (Greenford, GB), Mutton; Ian Martin (Greenford, GB), Penn; Charles Richard (Greenford, GB), Williamson; Christopher (Greenford, GB), Storer; Richard (Greenford, GB)
Assignee: BioChem Pharma Inc. (Laval, CA)
Application Number:07/835,964
Patent Claims: 1. A method for treating a human suffering from HIV infection comprising administering to said human a pharmaceutical composition comprising: a compound which is (-)-cis-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5yl)-(1H)-pyrimidin-2-on e or a pharmaceutically acceptable salt thereof, another agent having antiviral activity, and a pharmaceutically acceptable carrier, and

wherein the amount of the (+)-enantiomer of said compound or of said pharmaceutically acceptable salt present in said composition is no more than 5% w/w, relative to the combined weight of the (-) and (+)-enantiomers thereof.

2. A method according to claim 1, wherein said agent is an acyclic nucleoside, an interferon, a renal excretion inhibitor, a nucleoside transport inhibitor, a 2',3'-dideoxynucleoside, an immunomodulator, erythropoietin, ampligen, thyomodulin, thymopentin, foscarnet, ribavirin, or an inhibitor of HIV binding to CD4.

3. A method according to claim 1, wherein the amount of said compound or pharmaceutically acceptable salt is 10-1500 mg.

4. A method according to claim 3, wherein the amount of said compound or pharmaceutically acceptable salt is 20-1000 mg.

5. A method according to claim 4, wherein the amount of said compound or pharmaceutically acceptable salt is 50-70 mg.

6. A method according to claim 1, wherein said composition contains an amount of the (+)-enantiomer of no more than 2% w/w.

7. A method according to claim 6, wherein said composition contains an amount of the (+)-enantiomer of no more than 1% w/w.

8. A method according to claim 1, wherein said compound or pharmaceutically acceptable salt and said agent are administered sequentially.

9. A method according to claim 1, wherein said compound or pharmaceutically acceptable salt and said agent are administered simultaneously.

10. A method according to claim 1,

wherein said compound is administered at a dosage of 0.1-750 mg/kg of body weight per day.

11. A method according to claim 10, wherein said compound or pharmaceutically acceptable salt is administered at a dosage of 0.5-60 mg/kg of body weight per day.

12. A method according to claim 11, wherein said compound or pharmaceutically acceptable salt is administered at a dosage of 1-20 mg/kg of body weight per day.

13. A pharmaceutical composition comprising:

a pharmaceutically acceptable carrier, a compound which is (-)-cis-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-o ne or a pharmaceutically acceptable salt thereof, and another agent having antiviral activity

wherein the amount of the (+)-enantiomer of said compound or of said pharmaceutically acceptable salt present in said composition is no more than 5% w/w, relative to the combined weight of the (-) and (+)-enantiomers thereof.

14. A composition according to claim 13, wherein said agent is an acyclic nucleoside, an interferon, a renal excretion inhibitor, a nucleoside transport inhibitor, a 2',3'-dideoxynucleoside, an immunomodulator, erythropoetin, ampligen, thyomodulin, thymopentin, foscarnet, ribavirin, or an inhibitor of HIV binding to CD4.

15. A composition according to claim 13, wherein said composition contains 10-1500 mg of said compound or pharmaceutically acceptable salt.

16. A composition according to claim 15, wherein said composition contains 20-1000 mg of said compound or pharmaceutically acceptable salt.

17. A composition according to claim 16, wherein said composition contains 50-700 mg of said compound or pharmaceutically acceptable salt.

18. A composition according to claim 13, wherein said compound is (-)-cis-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-o ne.

19. A composition according to claim 18, wherein said agent is an acyclic nucleoside, an interferon, a renal excretion inhibitor, a nucleoside transport inhibitor, a 2',3'-dideoxynucleoside, an immunomodulator, erythropoetin, ampligen, thyomodulin, thymopentin, foscarnet, ribavirin, or an inhibitor of HIV binding to CD4.

20. A composition according to claim 18, wherein said composition contains 10-1500 mg of said compound.

21. A composition according to claim 20, wherein said composition contains 20-1000 mg of said compound.

22. A composition according to claim 21, wherein said composition contains 50-700 mg of said compound.

23. A composition according to claim 13, wherein said composition contains an amount of the (+)-enantiomer of no more than 2% w/w.

24. A composition according to claim 23, wherein said composition contains an amount of the (+)-enantiomer of no more than 1% w/w.

25. A composition according to claim 18, wherein said composition contains an amount of the (+)-enantiomer of no more than 2% w/w.

26. A composition according to claim 25, wherein said composition contains an amount of the (+)-enantiomer of no more than 1% w/w.

27. A method according to claim 1, wherein said compound is (-)-cis-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-o ne.

28. A method according to claim 2, wherein said compound is (-)-cis-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-o ne.

29. A method according to claim 28, wherein the amount of said compound is 10-1500 mg.

30. A method according to claim 29, wherein the amount of said compound is 20-1000 mg.

31. A method according to claim 30, wherein the amount of said compound is 50-700 mg.

32. A method according to claim 28, wherein said composition contains an amount of the (+)-enantiomer of no more than 2% w/w.

33. A method according to claim 32, wherein said composition contains an amount of the (+)-enantiomer of no more than 1% w/w.

34. A method according to claim 27, wherein said composition contains an amount of the (+)-enantiomer of no more than 2% w/w.

35. A method according to claim 34, wherein said composition contains an amount of the (+)-enantiomer of no more than 1% w/w.

36. A method according to claim 28, wherein said compound and said agent are administered sequentially.

37. A method according to claim 28, wherein said compound and said agent are administered sequentially.

38. A method according to claim 28, wherein said compound is administered at a dosage of 0.1-750 mg/kg of body weight per day.

39. A method according to claim 38, wherein said compound is administered at a dosage of 0.5-60 mg/kg of body weight per day.

40. A method according to claim 38, wherein said compound is administered at a dosage of 1-20 mg/kg of body weight per day.

41. A composition according to claim 19, wherein said composition contains 10-1500 mg of said compound or pharmaceutically acceptable salt.

42. A composition according to claim 41, wherein said composition contains 20-1000 mg of said compound or pharmaceutically acceptable salt.

43. A composition according to claim 42, wherein said composition contains 50-700 mg of said compound or pharmaceutically acceptable salt.

44. A composition according to claim 41, wherein said composition contains an amount of the (+)-enantiomer of no more than 2% w/w.

45. A composition according to claim 44, wherein said composition contains an amount of the (+)-enantiomer of no more than 1% w/w.

46. A method according to claim 1, wherein said compound or pharmaceutically acceptable salt and said agent are administered in combination.

47. A method according to claim 2, wherein said compound or pharmaceutically acceptable and said agent are administered in combination.

48. A method according to claim 28, wherein said compound and said agent are administered in combination.

49. A method for treating a human suffering from HIV infection comprising administering to said human a pharmaceutical composition comprising: a compound which is (-)-cis-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-1H)-pyrimidin-2-on e or a pharmaceutically acceptable salt thereof, and another agent having antiviral activity,

wherein the amount of the (+)-enantiomer of said compound or of said pharmaceutically acceptable salt present in said composition is not more than 5% w/w, relative to the combined weight of the (-) and (+)-enantiomers thereof.

50. A method according to claim 49, wherein said composition contains (-)-cis-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-o ne.

51. A method according to claim 49, wherein said agent is an acyclic nucleoside, an interferon, a renal excretion inhibitor, a nucleoside transport inhibitor, a 2',3'-dideoxynucleoside, an immunomodulator, erythropoietin, ampligen, thyomodulin, thymopentin, foscarnet, ribavirin, or an inhibitor of HIV binding to CD4.

52. A method according to claim 50, wherein said agent is an acyclic nucleoside, an interferon, a renal excretion inhibitor, a nucleoside transport inhibitor, a 2',3'-dideoxynucleoside, an immunomodulator, erythropoietin, ampligen, thyomodulin, thymopentin, foscarnet, ribavirin, or an inhibitor of HIV binding to CD4.

53. A pharmaceutical composition comprising:

a compound which is (-)-cis-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-o ne or a pharmaceutically acceptable salt thereof, and another agent having antiviral activity

wherein the amount of the (+)-enantiomer of said compound or of said pharmaceutically acceptable salt present in said composition is no more than 5% w/w, relative to the combined weight of the (-) and (+)-enantiomers thereof.

54. A composition according to claim 53, wherein said composition contains (-)-cis-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-o ne.

55. A composition according to claim 53, wherein said agent is an acyclic nucleoside, an interferon, a renal excretion inhibitor, a nucleoside transport inhibitor, a 2',3'-dideoxynucleoside, an immunomodulator, erythropoietin, ampligen, thyomodulin, thymopentin, foscarnet, ribavirin, or an inhibitor of HIV binding to CD4.

56. A composition according to claim 54, wherein said agent is an acyclic nucleoside, an interferon, a renal excretion inhibitor, a nucleoside transport inhibitor, a 2',3'-dideoxynucleoside, an immunomodulator, erythropoietin, ampligen, thyomodulin, thymopentin, foscarnet, ribavirin, or an inhibitor of HIV binding to CD4.

57. A combination comprising:

a compound which is (-)-cis-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H )-pyrimidin-2-one or a pharmaceutically accepted salt thereof, and another agent having antiviral activity

wherein the amount of the (+)-enantiomer of said compound or of said pharmaceutically acceptable salt present in said combination is no more than 5% w/w, relative to the combined weight of the (-) and (+)-enantiomers thereof.

58. A combination accroding to claim 57, wherein said combination contains (-)-cis-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H )-pyrimidin-2-one.

59. A combination according to claim 57, wherein said agent is an acyclic nucleoside, an interferon, a renal extretion inhibitor, a nucleoside transport inhibitor, a 2',3'-dideoxynucleoside, an immunomodulator, erythropoietin, ampligen, thyomodulin, thymopentin, foscarnet, ribavirin, or an inhibitor of HIV binding to CD4.

60. A combination according to claim 58, wherein said agent is an acyclic nucleoside, an interferon, a renal excretion inhibitor, a nucleoside transport inhibitor, a 2',3'-dideoxynucleoside, an immunomodulator, erythropoietin, ampligen, thyomodulin, thymopentin, foscarnet, ribavirin, or an inhibitor of HIV binding to CD4.

61. An article of manufacture according to claim 61, wherein said first amount contains (-)-cis-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-o ne or a pharmaceutically acceptable salt thereof, wherein the content of the (+)-enantiomer of said compound or of said pharmaceutically acceptable salt present in said fist amount is no more than 5% w/w/, relative to the combined weight of the (-) and (+)-enantiomers thereof, and

a second amount of another agent having antiviral activity.

62. An article of manufacture according to claim 61, wherein said first amount contains (-)-cis-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-o ne.

63. An article of manufacture according to claim 61, wherein said agent is an acyclic nucleoside, an interferon, a renal excretion inhibitor, a nucleoside transport inhibitor, a 2',3'-dideoxynucleoside, an immunomodulator, erythropoietin, ampligen, thyomodulin, thymopentin, foscarnet, ribavirin, or an inhibitor of HIV binding to CD4.

64. An article of manufacture according to claim 61, wherein said agent is an acyclic nucleoside, an interferon, a renal excretion inhibitor, a nucleoside transport inhibitor, a 2',3'-dideoxynucleoside, an immunomodulator, erythropoietin, ampligen, thyomodulin, thymopentin, foscarnet, ribavirin, or an inhibitor of HIV binding to CD4.
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