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Claims for Patent: 7,402,588

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Claims for Patent: 7,402,588

Title:Antiviral activity and resolution of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane
Abstract:A method and composition for the treatment of HIV and HBV infections in humans is disclosed that includes administering an effective amount of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane, a pharmaceutically acceptable derivative thereof, including a 5' or N.sup.4 alkylated or acylated derivative, or a pharmaceutically acceptable salt thereof, in a pharmaceutically acceptable carrier.A process for the resolution of a racemic mixture of nucleoside enantiomers is also disclosed that includes the step of exposing the racemic mixture to an enzyme that preferentially catalyzes a reaction in one of the enantiomers.
Inventor(s): Liotta; Dennis C. (Stone Mountain, GA), Schinazi; Raymond F. (Decatur, GA), Choi; Woo-Baeg (North Brunswick, NJ)
Assignee: Emory University (Atlanta, GA)
Application Number:11/390,861
Patent Claims: 1. A method for treating HIV infection in humans comprising administering an effective amount of (-)-.beta.-L-2-hydroxymethyl-5-(5-fluorocytosine-1-yl)-1,3-oxathiolane, or a compound of the formula: ##STR00008## wherein R.sub.1 and R.sub.2 are independently alkyl, acyl or an amino acid; and wherein one of R.sub.1 and R.sub.2 can be H, or physiologically acceptable salt, in a gelatin capsule for oral delivery.

2. A method for treating HIV infection in humans comprising administering an effective amount of (-)-.beta.-L-2-hydroxymethyl-5-(5-fluorocytosine-1-yl)-1,3-oxathiolane, or a compound of the formula: ##STR00009## wherein R.sub.1 and R.sub.2 are independently alkyl, acyl or an amino acid; and wherein one of R.sub.1 and R.sub.2 can be H, or physiologically acceptable salt, in a pharmaceutically acceptable carrier for oral delivery wherein the carrier comprises cellulose.

3. The method of claim 2 wherein the carrier comprises microcrystalline cellulose.

4. A method for treating HIV infection in humans comprising administering an effective amount of (-)-.beta.-L-2-hydroxymethyl-5-(5-fluorocytosine-1-yl)-1,3-oxathiolane, or a compound of the formula: ##STR00010## wherein R.sub.1 and R.sub.2 are independently alkyl, acyl or an amino acid; and wherein one of R.sub.1 and R.sub.2 can be H, or physiologically acceptable salt, in a pharmaceutically acceptable carrier for oral delivery wherein the carrier comprises magnesium stearate.

5. The method of claim 1 wherein R.sub.2 is H.

6. The method of claim 1 wherein R.sub.1 is alkyl.

7. The method of claim 1 wherein R.sub.1 is acyl.

8. The method of claim 1 wherein R.sub.1 is alkyl and R.sub.2 is H.

9. The method of claim 1 wherein R.sub.1 is acyl and R.sub.2 is H.

10. The method of claim 1 wherein R.sub.1 is H.

11. The method of claim 1 wherein R.sub.2 is alkyl.

12. The method of claim 1 wherein R.sub.2 is acyl.

13. The method of claim 1 wherein R.sub.2 is alkyl and R.sub.1 is H.

14. The method of claim 1 wherein R.sub.2 is acyl and R.sub.1 is H.

15. The method of claim 2 wherein R.sub.2 is H.

16. The method of claim 2 wherein R.sub.1 is alkyl.

17. The method of claim 2 wherein R.sub.1 is acyl.

18. The method of claim 2 wherein R.sub.1 is alkyl and R.sub.2 is H.

19. The method of claim 2 wherein R.sub.1 is acyl and R.sub.2 is H.

20. The method of claim 2 wherein R.sub.1 is H.

21. The method of claim 2 wherein R.sub.2 is alkyl.

22. The method of claim 2 wherein R.sub.2 is acyl.

23. The method of claim 2 wherein R.sub.2 is alkyl and R.sub.1 is H.

24. The method of claim 2 wherein R.sub.2 is acyl and R.sub.1 is H.

25. The method of claim 4 wherein R.sub.2 is H.

26. The method of claim 4 wherein R.sub.1 is alkyl.

27. The method of claim 4 wherein R.sub.1 is acyl.

28. The method of claim 4 wherein R.sub.1 is alkyl and R.sub.2 is H.

29. The method of claim 4 wherein R.sub.1 is acyl and R.sub.2 is H.

30. The method of claim 4 wherein R.sub.1 is H.

31. The method of claim 4 wherein R.sub.2 is alkyl.

32. The method of claim 4 wherein R.sub.2 is acyl.

33. The method of claim 4 wherein R.sub.2 is alkyl and R.sub.1 is H.

34. The method of claim 4 wherein R.sub.2 is acyl and R.sub.1 is H.

35. The method of claim 1, wherein an effective amount of (-)-.beta.-L-2-hydroxymethyl-5-(5-fluorocytosine-1-yl)-1,3-oxathiolane is administered.

36. The method of claim 2, wherein an effective amount of (-)-.beta.-L-2-hydroxymethyl-5-(5-fluorocytosine-1-yl)-1,3-oxathiolane is administered.

37. The method of claim 4, wherein an effective amount of (-)-.beta.-L-2-hydroxymethyl-5-(5-fluorocytosine-1-yl)-1,3-oxathiolane is administered.

38. A pharmaceutical composition for treating HIV infection in humans comprising an effective amount of (-)-.beta.-L-2-hydroxymethyl-5-(5-fluorocytosine-1-yl)-1,3-oxathiolane, or a compound of the formula: ##STR00011## wherein R.sub.1 and R.sub.2 are independently alkyl, acyl or an amino acid; and wherein one of R.sub.1 and R.sub.2 can be H, or physiologically acceptable salt, in a gelatin capsule for oral delivery.

39. A pharmaceutical composition for treating HIV infection in humans comprising an effective amount of (-)-.beta.-L-2-hydroxymethyl-5-(5-fluorocytosine-1-yl)-1,3-oxathiolane, or a compound of the formula: ##STR00012## wherein R.sub.1 and R.sub.2 are independently alkyl, acyl or an amino acid; and wherein one of R.sub.1 and R.sub.2 can be H, or physiologically acceptable salt, in a pharmaceutically acceptable carrier for oral delivery wherein the carrier comprises cellulose.

40. The pharmaceutical composition of claim 39 wherein the carrier comprises microcrystalline cellulose.

41. A pharmaceutical composition for treating HIV infection in humans comprising an effective amount of (-)-.beta.-L-2-hydroxymethyl-5-(5-fluorocytosine-1-yl)-1,3-oxathiolane, or a compound of the formula: ##STR00013## wherein R.sub.1 and R.sub.2 are independently alkyl, acyl or an amino acid; and wherein one of R.sub.1 and R.sub.2 can be H, or physiologically acceptable salt, in a pharmaceutically acceptable carrier for oral delivery wherein the carrier compnses magnesium stearate.

42. The pharmaceutical composition of claim 38 wherein R.sub.2 is H.

43. The pharmaceutical composition of claim 38 wherein R.sub.1 is alkyl.

44. The pharmaceutical composition of claim 38 wherein R.sub.1 is acyl.

45. The pharmaceutical composition of claim 38 wherein R.sub.1 is alkyl and R.sub.2 is H.

46. The pharmaceutical composition of claim 38 wherein R.sub.1 is acyl and R.sub.2 is H.

47. The pharmaceutical composition of claim 38 wherein R.sub.1 is H.

48. The pharmaceutical composition of claim 38 wherein R.sub.2 is alkyl.

49. The pharmaceutical composition of claim 38 wherein R.sub.2 is acyl.

50. The pharmaceutical composition of claim 38 wherein R.sub.2 is alkyl and R.sub.1 is H.

51. The pharmaceutical composition of claim 38 wherein R.sub.2 is acyl and R.sub.1 is H.

52. The pharmaceutical composition of claim 39 wherein R.sub.2 is H.

53. The pharmaceutical composition of claim 39 wherein R.sub.1 is alkyl.

54. The pharmaceutical composition of claim 39 wherein R.sub.1 is acyl.

55. The pharmaceutical composition of claim 39 wherein R.sub.1 is alkyl and R.sub.2 is H.

56. The pharmaceutical composition of claim 39 wherein R.sub.1 is acyl and R.sub.2 is H.

57. The pharmaceutical composition of claim 39 wherein R.sub.1 is H.

58. The pharmaceutical composition of claim 39 wherein R.sub.2 is alkyl.

59. The pharmaceutical composition of claim 39 wherein R.sub.2 is acyl.

60. The pharmaceutical composition of claim 39 wherein R.sub.2 is alkyl and R.sub.1 is H.

61. The pharmaceutical composition of claim 39 wherein R.sub.2 is acyl and R.sub.1 is H.

62. The pharmaceutical composition of claim 41 wherein R.sub.2 is H.

63. The pharmaceutical composition of claim 41 wherein R.sub.1 is alkyl.

64. The pharmaceutical composition of claim 41 wherein R.sub.1 is acyl.

65. The pharmaceutical composition of claim 41 wherein R.sub.1 is alkyl and R.sub.2 is H.

66. The pharmaceutical composition of claim 41 wherein R.sub.1 is acyl and R.sub.2 is H.

67. The pharmaceutical composition of claim 41 wherein R.sub.1 is H.

68. The pharmaceutical composition of claim 41 wherein R.sub.2 is alkyl.

69. The pharmaceutical composition of claim 41 wherein R.sub.2 is acyl.

70. The pharmaceutical composition of claim 41 wherein R.sub.2 is alkyl and R.sub.1 is H.

71. The pharmaceutical composition of claim 41 wherein R.sub.2 is acyl and R.sub.1 is H.

72. The pharmaceutical composition of claim 41 wherein R.sub.2 is H.

73. The pharmaceutical composition of claim 38, wherein the composition comprises an effective amount of (-)-.beta.-L-2-hydroxymethyl-5-(5-fluorocytosine-1-yl)-1,3-oxathiolane.

74. The pharmaceutical composition of claim 39, wherein the composition comprises an effective amount of (-)-.beta.-L-2-hydroxymethyl-5-(5-fluorocytosine-1-yl)-1,3-oxathiolane.

75. The pharmaceutical composition of claim 41, wherein the composition comprises an effective amount of (-)-.beta.-L-2-hydroxymethyl-5-(5-fluorocytosine-1-yl)-1,3-oxathiolane.
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