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Claims for Patent: 6,703,396

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Claims for Patent: 6,703,396

Title: Method of resolution and antiviral activity of 1,3-oxathiolane nuclesoside enantiomers
Abstract:A process for the resolution of a racemic mixture of nucleoside enantiomers that includes the step of exposing the racemic mixture to an enzyme that preferentially catalyzes a reaction in one of the enantiomers. The nucleoside enantiomer (-)-2-hydroxymethyl-5-(5-flurocytosin-1-yl)-1,3-oxathiolane is an effective antiviral agent against HIV, HBV, and other viruses replicating in a similar manner.
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:08/402,730
Patent Claims: 1. The (-)-enantiomer of cis-4-amino-5-fluoro-1-(2-hydroxymethyl-1,3-oxathiolane-5-yl)-(1H)-pyrimid in-2-one that is at least 95% free of the corresponding (+)-enantiomer.

2. (-)-Cis-4-amino-5-fluoro-1-(2-hydroxymethyl-1,3-oxathiolane-5-yl)-(1H)-pyr imidin-2-one or a pharmaceutically acceptable salt, ester or salt of an ester thereof.

3. The substantially pure (-)-enantiomer of cis-4-amino-5-fluoro-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidi n-2-one or a pharmaceutically acceptable salt, ester, or salt of an ester thereof, wherein the (+) enantiomer is present in an amount of no more than 5% w/w.

4. The compound of claim 3 wherein the (+)-enantiomer is present in an amount of no more than about 2% w/w.

5. The compound of claim 3 wherein the (+)-enantiomer is present in an amount of less than 1% w/w.

6. A pharmaceutical composition comprising a compound as claimed in any one of claims 2-5 in combination with a pharmaceutically acceptable carrier.

7. (-)-Cis-4-amino-5-fluoro-1-(2-hydroxymethyl-1,3-oxathiolane-5-yl)-(1H)-pyr imidin-2-one or a pharmaceutically acceptable salt thereof.

8. The 5'-O-alkyl derivative of the (-)-enantiomer of cis-4-amino-5-fluoro-1-(2-hydroxymethyl-1,3-oxathiolane-5-yl)-(1H)-pyrimid in-2-one.

9. The 5'-O-alkylC(O)-derivative of the (-)-enantiomer of cis-4-amino-5-fluoro-1-(2-hydroxymethyl-1,3-oxathiolane-5-yl)-(1H)-pyrimid in-2-one.

10. The derivative of claim 9, wherein alkylC(O)-- is selected from the group consisting of acetic, propionic, butyric, and pentanoic.

11. The monophosphate, diphosphate, or triphosphate of the (-)-enantiomer of cis-4-amino-5-fluoro-1-(2-hydroxymethyl-1,3-oxathiolane-5-yl)-(1H)-pyrimid in-2-one.

12. A pharmaceutically acceptable salt of the (-)-enantiomer of cis-4-amino-5-fluoro-1-(2-hydroxymethyl-1,3-oxathiolane-5-yl)-(1H)-pyrimid in-2-one that is at least 95% free of the corresponding (+)-enantiomer.

13. A pharmaceutical composition comprising an effective HIV treatment amount for humans of the (-)-enantiomer of cis-4-amino-5-fluoro-1-(2-hydroxymethyl-1,3-oxathiolane-5-yl)-(1H)-pyrimid in-2-one that is at least 95% free of the corresponding (+)-enantiomer, in combination with a pharmaceutically acceptable carrier or diluent.

14. A pharmaceutical composition comprising an effective HIV treatment amount for humans of the (-)-enantiomer of a pharmaceutically acceptable salt of a compound of cis-4-amino-5-fluoro-1-(2-hydroxymethyl-1,3-oxathiolane-5-yl)-(1H)-pyrimdi n-2-one that is at least 95% free of the corresponding (+)-enantiomer, in combination with a pharmaceutically acceptable carrier or diluent.

15. The pharmaceutical composition of claim 13, in a form for oral administration.

16. The pharmaceutical composition of claim 15, wherein the composition is in tablet form.

17. The pharmaceutical composition of claim 15, wherein the composition is in capsule form.

18. The pharmaceutical composition of claim 13, wherein the composition is a liquid.

19. The pharmaceutical composition of claim 13, in a form for intravenous administration.

20. The pharmaceutical composition of claim 19, wherein the carrier comprises a sterile diluent for injection.

21. The pharmaceutical composition of claim 13, in a form for topical administration.

22. The pharmaceutical composition of claim 14, in a form for oral administration.

23. The pharmaceutical composition of claim 22, wherein the composition is in tablet form.

24. The pharmaceutical composition of claim 22, wherein the composition is in capsule form.

25. The pharmaceutical composition of claim 14, wherein the composition is a liquid.

26. The pharmaceutical composition of claim 14, in a form for intravenous administration.

27. The pharmaceutical composition of claim 17, wherein the carrier comprises a sterile diluent for injection.

28. The pharmaceutical composition of claim 14, in a form for topical administration.
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