- 专利标题: COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF ANDROGEN RECEPTOR
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申请号: US15663273申请日: 2017-07-28
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公开(公告)号: US20170327469A1公开(公告)日: 2017-11-16
- 发明人: Andrew P. Crew , Hanqing Dong , Jing Wang , Caterina Ferraro , Xin Chen , Yimin Qian
- 申请人: Arvinas, Inc.
- 主分类号: C07D233/86
- IPC分类号: C07D233/86 ; C07D471/10 ; C07D401/08 ; C07D401/04 ; C07D241/28 ; C07D239/42 ; C07D237/24 ; C07D235/02 ; C07D231/14 ; C07D213/82 ; C07C271/24 ; C07C255/54 ; A61K45/06 ; A61K31/454 ; A61K31/4439 ; A61K31/435 ; A61K31/4188 ; A61K31/4184 ; A61K31/4166 ; A61K31/277 ; A61K47/54 ; C07D491/107 ; C07C2601/04
摘要:
The present disclosure 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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