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:
Nov. 29, 2022

Filed:

Jun. 18, 2020
Applicants:

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

Yale University, New Haven, CT (US);

Inventors:

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

Craig M. Crews, New Haven, CT (US);

Xin Chen, Trumbull, CT (US);

Hanqing Dong, Madison, CT (US);

Caterina Ferraro, Stamford, CT (US);

Yimin Qian, Plainsboro, NJ (US);

Kam Siu, Milford, CT (US);

Jing Wang, Milford, CT (US);

Meizhong Jin, East Northport, NY (US);

Michael Berlin, Flemington, NJ (US);

Kurt Zimmermann, Durham, CT (US);

Assignees:

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

Yale University, New Haven, CT (US);

Attorneys:
Primary Examiner:
Int. Cl.
CPC ...
C07D 521/00 (2006.01); C07D 413/14 (2006.01); C07D 471/12 (2006.01); C07D 417/14 (2006.01); C07D 207/16 (2006.01); C07D 207/26 (2006.01); C07D 401/06 (2006.01); C07D 401/10 (2006.01); C07D 403/06 (2006.01); C07D 405/06 (2006.01); C07D 405/12 (2006.01); C07D 413/06 (2006.01); C07D 413/12 (2006.01); A61K 31/422 (2006.01); A61K 31/437 (2006.01); A61K 31/4439 (2006.01); A61K 31/5377 (2006.01); C07D 471/04 (2006.01); A61K 45/06 (2006.01); C07D 417/12 (2006.01); C07D 403/14 (2006.01); C07D 401/14 (2006.01); C07D 405/14 (2006.01); C07D 495/04 (2006.01);
U.S. Cl.
CPC ...
C07D 471/04 (2013.01); A61K 45/06 (2013.01); C07D 401/14 (2013.01); C07D 403/06 (2013.01); C07D 403/14 (2013.01); C07D 405/14 (2013.01); C07D 413/14 (2013.01); C07D 417/12 (2013.01); C07D 417/14 (2013.01); C07D 495/04 (2013.01);
Abstract

The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present invention. 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 a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of targeted polypeptides.


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