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Details for Patent: 8,093,283

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Details for Patent: 8,093,283

Title:Solid forms comprising (+)-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisi- noline-1,3-dione, compositions thereof, and uses thereof
Abstract: Solid forms comprising (+)-2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoi- soindoline-1,3-dione, compositions comprising the solid forms, methods of making the solid forms and methods of their use are disclosed. The methods include methods of treating and/or preventing disorders ameliorated by the reduction of levels of TNF-.alpha. or the inhibition of PDE4.
Inventor(s): Muller; George W. (Bridgewater, NJ), Schafer; Peter H. (Somerset, NJ), Man; Hon-Wah (Princeton, NJ), Ge; Chuansheng (Belle Mead, NJ), Xu; Jean (Warren, NJ)
Assignee: Celgene Corporation (Summit, NJ)
Filing Date:Nov 12, 2010
Application Number:12/945,800
Claims:1. An unsolvated crystal form of the compound of Formula (I): ##STR00002## which is enantiomerically pure, wherein the crystal form is Form A, which has an X-ray powder diffraction pattern comprising peaks at about 8.1, 14.4, 17.4, 23.6 and 25.1 degrees 2.theta., or Form F, which has an X-ray powder diffraction pattern comprising peaks at about 8.1, 15.6, 17.3, and 25.4 degrees 2.theta..

2. The crystal form of claim 1, wherein the crystal form is Form A, which has an X-ray powder diffraction pattern comprising peaks at about 8.1, 14.4, 17.4, 23.6 and 25.1 degrees 2.theta..

3. The crystal form of claim 1, wherein the crystal form is Form A, which has an X-ray powder diffraction pattern comprising peaks at about 8.1, 14.4, 15.2, 17.4, 18.4, 19.2, 20.5, 22.8, 23.2, 23.6, 24.5 and 25.1 degrees 2.theta..

4. The crystal form of claim 1, wherein the crystal form is Form A, which has an X-ray powder diffraction pattern matching the pattern depicted in FIG. 1.

5. The crystal form of claim 1, wherein the crystal form is Form A, which has a differential scanning calorimetry plot comprising an endothermic event with an onset temperature of about 155.degree. C.

6. The crystal form of claim 1, wherein the crystal form is Form A, which has a differential scanning calorimetry plot matching the plot depicted in FIG. 2.

7. The crystal form of claim 1, wherein the crystal form is Form A, which has a thermal gravimetric analysis plot comprising a mass loss of less than about 1% when heated from about 25.degree. C. to about 140.degree. C.

8. The crystal form of claim 7, wherein the mass loss is about 0.05%.

9. The crystal form of claim 1, wherein the crystal form is Form A, which has a thermal gravimetric analysis plot matching the plot depicted in FIG. 3.

10. The crystal form of claim 1, wherein the crystal form is Form A, which exhibits a mass increase of less than about 1% when subjected to an increase in relative humidity from about 0% to about 95% relative humidity.

11. The crystal form of claim 10, wherein the mass increase is about 0.4%.

12. The crystal form of claim 1, wherein the crystal form is Form A, which has a moisture sorption isotherm plot matching the plot depicted in FIG. 4.

13. The crystal form of claim 1, wherein the crystal form is Form A, which is stable upon exposure to about 40.degree. C. and about 75% relative humidity for about 4 weeks.

14. The crystal form of claim 1, wherein the crystal form is Form F, which has an X-ray powder diffraction pattern comprising peaks at about 8.1, 15.6, 17.3 and 25.4 degrees 2.theta..

15. The crystal form of claim 1, wherein the crystal form is Form F, which has an X-ray powder diffraction pattern comprising peaks at about 8.1, 8.6, 15.6, 17.3, 19.3, 21.4, 22.8, 24.6, 25.4, 25.9, 26.6 and 27.7 degrees 2.theta..

16. The crystal form of claim 1, wherein the crystal form is Form F, which has an X-ray powder diffraction pattern matching the pattern depicted in FIG. 21.

17. The crystal form of claim 1, wherein the crystal form is Form F, which has a differential scanning calorimetry plot comprising an endothermic event with an onset temperature of about 145.degree. C.

18. The crystal form of claim 1, wherein the crystal form is Form F, which has a differential scanning calorimetry plot matching the plot depicted in FIG. 22.

19. The crystal form of claim 1, wherein the crystal form is Form F, which has a thermal gravimetric analysis plot comprising a mass loss of less than about 1% when heated from about 25.degree. C. to about 180.degree. C.

20. The crystal form of claim 19, wherein the mass loss is about 0.1%.

21. The crystal form of claim 1, wherein the crystal form is Form F, which has a thermal gravimetric analysis plot matching the plot depicted in FIG. 23.

22. The crystal form of claim 1, wherein the crystal form is Form F, which exhibits a mass increase of less than about 1% when subjected to an increase in relative humidity from about 0% to about 95% relative humidity.

23. The crystal form of claim 22, wherein the mass increase is about 0.2%.

24. The crystal form of claim 1, wherein the crystal form is Form F, which has a moisture sorption isotherm plot matching the plot depicted in FIG. 24.

25. The crystal form of claim 1, wherein the crystal form is Form F, which is stable upon exposure to about 40.degree. C. and about 75% relative humidity for about 4 weeks.

26. The crystal form of claim 1, which is substantially pure.

27. A solid pharmaceutical composition comprising the crystal form of claim 2.

28. The crystal form of claim 1, which is anhydrous.

29. The crystal form of claim 1, which contains less than about 10 percent by weight of one or more other solid forms or other chemical compounds.

30. The crystal form of claim 1, which contains less than about 5 percent by weight of one or more other solid forms or other chemical compounds.

31. A pharmaceutical composition suitable for oral administration, comprising about 1 mg to about 200 mg of the crystal form of claim 1.

32. The pharmaceutical composition of claim 31, wherein the pharmaceutical composition comprises about 10 mg to about 100 mg of the crystal form.

33. The pharmaceutical composition of claim 31, wherein the pharmaceutical composition is in capsule form.

34. The pharmaceutical composition of claim 33, wherein the capsule contains about 10 mg of the compound.

35. The pharmaceutical composition of claim 33, wherein the capsule contains about 20 mg of the compound.

36. The pharmaceutical composition of claim 33, wherein the capsule contains about 25 mg of the compound.

37. The pharmaceutical composition of claim 33, wherein the capsule contains about 50 mg of the compound.

38. The pharmaceutical composition of claim 31, wherein the pharmaceutical composition is in tablet form.

39. The pharmaceutical composition of claim 38, wherein the tablet contains about 10 mg of the compound.

40. The pharmaceutical composition of claim 38, wherein the tablet contains about 20 mg of the compound.

41. The pharmaceutical composition of claim 38, wherein the tablet contains about 25 mg of the compound.

42. The pharmaceutical composition of claim 38, wherein the tablet contains about 50 mg of the compound.
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