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Claims for Patent: 5,210,085

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Claims for Patent: 5,210,085

Title: Method for the synthesis, compositions and use of 2'-deoxy-5-fluoro-3'-thiacytidine and related compounds
Abstract:The present invention relates to a method of preparing the antiviral compounds 2'-deoxy-5-fluoro-3'thiacytidine (FTC) and various prodrug analogues of FTC from inexpensive precursors with the option of introducing functionality as needed; methods of using these compounds, particularly in the prevention and treatment of AIDS; and the compounds themselves. This synthetic route allows the stereoselective preparation of the biologically active isomer of these compounds and related compounds.
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:07/659,760
Patent Claims: 1. A method for treating a human having an HIV infection comprising administering to the human an effective HIV-treatment amount of a compound of the formula: ##STR9##

2. The method of claim 1, wherein the pharmaceutically acceptable derivative comprises a monophosphate, diphosphate, or triphosphate ester of 2'-deoxy-5-fluoro-3'-thiacytidine.

3. The method of claim 1, wherein the pharmaceutically acceptable carrier comprises a liposomal suspension.

4. A method for treating a human having an HIV infection comprising administering to the human an effective HIV-treatment amount of a .beta.-isomer of a substituted 2'-deoxy-5-fluoro-3'-thiacytidine having the formula: ##STR10## wherein Y is independently selected from the group consisting of H, alkyl, substituted alkyl, cycloalkyl and acyl; and

R is selected from the group consisting of H, hydroxyl, oxyacyl, monophosphate, diphosphate, and triphosphate.

5. The method of claim 4, wherein the substituted 2'-deoxy-5-fluoro-3'-thiacytidine is selected from the group consisting of the monophosphate, diphosphate, and triphosphate ester of 2'-deoxy-5-fluoro-3'-thiacytidine.

6. The method of claim 4, wherein the pharmaceutically acceptable carrier comprises a liposomal suspension.

7. The method of claim 4, wherein the .beta.-isomer of the substituted 2'-deoxy-5-fluoro-3'-thiacytidine is selected from the group consisting of 4-N-acetyl-2'-deoxy-5-fluoro-3'-thiacytidine; 4-N-acetyl-5'-butyryl-2'-deoxy-5-fluoro-3'-thiacytidine; and 5'-butyryl-2'-deoxy-5-fluoro-3'-thiacytidine.

8. A method for treating a human having an HIV infection comprising administering to the human an effective HIV treatment amount of a compound of the formula: ##STR11## wherein Y is monophosphate, diphosphate, or triphosphate.

9. A method for treating a human having an HIV infection comprising administering to the human an effective HIV-treatment amount of a compound of the formula: ##STR12## wherein Y is independently selected from the group consisting of H, alkyl, cycloalkyl, and acyl; and

R is selected from the group consisting of H, hydroxyl, oxyacyl, monophosphate, diphosphate, and triphosphate.

10. A method for treating a human having an HIV infection comprising administering to the human an effective HIV-treatment amount of a pharmaceutically acceptable salt of a compound of the formula: ##STR13##

11. A method for treating a human having an HIV infection comprising administering to the human an effective HIV-treatment amount of the pharmaceutically acceptable salt of .beta.-isomer of a substituted 2'-deoxy-5-fluoro-3'-thiacytidine having the formula: ##STR14## wherein Y is independently selected from the group consisting of H, alkyl, substituted alkyl, cycloalkyl and acyl; and

R is selected from the group consisting of H, hydroxy, oxyacyl, monophosphate, diphosphate, and triphosphate.

12. A method for treating a human having an HIV infection comprising administering to the human an effective HIV-treatment amount of a pharmaceutically acceptable salt of a compound of the formula: ##STR15## wherein Y is monophosphate, diphosphate, or triphosphate.

13. A method for treating a human having an HIV infection comprising administering to the human an effective HIV treatment amount of the pharmaceutically acceptable salt of a compound of the formula: ##STR16## wherein Y is independently selected from the group consisting of H, alkyl, cycloalkyl and acyl; and

R is selected from the group consisting of H, hydroxyl, oxyacyl, monophosphate, diphosphate, and triphosphate.

14. The method of claim 1, wherein the compound is administered in a pharmaceutically acceptable carrier.

15. The method of claim 4, wherein the compound is administered in a pharmaceutically acceptable carrier.

16. The method of claim 8, wherein the compound is administered in a pharmaceutically acceptable carrier.

17. The method of claim 9, wherein the compound is administered in a pharmaceutically acceptable carrier.

18. The method of claim 10, wherein the compound is administered in a pharmaceutically acceptable carrier.

19. The method of claim 11, wherein the compound is administered in a pharmaceutically acceptable carrier.

20. The method of claim 12, wherein the compound is administered in a pharmaceutically acceptable carrier.

21. The method of claim 13, wherein the compound is administered in a pharmaceutically acceptable carrier.
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