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Details for Patent: 8,563,530

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Details for Patent: 8,563,530

Title:Purine nucleoside phosphoramidate
Abstract: Disclosed herein is a compound represented by formula 1 or its hydrate thereof in crystalline or crystal-like form. ##STR00001##
Inventor(s): Chang; Wonsuk (Princeton, NJ), Naduthambi; Devan (Plainsboro, NJ), Nagarathnam; Dhanapalan (Bethany, CT), Pamulapati; Ganapati Reddy (Plainsboro, NJ), Ross; Bruce S. (Plainsboro, NJ), Sofia; Michael Joseph (Doylestown, PA), Zhang; Hai-Ren (Ellicott City, MD)
Assignee: Gilead Pharmassel LLC (Foster City, CA)
Filing Date:Mar 31, 2011
Application Number:13/076,718
Claims:1. A compound represented by formula 1, its hydrate or solvate thereof in crystalline or crystal-like form. ##STR00021##

2. The compound of claim 1, represented by 1.mH.sub.2O, wherein m varies in an integer or non-integer amount from about 0 to about 5 and is not 0.

3. The compound of claim 2, wherein m is about 1.

4. The compound of claim 2, wherein m is about 1/2.

5. The compound of claim 2, wherein m is about 1, that further comprises an amount of adsorbed water.

6. The compound of claim 5, wherein the amount of adsorbed water ranges from about 0 wt. % to about 10 wt. % based on the weight of the 1.H.sub.2O.

7. The compound of claim 2, wherein the compound is a monohydrate in crystalline form.

8. The compound of claim 7 having an XRPD 2.theta.-reflection (.degree.) at about 14.8.

9. The compound of claim 8 having XRPD 2.theta.-reflections (.degree.) at about 14.8 and about 17.6.

10. The compound of claim 9 having XRPD 2.theta.-reflections (.degree.) at about 20.4.

11. The compound of claim 9 having XRPD 2.theta.-reflections (.degree.) at about 8.7.

12. The compound of claim 9 having XRPD 2.theta.-reflections (.degree.) at about 13.6.

13. The compound of claim 9 having XRPD 2.theta.-reflections (.degree.) at about.

14. The compound of claim 9 having a pattern substantially as that shown in FIG. 1.

15. The compound of claim 7, wherein the compound is an orthorhombic crystalline.

16. The orthorhombic crystalline of claim 15, having the following unit cell parameters a.about.10.99 .ANG., b.about.13.09 .ANG., and c.about.20.36 .ANG..

17. A composition comprising the compound of claim 1.

18. A method for treating HCV in a patient in need thereof, which comprises administering to the patient a therapeutically effective amount of the compound of claim 1.

19. A method for treating HCV in a patient in need thereof, which comprises administering to the patient a therapeutically effective amount of the compound of claim 7.

20. A method for treating HCV in a patient in need thereof, which comprises administering to the patient a therapeutically effective amount of the compound of claim 1 in combination or in alternation with a therapeutically effective amount of another antiviral.

21. The method of claim 20, wherein the other antiviral is selected from the group consisting of ##STR00022## telaprevir; boceprevir; BMS-790052; ITMN-191; ANA-598; TMC435; and combinations thereof.

22. A co-therapy method for treating HCV in a patient in need thereof, which comprises administering to the patient a therapeutically effective amount of the compound of claim 7 in combination or in alternation with a therapeutically effective amount of another antiviral.

23. The co-therapy method of claim 22, wherein the other antiviral is selected from the group consisting of ##STR00023## telaprevir; boceprevir; BMS-790052; ITMN-191; ANA-598; TMC435; and combinations thereof.

24. A process for preparing the compound of claim 1 in a crystalline form, which comprises crystallizing the compound of claim 1.

25. The process of claim 24, which further comprises dissolving or suspending the compound of claim 1 in a solvent or solvent mixture.

26. The process of claim 25, wherein the solvent or solvent mixture is selected from the group consisting of anisole, ethyl acetate; xylenes; toluene; isopropanol; acetone; dichloromethane; diethyl ether; isopropyl acetate; t-butyl methyl ether; and combinations thereof.

27. The process of claim 25, wherein the solvent mixture is selected from the group consisting of anisole/ethyl acetate; heptanes/ethyl acetate; xylenes/ethyl acetate/water; anisole/water; ethyl acetate/xylenes; isopropanol/xylenes; acetone/xylenes; dichloromethane/xylenes; dichloromethane/hexanes; ethyl acetate/toluene; diethyl ether/xylenes; isopropyl acetate/xylenes; isopropyl acetate/heptanes; ethyl acetate/water; t-butyl methyl ether/water; and t-butyl methyl ether/ethyl ether.

28. A method for determining the crystallinity of the compound of claim 1, which comprises analyzing the compound by XRPD or single-crystal X-ray crystallography.
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