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The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Patent No.:

US 11427548 B1

PDFFull Text
Date of Patent:
Aug. 30, 2022

Filed:

Oct. 17, 2019

Compounds and methods for the targeted degradation of androgen receptor

Applicant:

Arvinas Operations, Inc., New Haven, CT (US);

Inventors:

Andrew P. Crew, Guilford, CT (US);

Hanqing Dong, Madison, CT (US);

Jing Wang, Milford, CT (US);

Xin Chen, Trumbull, CT (US);

Yimin Qian, Plainsboro, NJ (US);

Kurt Zimmermann, Durham, CT (US);

Michael Berlin, Flemington, NJ (US);

Lawrence Snyder, Killingworth, CT (US);

Assignee:

ARVINAS OPERATIONS, INC., New Haven, CT (US);

Attorneys:

Bryan D. Zerhusen, Esq.

Nicholas R. Herrel, Esq.

Cantor Colburn LLP

Primary Examiner:

Po-Chih Chen

Int. Cl.
CPC ...
C07D 233/86 (2006.01); C07D 417/14 (2006.01); C07D 413/12 (2006.01); C07D 417/12 (2006.01); A61K 45/06 (2006.01); C07D 491/107 (2006.01); C07D 471/10 (2006.01); C07D 235/02 (2006.01); C07D 401/04 (2006.01); C07D 401/08 (2006.01); C07C 255/54 (2006.01); C07D 237/24 (2006.01); C07C 271/24 (2006.01); C07D 241/28 (2006.01); C07D 239/42 (2006.01); C07D 231/14 (2006.01); C07D 213/82 (2006.01); A61K 31/4166 (2006.01); A61K 47/54 (2017.01); A61K 31/4439 (2006.01); A61K 31/4188 (2006.01); A61K 31/435 (2006.01); A61K 31/454 (2006.01); A61K 31/4184 (2006.01); A61K 31/277 (2006.01); C07D 413/14 (2006.01);
U.S. Cl.
CPC ...
C07D 233/86 (2013.01); A61K 31/277 (2013.01); A61K 31/4166 (2013.01); A61K 31/4184 (2013.01); A61K 31/4188 (2013.01); A61K 31/435 (2013.01); A61K 31/4439 (2013.01); A61K 31/454 (2013.01); A61K 45/06 (2013.01); A61K 47/545 (2017.08); C07C 255/54 (2013.01); C07C 271/24 (2013.01); C07D 213/82 (2013.01); C07D 231/14 (2013.01); C07D 235/02 (2013.01); C07D 237/24 (2013.01); C07D 239/42 (2013.01); C07D 241/28 (2013.01); C07D 401/04 (2013.01); C07D 401/08 (2013.01); C07D 413/12 (2013.01); C07D 413/14 (2013.01); C07D 417/12 (2013.01); C07D 417/14 (2013.01); C07D 471/10 (2013.01); C07D 491/107 (2013.01); C07C 2601/04 (2017.05);
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.

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