- 专利标题: PYRIDINE SUBSTITUTED 2-AMINOPYRIDINE PROTEIN KINASE INHIBITOR CRYSTAL
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申请号: EP16829879.2申请日: 2016-07-29
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公开(公告)号: EP3330264A1公开(公告)日: 2018-06-06
- 发明人: GONG, Feng , LI, Xinlu , ZHAO, Rui , ZHANG, Xiquan , XU, Xinhe , LIU, Xijie , XIAO, Dengming , HAN, Yongxin
- 申请人: Chia Tai Tianqing Pharmaceutical Group Co.,Ltd , Lianyungang Runzhong Pharmaceutical Co., Ltd. , Centaurus BioPharma Co., Ltd.
- 申请人地址: No. 369 Yuzhou South Road Haizhou District Lianyungang, Jiangsu 222062 CN
- 专利权人: Chia Tai Tianqing Pharmaceutical Group Co.,Ltd,Lianyungang Runzhong Pharmaceutical Co., Ltd.,Centaurus BioPharma Co., Ltd.
- 当前专利权人: Chia Tai Tianqing Pharmaceutical Group Co.,Ltd,Lianyungang Runzhong Pharmaceutical Co., Ltd.,Centaurus BioPharma Co., Ltd.
- 当前专利权人地址: No. 369 Yuzhou South Road Haizhou District Lianyungang, Jiangsu 222062 CN
- 代理机构: Greiner, Elisabeth
- 优先权: CN201510458524 20150730
- 国际公布: WO2017016514 20170202
- 主分类号: C07D401/14
- IPC分类号: C07D401/14 ; A61K31/496 ; A61P35/00
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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