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
US11111248B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Mar 17, 2017 |
| Grant date | Sep 7, 2021 |
| Priority date | — |
| Expiry date | Mar 17, 2037 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07B2200/13
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
The present invention relates to a crystal form of 2-(6-methyl-pyridin-2-yl)-3-(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 of preparing the crystal forms 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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.