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.

Date of Patent:
Jun. 07, 2022

Filed:

Jan. 20, 2016
Applicant:

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

Inventors:

Meizhong Jin, East Northport, NY (US);

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);

Assignee:

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

Attorneys:
Primary Examiner:
Int. Cl.
CPC ...
C07D 417/14 (2006.01); C07D 413/14 (2006.01); A61K 31/422 (2006.01); A61K 31/4439 (2006.01); C07D 417/12 (2006.01); A61K 45/06 (2006.01); A61K 31/4545 (2006.01); C07D 233/86 (2006.01); C07D 401/04 (2006.01); C07D 491/107 (2006.01); C07D 471/10 (2006.01); A61K 31/427 (2006.01); C07D 413/12 (2006.01); C07K 5/078 (2006.01); A61P 35/00 (2006.01); A61P 25/28 (2006.01);
U.S. Cl.
CPC ...
C07D 417/14 (2013.01); A61K 45/06 (2013.01); A61P 25/28 (2018.01); A61P 35/00 (2018.01); C07D 233/86 (2013.01); C07D 401/04 (2013.01); C07D 413/12 (2013.01); C07D 413/14 (2013.01); C07D 417/12 (2013.01); C07D 471/10 (2013.01); C07D 491/107 (2013.01); C07K 5/06165 (2013.01);
Abstract

The present invention 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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