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Details for Patent: 8,629,173

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Details for Patent: 8,629,173

Title:Solid forms comprising (+)-2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoi- soindoline-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 18, 2011
Application Number:13/300,458
Claims:1. A method of treating psoriasis, which comprises orally administering to a patient having psoriasis about 20 mg twice daily of an unsolvated crystal form of the compound of Formula (I): ##STR00002## which is enantiomerically pure, wherein the crystal form is Form A or Form F; and wherein the patient achieves at least about a 50% reduction in Psoriasis Area and Severity Index score compared to baseline.

2. The method of claim 1, wherein the psoriasis is moderate to severe plaque-type psoriasis.

3. The method of claim 1, wherein the patient achieves at least about a 75% reduction in Psoriasis Area and Severity Index score compared to baseline.

4. The method of claim 1, wherein the patient achieves at least about a 90% reduction in Psoriasis Area and Severity Index score compared to baseline.

5. The method of claim 1, wherein the crystal form is administered in the form of a tablet or capsule.

6. The method 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..

7. The method 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..

8. The method 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.

9. The method 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.

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

11. The method 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.

12. The method of claim 11, wherein the mass loss is about 0.05%.

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

14. The method 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.

15. The method of claim 14, wherein the mass increase is about 0.4%.

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

17. The method 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.

18. The method 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..

19. The method 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..

20. The method 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.

21. The method 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.

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

23. The method 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.

24. The method of claim 23, wherein the mass loss is about 0.1%.

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

26. The method 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.

27. The method of claim 26, wherein the mass increase is about 0.2%.

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

29. The method 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.

30. The method of claim 5, wherein the crystal form is administered in the form of a capsule.

31. The method of claim 30, wherein the capsule contains about 10 mg of the compound.

32. The method of claim 30, wherein the capsule contains about 20 mg of the compound.

33. The method of claim 30, wherein the capsule contains about 25 mg of the compound.

34. The method of claim 30, wherein the capsule contains about 50 mg of the compound.

35. The method of claim 5, wherein the crystal form is administered in the form of a tablet.

36. The method of claim 35, wherein the tablet contains about 10 mg of the compound.

37. The method of claim 35, wherein the tablet contains about 20 mg of the compound.

38. The method of claim 35, wherein the tablet contains about 25 mg of the compound.

39. The method of claim 35, wherein the tablet contains about 50 mg of the compound.
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