IP Library › Granted Patent US 11,236,051
Granted Patent B2
US 11,236,051 · App. 16/938,864 · Granted Feb 1, 2022

Compounds and methods for the targeted degradation of androgen receptor

Inventors: Andrew P. Crew (Guilford, CT); Kurt Zimmermann (Durham, CT); Hanqing Dong (Madison, CT); Lawrence B. Snyder (Killingworth, CT)
Assignee: Arvinas Operations, Inc.
C07D233/42A61K31/02A61K31/166A61K31/277A61K31/496A61K31/497A61K31/501A61K31/506A61K45/06A61K47/10C07D205/04C07D209/48C07D211/76C07D213/72C07D221/20C07D231/12C07D237/08C07D239/24C07D241/04C07D401/04C07D401/14
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Quick Facts
Patent No.
US 11,236,051
App. No.
16/938,864
Granted
Feb 1, 2022
Kind
B2
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.

Claims (5)

1. A compound that is

or a pharmaceutically acceptable salt thereof.

2. A compound that is

or a pharmaceutically acceptable salt thereof.

3. A compound that is

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 2, 2020
From: CREW, ANDREW P.; HORNBERGER, KEITH R.; SNYDER, LAWRENCE B.; ZIMMERMANN, KURT; WANG, JING; BERLIN, MICHAEL; CREWS, CRAIG M.; DONG, HANQING
To: ARVINAS, INC.
Reel/Frame 053956/0976 →
CHANGE OF NAME Recorded Oct 2, 2020
From: ARVINAS, INC.
To: ARVINAS OPERATIONS, INC.
Reel/Frame 053971/0738 →
Continuity (5)
Continuation 16577901 · Sep 20, 2019
Division 15730728 · Oct 11, 2017
Provisional Application 62528385 · Jul 3, 2017
Provisional Application 62406888 · Oct 11, 2016
Related Publication 20210009528A1 · Jan 14, 2021
Cited By (4)
US 12,239,711 US 12,427,144 US 12,441,708 US 12,496,301