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公开(公告)号：EP3177626A4
公开(公告)日：2017-12-27
申请号：EP15830298
申请日：2015-08-07
发明人： BRADNER JAMES E , BUCKLEY DENNIS
IPC分类号： C07D487/04 , A61K31/5513 , A61P35/00 , C07D243/06
CPC分类号： C07D487/04
摘要： The present disclosure provides compounds of Formula (I), and pharmaceutically compositions thereof. Compounds of Formula (I) have been found to bind bromodomains and/or bromodomain-containing proteins (e.g., bromo and extra terminal (BET) proteins). Also provided are methods, uses, and kits of the compounds and pharmaceutical compositions for inhibiting the activity (e.g., increased activity) of bromodomains and/or bromodomain-containing proteins and for treating and/or preventing in a subject diseases associated with bromodomains or bromodomain-containing proteins (e.g., proliferative diseases, cardiovascular diseases, viral infections, fibrotic diseases, neurological diseases, metabolic diseases, endocrine diseases, and radiation poisoning). The compounds, pharmaceutical compositions, and kits are also useful for male contraception.
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2.发明公开DIHYDROPTERIDINONE DERIVATIVES AND USES THEREOF 审中-公开DIHYDROPTERIDINDINIVATE UND VERWENDUNGEN DAVON
公开(公告)号：EP3099171A4
公开(公告)日：2017-08-09
申请号：EP15743171
申请日：2015-02-02
发明人： BRADNER JAMES E , GRAY NATHANAEL , QI JUN , MCKEOWN MICHAEL R , BUCKLEY DENNIS
IPC分类号： C07D475/00 , A61K31/4985 , A61K31/519 , A61P3/00 , A61P9/00 , A61P31/12 , C07D471/04
CPC分类号： C07D471/04 , C07D475/00
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公开(公告)号：EP3024327A4
公开(公告)日：2017-03-01
申请号：EP14828728
申请日：2014-07-25
发明人： MARINEAU JASON J , BRADNER JAMES E , ZHANG WEI , QI JUN , MCKEOWN MICHAEL R , FU HARRY HONGNING , LIU SHUAI
IPC分类号： A01N43/02 , A01N43/40 , A01N43/54 , A61K31/519 , A61P35/00 , C07D401/00 , C07D413/10 , C07D471/04 , C07D487/04 , C07D491/048
CPC分类号： C07D487/04 , A61K31/519 , C07D413/10 , C07D471/04 , C07D491/048
摘要： The present invention provides novel compounds of any one of Formulae (I) to (IV), and pharmaceutically compositions thereof. Compounds of any one of Formulae (I) to (IV) are believed to be inhibitors of bromodomain-containing proteins (e.g., bromo and extra terminal proteins (BETs)). Also provided are methods, uses, and kits using the inventive compounds and pharmaceutical compositions for inhibiting the activity of the bromodomain-containing proteins and for treating and/or preventing in a subject in need thereof diseases associated with bromodomain-containing proteins, such as proliferative diseases.
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公开(公告)号：EP3177147A4
公开(公告)日：2018-01-24
申请号：EP15829064
申请日：2015-08-07
发明人： BRADNER JAMES E , BUCKLEY DENNIS
IPC分类号： C07D475/00 , A61K31/517 , A61P15/16 , A61P29/00 , A61P31/12 , A61P35/00
CPC分类号： C07D475/00
摘要： The present disclosure provides compounds of Formula (I), and pharmaceutically compositions thereof. Compounds of Formula (I) have been found to bind bromodomains and/or bromodomain-containing proteins (e.g., bromo and extra terminal (BET) proteins). Also provided are methods, uses, and kits of the compounds and pharmaceutical compositions for inhibiting the activity (e.g., increased activity) of bromodomains and/or bromodomain-containing proteins and for treating and/or preventing in a subject diseases associated with bromodomains or bromodomain-containing proteins (e.g., proliferative diseases, cardiovascular diseases, viral infections, fibrotic diseases, neurological diseases, metabolic diseases, endocrine diseases, and radiation poisoning). The compounds, pharmaceutical compositions, and kits are also useful for male contraception.
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5.发明公开COMBINATION THERAPY FOR CANCER USING BROMODOMAIN AND EXTRA-TERMINAL (BET) PROTEIN INHIBITORS 审中-公开KOMBINATIONSTHERAPIE GEGEN KREBS MIT EINERBROMDOMÄNEUND EXTRATERMINALEN（BET）-PROTEINHEMMERN
公开(公告)号：EP3066101A4
公开(公告)日：2017-05-31
申请号：EP14860080
申请日：2014-11-07
发明人： BRADNER JAMES E , MCKEOWN MICHAEL R , SHIPP MARGARET A , CHAPUY BJOERN , WONG KWOK KIN , CHEN ZHAO
IPC分类号： A61K31/551 , A61P35/00 , C07D495/14
CPC分类号： A61K31/551 , A61K31/404 , A61K31/453 , A61K31/5377 , A61K45/06 , C07D487/04 , C07D495/14
摘要： The present invention provides methods for treating cancer using combinations of bromodomain and extra-terminal (BET) protein inhibitors and certain chemotherapeutic drugs.
摘要翻译： 本发明提供了使用溴结构域和额外（BET）蛋白质抑制剂和某些化学治疗药物的组合治疗癌症的方法。
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公开(公告)号：EP1994209A4
公开(公告)日：2013-11-13
申请号：EP07835647
申请日：2007-01-03
CPC分类号： G01N33/6803 , B01J19/0046 , B01J2219/00527 , B01J2219/00605 , B01J2219/00626 , B01J2219/00659 , B01J2219/0072 , B01J2219/0074 , C40B30/04 , C40B40/04 , C40B80/00 , G01N33/50 , G01N33/53 , G01N33/543 , G01N33/54353 , G01N33/547 , G01N33/552 , G01N33/553
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公开(公告)号：EP3204504A4
公开(公告)日：2018-03-21
申请号：EP15848994
申请日：2015-10-09
发明人： KAELIN WILLIAM , LU GANG , MIDDLETON RICHARD , WONG KWOK KIN , BRADNER JAMES E
CPC分类号： G01N33/6845 , C12N15/1082 , C12N15/113 , C12N15/1137 , C12N15/64 , C12N2310/10 , C12N2310/14 , C12N2310/20 , C12N2330/51 , G01N2500/10 , C12N2310/531
摘要： The present application relates, in some aspects, to the development of a plasmid that can be used to efficiently monitor the stabilities of thousands of proteins after specific perturbations. The plasmid allows for the co-expression of two reporter proteins, each of which is placed under the control of an IRES. Other aspects of the invention relate to a plasmid library, screening methods to identify proteins whose levels are modulated by a compound of interest, and methods for monitoring treatment of a subject with an IMiD compound.
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公开(公告)号：EP3099693A4
公开(公告)日：2017-08-16
申请号：EP15743564
申请日：2015-02-02
发明人： BRADNER JAMES E , GRAY NATHANAEL , QI JUN , MCKEOWN MICHAEL R , BUCKLEY DENNIS
CPC分类号： C07D487/04 , A61K31/551 , A61K31/5513 , A61K31/5517 , A61K2300/00
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公开(公告)号：EP3099677A4
公开(公告)日：2017-07-26
申请号：EP15742537
申请日：2015-02-02
发明人： BRADNER JAMES E , QI JUN , TANAKA MINORU
IPC分类号： C07D403/14 , A61K31/506 , A61K31/5377
CPC分类号： C07D403/12 , C07D239/42 , C07D239/48
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公开(公告)号：EP3099696A4
公开(公告)日：2017-07-05
申请号：EP15744026
申请日：2015-02-02
发明人： BRADNER JAMES E , GRAY NATHANAEL , QI JUN , MCKEOWN MICHAEL R , BUCKLEY DENNIS
IPC分类号： C07D471/04 , A61K31/551 , A61K31/5517 , A61P3/00 , A61P29/00 , A61P31/00 , A61P35/00 , C07D487/04 , C07D487/14
CPC分类号： C07D471/04 , C07D487/04 , C07D487/14 , C07D495/14
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