发明申请
US20160214972A1 COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF ANDROGEN RECEPTOR
审中-公开
化合物和方法对靶向降解的雄激素受体
- 专利标题： COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF ANDROGEN RECEPTOR
- 专利标题（中）： 化合物和方法对靶向降解的雄激素受体
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申请号： US15002303申请日： 2016-01-20
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公开(公告)号： US20160214972A1公开(公告)日： 2016-07-28
- 发明人: Meizhong Jin , Andrew P. Crew , Hanqing Dong , Jing Wang , Kam Siu , Caterina Ferraro , Xin Chen , Yimin Qian
- 申请人： Arvinas, Inc.
- 主分类号： C07D417/14
- IPC分类号： C07D417/14 ; C07D413/14 ; A61K31/422 ; A61K31/4439 ; C07D417/12 ; A61K45/06 ; A61K31/4545 ; C07D233/86 ; C07D401/04 ; C07D491/107 ; C07D471/10 ; A61K31/427 ; C07D413/12
摘要：
The present invention relates to bifunctional compounds, which find utility to degrade and (inhibit) Androgen Receptor. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the ubiquitin ligase and on the other end a moiety which binds Androgen Receptor such that Androgen Receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of Androgen Receptor. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of Androgen Receptor.
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