Pyridine substituted 2-aminopyridine protein kinase inhibitor crystal
US10385038B2 · kind B2 · utility
Assignees
Inventors
Key dates
| Filing date | Jul 29, 2016 |
| Grant date | Aug 20, 2019 |
| Priority date | — |
| Expiry date | Jul 29, 2036 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07B2200/13
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
The present invention discloses a crystal of citrate salt of pyridine-substituted 2-aminopyridine-based protein kinase inhibitors, in particular, to crystal of 5-((R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy)-4′-methoxy-6′-((S)-2-methylpiperazin-1-yl)-3,3′-bipyridin-6-amine citrate salt, a method for preparation thereof, a crystalline composition and a pharmaceutical composition comprising the crystal, and further discloses the use of crystals of citrate salt of the compound of Formula I in protein kinase-related diseases. The crystals of citrate salt according to the present invention are superior to 5-((R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy)-4′-methoxy-6′-((S)-2-methylpiperazin-1-yl)-3,3′-bipyridin-6-amine or other salts of 5-((R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy)-4′-methoxy-6′-((S)-2-methylpiperazin-1-yl)-3,3′-bipyridin-6-amine in at least one aspect of bioavailability, hygroscopicity, stability, solubility, purity, ease of preparation, and the like.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.