Tope-McKay & Associates
Pyridine substituted 2-aminopyridine protein kinase inhibitor crystal
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.
CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD. LIANYUNGANG RUNZHONG PHARMACEUTICAL CO., LTD. CENTAURUS BIOPHARMA CO., LTD.
C A A C
C07D A61P A61K C07B
inventional inventional inventional additional
Xinlu Xinhe Xijie Yongxin Xiquan Feng Dengming Rui
Li Xu Liu Han Zhang Gong Xiao Zhao