发明公开
EP3110818A1 9H-PYRIMIDO[4,5-B]INDOLES AND RELATED ANALOGS AS BET BROMODOMAIN INHIBITORS
审中-公开
9H-PYRIMIDO [4,5-B] INDOLE UND VERWANDTE ANALOGA ALS BET-BROMODOMÄNEN-HEMMER
- 专利标题： 9H-PYRIMIDO[4,5-B]INDOLES AND RELATED ANALOGS AS BET BROMODOMAIN INHIBITORS
- 专利标题（中）： 9H-PYRIMIDO [4,5-B] INDOLE UND VERWANDTE ANALOGA ALS BET-BROMODOMÄNEN-HEMMER
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申请号： EP15711599.9申请日： 2015-02-27
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公开(公告)号： EP3110818A1公开(公告)日： 2017-01-04
- 发明人: WANG, Shaomeng , ZHAO, Yujun , ZHOU, Bing , AGUILAR, Angelo , LIU, Liu , BAI, Longchuan , MCEACHERN, Donna , SUN, Duxin , WEN, Bo , LUO, Ruijuan , ZHAO, Ting , CHINNAIYAN, Arul , ASANGANI, Irfan, A. , STUCKEY, Jeanne , MEAGHER, Jennifer, Lynn , RAN, Xu , HU, Yang
- 申请人： The Regents of The University of Michigan
- 申请人地址： Office of Technology Transfer 1600 Huron Parkway, 2nd Floor Ann Arbor, MI 48109-2590 US
- 专利权人： The Regents of The University of Michigan
- 当前专利权人： The Regents of The University of Michigan
- 当前专利权人地址： Office of Technology Transfer 1600 Huron Parkway, 2nd Floor Ann Arbor, MI 48109-2590 US
- 代理机构： Clements, Andrew Russell Niel
- 优先权： US201461946501P 20140228; US201461950406P 20140310; US201462031640P 20140731; US201462048388P 20140910
- 国际公布： WO2015131005 20150903
- 主分类号： C07D487/04
- IPC分类号： C07D487/04 ; A61K31/519
摘要：
The present disclosure provides substituted 9H-pyrimido[4,5-b]indoles and 5H-pyrido[4,3-b]indoles and related analogs represented by Formula I: and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1a, A, B1, B2, G, X1, Y1, Y2, and Y3 are as defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I to treat a condition or disorder responsive to inhibition of BET bromodomains. Compounds of the present disclosure are especially useful for treating cancer.
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