Invention Grant
- Patent Title: Compounds and methods for the targeted degradation of androgen receptor
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Application No.: US16656526Application Date: 2019-10-17
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Publication No.: US11427548B2Publication Date: 2022-08-30
- Inventor: Andrew P. Crew , Hanqing Dong , Jing Wang , Xin Chen , Yimin Qian , Kurt Zimmermann , Michael Berlin , Lawrence Snyder
- Applicant: Arvinas Operations, Inc.
- Applicant Address: US CT New Haven
- Assignee: Arvinas Operations, Inc.
- Current Assignee: Arvinas Operations, Inc.
- Current Assignee Address: US CT New Haven
- Agency: Cantor Colburn LLP
- Agent Bryan D. Zerhusen, Esq.; Nicholas R. Herrel, Esq.
- Main IPC: C07D233/86
- IPC: C07D233/86 ; C07D417/14 ; C07D413/12 ; C07D417/12 ; A61K45/06 ; C07D491/107 ; C07D471/10 ; C07D235/02 ; C07D401/04 ; C07D401/08 ; C07C255/54 ; C07D237/24 ; C07C271/24 ; C07D241/28 ; C07D239/42 ; C07D231/14 ; C07D213/82 ; A61K31/4166 ; A61K47/54 ; A61K31/4439 ; A61K31/4188 ; A61K31/435 ; A61K31/454 ; A61K31/4184 ; A61K31/277 ; C07D413/14
Abstract:
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.
Public/Granted literature
- US20200055825A1 COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF ANDROGEN RECEPTOR Public/Granted day:2020-02-20
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