Invention Grant
- Patent Title: Compounds and methods for the targeted degradation of androgen receptor
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Application No.: US16938864Application Date: 2020-07-24
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Publication No.: US11236051B2Publication Date: 2022-02-01
- Inventor: Andrew P. Crew , Kurt Zimmermann , Hanqing Dong , Lawrence B. 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: Cooley LLP
- Agent Ivor R. Elrifi; Thomas J. Paxton
- Main IPC: C07D401/04
- IPC: C07D401/04 ; 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

Abstract:
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.
Public/Granted literature
- US20210009528A1 COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF ANDROGEN RECEPTOR Public/Granted day:2021-01-14
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