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Title:
CRYSTAL FORM OF 2-(6-METHYL-PYRIDIN-2-YL)-3-YL-[6-AMIDO-QUINOLIN-4-YL]-5,6-DIHYDRO-4H-PYRROLO[1,2-B]PYRAZOLE, PREPARATION METHOD THEREFOR AND PHARMACEUTICAL COMPOSITION THEREOF
Document Type and Number:
WIPO Patent Application WO/2018/165979
Kind Code:
A1
Abstract:
The present invention relates to a crystal form of 2-(6-methyl-pyridin-2-yl)-3-yl-[6-amido-quinolin-4-yl]-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole (Galunisertib or LY2157299) represented by formula (I). Compared with the known solid form of Galunisertib, the crystal form of the present invention has advantages in terms of solubility, hygroscopicity, crystal stability, morphology, and the like. The present invention also relates to a process for preparing the crystal form of Galunisertib, a pharmaceutical composition thereof and a use thereof in the preparation of a medicament for the prevention and/or treatment of diseases associated with TGF-beta.

Inventors:
SHENG XIAOHONG (CN)
SHENG XIAOXIA (CN)
WANG JING (CN)
Application Number:
PCT/CN2017/077081
Publication Date:
September 20, 2018
Filing Date:
March 17, 2017
Export Citation:
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Assignee:
SOLIPHARMA LLC (CN)
International Classes:
C07D487/04; A61K31/4162; A61K31/4709; A61P35/00
Foreign References:
CN1714090A2005-12-28
US7872020B22011-01-18
CN102711799A2012-10-03
Other References:
JEFFRY K. NIEMEIER*ROGER R. ROTHHAAR*JEFFREY T. VICENZIJOHN A. WERNER: "Application of Kinetic Modeling and Competitive Solvent Hydrolysis in the Development of a Highly Selective Hydrolysis of a Nitrile to an Amide", ORGANIC PROCESS RESEARCH & DEVELOPMENT, vol. 18, no. 3, 11 February 2014 (2014-02-11), pages 410 - 416, XP055450253, DOI: 10.1021/op4003054
CHENG HUA, JIN ET AL.: "Synthesis and biological evaluation of 1-substituted-3(5)-(6-methylpyridin-2-yl)-4-(quinolin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors", BIOORGANIC & MEDICINAL CHEMISTRY, vol. 19, no. 8, 15 April 2011 (2011-04-15), pages 2633 - 2640, XP002794438, DOI: 10.1016/j.bmc.2011.03.008
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