![Cocrystal of 2-(6-methyl-pyridine-2-yl)-3-yl-[6-amide-quinoline-4-yl]-5,6-dihydro-4H-pyrrole[1,2-b]pyrazole, preparation method therefor, and pharmaceutical composition](/docs/US/2021-05-04/US10995083B2/abs.jpg.600x600.jpg)
- Patent Title: Cocrystal of 2-(6-methyl-pyridine-2-yl)-3-yl-[6-amide-quinoline-4-yl]-5,6-dihydro-4H-pyrrole[1,2-b]pyrazole, preparation method therefor, and pharmaceutical composition
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Application No.: US16496023Application Date: 2017-03-21
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Publication No.: US10995083B2Publication Date: 2021-05-04
- Inventor: Xiaohong Sheng , Xiaoxia Sheng , Jing Wang
- Applicant: Hangzhou SoliPharma Co., Ltd.
- Applicant Address: CN Zhejiang
- Assignee: Hangzhou SoliPharma Co., Ltd.
- Current Assignee: Hangzhou SoliPharma Co., Ltd.
- Current Assignee Address: CN Zhejiang
- Agency: Sterne, Kessler, Goldstein & Fox P.L.L.C.
- International Application: PCT/CN2017/077459 WO 20170321
- International Announcement: WO2018/170724 WO 20180927
- Main IPC: C07D401/14
- IPC: C07D401/14
![Cocrystal of 2-(6-methyl-pyridine-2-yl)-3-yl-[6-amide-quinoline-4-yl]-5,6-dihydro-4H-pyrrole[1,2-b]pyrazole, preparation method therefor, and pharmaceutical composition](/abs-image/US/2021/05/04/US10995083B2/abs.jpg.150x150.jpg)
Abstract:
The present invention relates to a cocrystal of 2-(6-methyl-pyridine-2-yl)-3-yl-[6-amide-quinoline-4-yl]-5,6-dihydro-4H-pyrrole[1,2-b]pyrazole (Galunisertib or LY2157299) represented by formula (I) and a cocrystal former. Compared with the known solid form of Galunisertib, the cocrystal of the present invention has advantages in terms of stability, solubility, etc. The present invention also relates to a crystal form of the cocrystal, a preparation method therefor, a pharmaceutical composition thereof, and an application thereof in preparation of drugs for preventing and/or treating diseases relevant to TGF-β.
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