- 专利标题: COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF ANDROGEN RECEPTOR
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申请号: US16048191申请日: 2018-07-27
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公开(公告)号: US20180346461A1公开(公告)日: 2018-12-06
- 发明人: Andrew P. Crew , Hanqing Dong , Jing Wang , Xin Chen , Yimin Qian , Kurt Zimmermann , Craig M. Crews , Michael Berlin , Lawrence Snyder
- 申请人: Arvinas, Inc.
- 主分类号: C07D417/14
- IPC分类号: C07D417/14 ; A61P25/28 ; A61P35/00 ; C07K5/078 ; C07D413/14 ; C07D417/12 ; C07D471/10 ; C07D491/107 ; C07D401/04 ; C07D233/86 ; C07D413/12 ; A61K45/06
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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