- 专利标题: COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF ANDROGEN RECEPTOR
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申请号: EP20150564.1申请日: 2017-10-11
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公开(公告)号: EP3660004A1公开(公告)日: 2020-06-03
- 发明人: CREW, Andrew P. , HORNBERGER, Keith R. , SNYDER, Lawrence B. , ZIMMERMANN, Kurt , WANG, Jing , BERLIN, Michael , CREWS, Craig M. , DONG, Hanqing
- 申请人: Arvinas Operations, Inc.
- 申请人地址: 5 Science Park New Haven, CT 06511 US
- 专利权人: Arvinas Operations, Inc.
- 当前专利权人: Arvinas Operations, Inc.
- 当前专利权人地址: 5 Science Park New Haven, CT 06511 US
- 代理机构: Cooley (UK) LLP
- 优先权: US201662406888P 20161011; US201762528385P 20170703
- 主分类号: C07D233/86
- IPC分类号: C07D233/86 ; C07D401/04 ; C07D491/107 ; C07D471/10 ; A61K31/4164 ; A61K31/4439
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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