- 专利标题： Compounds and methods for the targeted degradation of androgen receptor
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申请号： US15002303申请日： 2016-01-20
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公开(公告)号： US11352351B2公开(公告)日： 2022-06-07
- 发明人: Meizhong Jin , Andrew P. Crew , Hanqing Dong , Jing Wang , Xin Chen , Yimin Qian
- 申请人： Arvinas, Inc.
- 申请人地址： US CT New Haven
- 专利权人： Arvinas, Inc.
- 当前专利权人： Arvinas, Inc.
- 当前专利权人地址： US CT New Haven
- 代理机构： Cantor Colburn LLP
- 代理商 Bryan D. Zerhusen, Esq.; Nicholas R. Herrel, Esq.
- 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 ; C07K5/078 ; A61P35/00 ; A61P25/28
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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