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

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

Document Type and Number:

WIPO Patent Application WO/2018/170724

Kind Code:

A1

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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Inventors:

SHENG XIAOHONG (CN)
SHENG XIAOXIA (CN)
WANG JING (CN)

Application Number:

PCT/CN2017/077459

Publication Date:

September 27, 2018

Filing Date:

March 21, 2017

Export Citation:

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Assignee:

SOLIPHARMA LLC (CN)

International Classes:

A61K31/47; A61K9/02; A61K9/06; A61K9/08; A61K9/12; A61K9/14; A61K9/20; A61K9/48; A61K31/16; A61K31/185; A61P11/00; A61P35/00

Domestic Patent References:

WO2014072517A1	2014-05-15
WO2016123573A1	2016-08-04

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