Crystalline and non-crystalline forms of tofacitinib, and a pharmaceutical composition comprising tofacitinib and a penetration enhancer

A composition and form technology for drug combination, drug delivery, non-central analgesics, etc., capable of solving problems such as unpredictable, daunting results
CN103459394AInactive Publication Date: 2013-12-18PFIZER INC

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

The present invention discloses novel crystalline and non-crystalline forms of 3-((3R, 4R)-4-methyl-3-[methyl-(7H-pyrrolo[2, 3-d]pyrimidin-4-yl)-amino]-piperidin-1-yl)-3-oxopropionitrile, pharmaceutical composition containing the same, preparations thereof and the uses thereof.
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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...

Claims

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