Crystalline and non-crystalline forms of tofacitinib, and a pharmaceutical composition comprising tofacitinib and a penetration enhancer
Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- PFIZER INC
- Publication Date
- 2013-12-18
- Estimated Expiration
- Not applicable · inactive patent
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Abstract
Description
【Technical field】
[0001] The present invention relates to 3-((3R,4R)-4-methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino in crystalline or non-crystalline form ]-piperidin-1-yl)-3-oxopropionitrile. The invention also relates to pharmaceutical compositions comprising crystalline or non-crystalline forms, and methods of preparing such forms. The invention further relates to the use of crystalline or non-crystalline forms for topical treatment of various diseases. 【Background technique】
[0002] 3-((3R,4R)-4-Methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]-piperidin-1-yl)- 3-oxopropionitrile has the formula C 16 h 20 N 6 O and the following structural formula:
[0003]
[0004] 3-((3R,4R)-4-Methyl-3-[methyl-(7H-pyrrolo[2,3-d]-pyrimidin-4-yl)-amino]-piperidin-1-yl) - The synthesis of 3-oxopropionitrile is described in WO 2001 / 42246 and WO 2002 / 096909, commonly assigned to the assignee of the present invention and incorporated herein by reference in thei...