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Claims for Patent: 5,905,082

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Claims for Patent: 5,905,082

Title: Crystalline oxathiolane derivatives
Abstract:(-)cis-4-Amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(IH)-pyrimidine-2-on e in crystalline form, in particular as needle-shaped or bypyramidyl crystals, pharmaceutical formulations thereof, methods for their preparation and their use in medicine.
Inventor(s): Roberts; Tony Gordon (Ware, GB), Evans; Paul (Ware, GB)
Assignee: Glaxo Group Limited (Greenford, GB)
Application Number:07/892,029
Patent Claims: 1. A pharmaceutical formulation in solid dosage unit form comprising an effective amount of (-)-cis-4-amino-1-(2-hydroxymethyl)-1,3-oxathiolan-5-yl)-(1H)pyrimidine-2- one in bipyramidal crystalline form and a pharmaceutically acceptable carrier therefor.

2. A pharmaceutical formulation as claimed in claim 1 in the form of a tablet or capsule.

3. (-)-cis-4-Amino- 1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one in the form of bipyramidyl crystals.

4. The crystalline form as claimed in claim 3 having a melting point of greater than 170.degree. C.

5. The crystalline form as claimed in claim 3, having a melting point of 177-178.degree. C.

6. The crystalline form as claimed in claim 3 having absorption bands in its infra-red spectrum of 920 and 850 wave numbers.

7. The crystalline form as claimed in claim 3 having no absorption band in its infra-red spectrum at 1110 wave numbers.

8. The crystalline form as claimed in 3 having an endotherm with an onset temperature at 177-178.degree. C. in its differential scanning calorimetry profile.

9. A pharmaceutical composition in solid dosage unit form consisting essentially of a therapeutically effective amount (-)-cis-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-o ne in bipyramidyl crystalline form in combination with a pharmaceutically acceptable carrier therefor.

10. A pharmaceutical composition in solid dosage unit form comprising a therapeutically effective amount of (-)-cis-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(IH)-pyrimidin-2-o ne in bipyramidal crystalline form in combination with a pharmaceutically acceptable carrier therefor.

11. A pharmaceutical composition according to claim 10 where in the (-)-cis-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(IH)-pyrimidin-2-o ne in bipyramidal crystalline form is substantially free of non-crystalline (-)-cis-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(IH)-pyrimidin-2-o ne.

12. A pharmaceutical composition according to claim 10 wherein the (-)-cis-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(IH)-pyrimidin-2-o ne in bipyramidal crystalline is substantially free of needle crystals of (-)-cis-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(IH)-pyrimidin-2-o ne.

13. A pharmaceutical composition according to claim 10 in oral administration form.

14. A pharmaceutical composition useful for treating HIV infections in humans which comprises a therapeutically effective amount of a combination of 3'-azido-3'-deoxythymidine (AZT) and (-)-cis-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-IH-pyrimidin-2-one in bipyramidal crystalline form, in combination with a pharmaceutically acceptable carrier.

15. A pharmaceutical composition useful for treating HIV infections in humans which comprises a therapeutically effective amount of a combination of 3'-azido-3'-deoxythymidine (AZT) and (-)-cis-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-IH-pyrimidin-2-one in bipyramidal crystalline form substantially free of non-crystalline (-)-cis-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5yl)-(IH)-pyrimidin-2-on e, in combination with a pharmaceutically acceptable carrier.

16. A pharmaceutical composition useful for treating HIV infections in humans which comprises a therapeutically effective amount of a combination of 3'-azido-3'-deoxythymidine (AZT) and (-)-cis-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-1H-pyrimidin-1-one in bipyramidal crystalline form substantially free of needle crystals, in combination with a pharmaceutically acceptable carrier.

17. A pharmaceutical composition according to claim 14 in oral administration form.

18. A pharmaceutical composition according to claim 17 in tablet form.

19. A pharmaceutical composition according to claim 17 in capsule form.

20. A method of treating HIV infections in humans which comprises administering to a human in need thereof a therapeutically effective amount of 3'-azido-3'-deoxythymidine (AZT) and (-)-cis-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5yl)-IH-pyrimidin-2-one in bipyramidal crystalline form, in combination with a pharmaceutically acceptable carrier.

21. A method of treating HIV infections in humans which comprises administering to a human in need thereof a therapeutically effective amount of 3'-azido-3'-deoxythymidine (AZT) and (-)-cis-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5yl)-IH-pyrimidin-2-one in bipyramidal crystalline form substantially free of non-crystalline (-)-cis-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5yl)-IH-pyrimidin-2-one, in combination with a pharmaceutically acceptable carrier.

22. A method of treating HIV infections in humans which comprises administering to a human in need thereof a therapeutically effective amount of 3'-azido-3'-deoxythymidine (AZT) and (-)-cis-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5yl)-IH-pyrimidin-2-one in bipyramidal crystalline form substantially free of needle crystals of (-)-cis-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5yl)-IH-pyrimidin-2-one, in combination with a pharmaceutically acceptable carrier.

23. A method according to claim 20 wherein the administration is sequential.

24. A method according to claim 20 wherein the administration is simultaneous.

25. A method according to claim 20 wherein the administration is oral.

26. A method according to claim 25 wherein the oral administration is in tablet form.

27. A method according to claim 25 wherein the oral administration is in capsule form.
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