- 专利标题: COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF ANDROGEN RECEPTOR
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申请号: US16938864申请日: 2020-07-24
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公开(公告)号: US20210009528A1公开(公告)日: 2021-01-14
- 发明人: Andrew P. CREW , Keith R. HORNBERGER , Kurt ZIMMERMANN , Jing WANG , Michael BERLIN , Craig M. CREWS , Hanqing DONG , Lawrence B. SNYDER
- 申请人: Arvinas Operations, Inc.
- 申请人地址: US CT New Haven
- 专利权人: Arvinas Operations, Inc.
- 当前专利权人: Arvinas Operations, Inc.
- 当前专利权人地址: US CT New Haven
- 主分类号: C07D233/42
- IPC分类号: C07D233/42 ; A61K31/166 ; C07D211/76 ; C07D241/04 ; C07D231/12 ; C07D213/72 ; C07D205/04 ; C07D237/08 ; C07D239/24 ; C07D221/20 ; A61K31/277 ; A61K47/10 ; A61K31/02 ; A61K31/497 ; C07D209/48 ; C07D401/14 ; A61K45/06 ; A61K31/506 ; A61K31/496 ; A61K31/501
摘要:
The present disclosure relates to bifunctional compounds, which find utility to degrade (and inhibit) Androgen Receptor. In particular, the present disclosure is directed to compounds, which contain on one end a cereblon ligand which binds to the E3 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 disclosure exhibits a broad range of pharmacological activities associated with compounds according to the present disclosure, consistent with the degradation/inhibition of Androgen Receptor.
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