专利名称 | 2 - Aminopyridine substituted pyridine protein kinase inhibitor for crystal | ||
申请号 | JP2018524523 | 申请日 | |
公开(公告)号 | JP6513294B2 | 公开(公告)日 | |
申请(专利权)人 | CHIA TAI TIANQING PHARMACEUTICAL GROUP CO LTD | 发明人 | ▲ゴン▼ 峰; 李 新路; ▲趙▼ ▲鋭▼; ▲張▼ 喜全; ▲許▼ 新合; ▲劉▼ 希杰; 校 登明; 韓 永信 |
专利来源 | 国家知识产权局 | 转化方式 | |
摘要 |
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. |
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