Granted Patent
B2
US 12,312,316 · App. 15/663,273 · Granted May 27, 2025
Compounds and methods for the targeted degradation of androgen receptor
Inventors:
Andrew P. Crew (Chester, CT); Hanqing Dong (Madison, CT); Xin Chen (Trumbull, CT); Yimin Qian (Plainsboro, NJ); Lawrence B. Snyder (Killingworth, CT)
Assignee:
Arvinas Operations, Inc.
C07D233/86A61K31/277A61K31/4166A61K31/4184A61K31/4188A61K31/435A61K31/4439A61K31/454A61K45/06A61K47/545C07C255/54C07C271/24C07D213/82C07D231/14C07D235/02C07D237/24C07D239/42C07D241/28C07D401/04C07D401/08C07D413/12C07D413/14C07D417/12C07D417/14C07D471/10C07D491/107C07C2601/04
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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.
Claims (2)
1. A compound selected from the group consisting of
and a pharmaceutically acceptable salt thereof.
Assignments (2)
CHANGE OF NAME
Recorded Oct 9, 2019
From: ARVINAS, INC.
To: ARVINAS OPERATIONS, INC.
Reel/Frame 050673/0807 →
ASSIGNMENT OF ASSIGNOR'S INTEREST
Recorded Sep 19, 2018
From: CREW, ANDREW P.; DONG, HANQING; WANG, JING; QIAN, YIMIN; ZIMMERMANN, KURT; CREWS, CRAIG M.; BERLIN, MICHAEL; SNYDER, LAWRENCE; CHEN, XIN
To: ARVINAS, INC.
Reel/Frame 046916/0429 →
Continuity (3)
Provisional Application
62105210
· Jan 20, 2015
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