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1.发明授权
公开(公告)号：EP2881395B1
公开(公告)日：2018-09-05
申请号：EP13825341.4
申请日：2013-07-24
申请人： Shanghai Institute of Materia Medica, Chinese Academy of Sciences , Shanghai Acebright Pharmaceuticals Co., Ltd.
发明人： ZHANG, Ao , MIAO, Zehong , YE, Na , HUAN, Xiajuan , SONG, Zilan , CHEN, Chuanhuizi , CHEN, Yi , DING, Jian
IPC分类号： C07D487/04 , A61K31/4985 , A61K31/501 , A61K31/502 , A61P9/10 , A61P25/28 , A61P35/00
CPC分类号： C07D487/04 , A61K31/4985 , A61K31/501 , A61K31/502
摘要： Provided is a piperazinotriazole compound represented by general formula I or an isomer, a pharmaceutically acceptable salt, ester, prodrug or hydrate thereof. Also provided are a method for preparing the compound, a drug composition containing the compound, and a use thereof as a high-selectivity poly(ADP-ribose)polymerase-1 (PARP 1) inhibitor in the preparation of drugs for the prevention and / or treatment of PARP-related diseases.
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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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4.发明公开
公开(公告)号：EP3381919A1
公开(公告)日：2018-10-03
申请号：EP16867946.2
申请日：2016-11-22
发明人： ZHANG, Ao , MIAO, Zehong , WANG, Pingyuan , SONG, Shanshan , SONG, Zilan , HUAN, Xiajuan , FAN, Zhoulong , DING, Jian
IPC分类号： C07D487/04 , C07D471/04 , A61K31/502 , A61K31/437 , A61K31/444 , A61P25/28 , A61P25/16 , A61P9/10 , A61P27/02 , A61P35/00
CPC分类号： C07D487/04 , A61K31/437 , A61K31/444 , A61K31/502 , A61P35/00 , C07D471/04
摘要： The present invention relates to a class of substituted triazolopiperazine compounds represented by formula ( I ), tautomers, enantiomers, diastereomers, racemates, metabolites, metabolic precursors, and pharmaceutically acceptable salts, esters, prodrugs or hydrate thereof, a preparation methods therefor, intermediates and a use thereof in the preparation of drugs for prevention and treatment of diseases associated with PARP including various ischemic diseases, neurodegenerative diseases and cancers.
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5.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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6.发明公开
公开(公告)号：EP3418277A1
公开(公告)日：2018-12-26
申请号：EP17752701.7
申请日：2017-02-17
发明人： ZHANG, Ao , GENG, Meiyu , XING, Li , AI, Jing , SONG, Zilan , PENG, Xia , GU, Wangting , DING, Jian
IPC分类号： C07D401/12 , C07D213/75 , C07D413/12 , C07D417/12 , C07D403/12 , C07D405/12 , A61K31/4427 , A61K31/44 , A61K31/4439 , A61K31/4545 , A61P35/00
CPC分类号： A61K31/44 , A61K31/4427 , A61K31/4439 , A61K31/4545 , C07D213/75 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12
摘要： Provided in the present invention are a substituted amino six-membered nitric heterocyclic ring compound and a preparation and use thereof. In particular, provided in the present invention is a compound as shown by general formula (I) below, wherein the definition of each group is as described in the description. The compound of the present invention has an excellent tyrosine kinase inhibitory activity, and can thus be used to prepare a series of medicines for treating diseases related to tyrosine kinase inhibitory activity.
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7.发明公开PIPERAZINOTRIZOLE COMPOUND, PREPARATION METHOD THEREFOR, AND USE THEREOF IN DRUG PREPARATION 审中-公开PIPERAZINOTRIZOLVERBINDUNG，生产方法和它们用于药品的生产
公开(公告)号：EP2881395A1
公开(公告)日：2015-06-10
申请号：EP13825341.4
申请日：2013-07-24
发明人： ZHANG, Ao , MIAO, Zehong , YE, Na , HUAN, Xiajuan , SONG, Zilan , CHEN, Chuanhuizi , CHEN, Yi , DING, Jian
IPC分类号： C07D487/04 , A61K31/4985 , A61K31/501 , A61K31/502 , A61P9/10 , A61P25/28 , A61P35/00
CPC分类号： C07D487/04 , A61K31/4985 , A61K31/501 , A61K31/502
摘要： Provided is a piperazinotriazole compound represented by general formula I or an isomer, a pharmaceutically acceptable salt, ester, prodrug or hydrate thereof. Also provided are a method for preparing the compound, a drug composition containing the compound, and a use thereof as a high-selectivity poly(ADP-ribose)polymerase-1 (PARP 1) inhibitor in the preparation of drugs for the prevention and / or treatment of PARP-related diseases.
摘要翻译： 本发明提供一种由通式表示的异构体，药学上可接受的盐，酯，前药或水合物的I或其化合物piperazinotriazole。 这样提供了用于制备所述化合物，药物组合物含有该化合物，并且作为高选择性的聚（ADP-核糖）在制备药物用于预防聚合酶-1（PARP 1）抑制剂及其使用的方法和/ 或治疗的PARP有关的疾病。
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