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1.发明授权
公开(公告)号：EP3546460B1
公开(公告)日：2020-07-08
申请号：EP17874613.7
申请日：2017-11-24
发明人： ZHANG, Ao , DING, Jian , XIE, Hua , SONG, Zilan , XUE, Yu , TONG, Linjiang , GENG, Meiyu
IPC分类号： C07D471/14 , C07D487/14 , A61K31/519 , A61P35/00 , A61P35/02 , A61P29/00 , A61P37/02
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2.发明公开
公开(公告)号：EP3546460A1
公开(公告)日：2019-10-02
申请号：EP17874613.7
申请日：2017-11-24
发明人： ZHANG, Ao , DING, Jian , XIE, Hua , SONG, Zilan , XUE, Yu , TONG, Linjiang , GENG, Meiyu
IPC分类号： C07D471/14 , C07D487/14 , A61K31/519 , A61P35/00 , A61P35/02 , A61P29/00 , A61P37/02
摘要： The present invention relates to a Pyrimido[5,4- b ]indolizine or pyrimido[5,4- b ] pyrrolizine compound, preparation method thereof and use thereof. The compounds of the present invention have good inhibitory activities against BTK at the molecular and cellular levels. Importantly, the compounds of the present invention have low activity against Ramos cells of normal human B lymphoma cells, and have high activity against BTK-sensitive human diffuse large B lymphoma TMD8 cells, indicating that these type of compounds with novel structural are highly selective, off-target phenomenon and corresponding side effects are low. Thus it is a selective inhibitor of BTK with development potential.
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3.发明公开
公开(公告)号：EP3960743A1
公开(公告)日：2022-03-02
申请号：EP20794381.2
申请日：2020-04-24
发明人： ZHANG, Ao , DING, Jian , XIE, Hua , SONG, Zilan , XUE, Yu , XING, Li , TONG, Linjiang , GENG, Meiyu
IPC分类号： C07D471/14 , C07D487/14 , A61K31/519 , A61P35/00 , A61P35/02 , A61P29/00 , A61P37/02
摘要： The present invention relates to a pyrimido[5,4-b]pyrrolizin compound represented by general formula I, an optical isomer thereof, a preparation method therefor, a pharmaceutical composition containing same, and a use thereof. The compound according to the present invention has good inhibitory activity on the kinase BTK at both the molecular level and the cellular level. Meanwhile, the compound also has good anti-tumor activity and pharmacokinetic properties in vivo.
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