Details for Patent: 8,822,499

Title:	Polymorphic forms of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione
Abstract:	Polymorphic forms of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione are disclosed. Compositions comprising the polymorphic forms, methods of making the polymorphic forms and methods of their use are also disclosed.
Inventor(s):	Jaworsky; Markian S. (Hopewell, NJ), Chen; Roger Shen-Chu (Edison, NJ), Muller; George W. (Rancho Santa Fe, CA), Saindane; Manohar T. (Monmouth Junction, NJ), Cameron; Louise M. (East Windsor, NJ)
Assignee:	Celgene Corporation (Summit, NJ)
Filing Date:	Sep 22, 2011
Application Number:	13/240,686
Claims:	1. A polymorphic mixture of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione comprising crystalline 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione dihydrate, wherein the crystalline 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione dihydrate is present at greater than about 97% by weight of the polymorphic mixture. 2. A polymorphic mixture of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione comprising crystalline 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione dihydrate, wherein the crystalline 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione dihydrate is present at greater than about 95% by weight of the polymorphic mixture. 3. A polymorphic mixture of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione comprising crystalline 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione dihydrate, wherein the crystalline 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione dihydrate is present at greater than about 90% by weight of the polymorphic mixture. 4. A polymorphic mixture of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione comprising crystalline 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione dihydrate, wherein the crystalline 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione dihydrate is present at greater than about 80% by weight of the polymorphic mixture. 5. The polymorphic mixture of any one of claims 1, 2, 3, and 4, wherein the dihydrate has an X-ray powder diffraction pattern comprising peaks at approximately 20, 24.5 and 29 degrees 2.theta.. 6. The polymorphic mixture of any one of claims 1, 2, 3, and 4, wherein the dihydrate has an X-ray powder diffraction pattern comprising peaks at 20.0, 24.7 and 28.6 degrees 2.theta.. 7. The polymorphic mixture of any one of claims 1, 2, 3, and 4, wherein the dihydrate loses about 12% by weight when heated from about 30.degree. C. to about 175.degree. C. 8. A pharmaceutical composition comprising the polymorphic mixture of any one of claims 1, 2, 3, and 4, and a pharmaceutically acceptable excipient, diluent, or carrier. 9. The pharmaceutical composition of claim 8, which is a capsule. 10. The pharmaceutical composition of claim 8, which is a tablet. 11. The pharmaceutical composition of claim 8, wherein the dihydrate is present in an amount of about 5 mg, about 10 mg, about 25 mg, or about 50 mg. 12. The pharmaceutical composition of claim 8, wherein the dihydrate is present in an amount of from about 0.1 mg to about 150 mg.