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专利概况
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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