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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 10730862 B1

PDFFull Text
Date of Patent:
Aug. 04, 2020

Filed:

Jan. 11, 2013

Compounds and methods for the enhanced degradation of targeted proteins and other polypeptides by an e3 ubiquitin ligase

Applicants:

Yale University, New Haven, CT (US);

Glaxosmithkline Intellectual Property Development Limited, Brentford, Middlesex, GB;

Cambridge Enterprise Limited University of Cambridge, Cambridge, GB;

Inventors:

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

Dennis Buckley, New Haven, CT (US);

Alessio Ciulli, Cambridge, GB;

William Jorgensen, Deep River, CT (US);

Peter C. Gareiss, Milford, CT (US);

Inge Van Molle, Cambridge, GB;

Jeffrey Gustafson, New Haven, CT (US);

Hyun-Seop Tae, New Haven, CT (US);

Julien Michel, Edinburgh, GB;

Denton Wade Hoyer, Niantic, CT (US);

Anke G. Roth, Levenhagen, DE;

John David Harling, Stevenage, GB;

Ian Edward David Smith, Stevenage, GB;

Afjal Hussain Miah, Stevenage, GB;

Sebastien Andre Campos, Stevenage, GB;

Joelle Le, Stevenage, GB;

Assignees:

Yale University, New Haven, CT (US);

Glaxosmithkline Intellectual Property Development, Brenford, Middlesex, GB;

Cambridge Enterprise Limited University of Cambridge, Cambridge, GB;

Attorneys:

Saul Ewing Arnstein & Lehr LLP

Kathryn Doyle

Domingos J. Silva

Primary Examiner:

Matthew P Coughlin

Int. Cl.
CPC ...
C07D 413/14 (2006.01); C07D 417/12 (2006.01); C07D 417/14 (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 207/16 (2006.01); C07D 413/12 (2006.01); C07D 207/26 (2006.01); C12N 9/00 (2006.01); A61K 47/54 (2017.01); A61K 47/64 (2017.01); A61K 47/55 (2017.01); A61K 31/422 (2006.01); A61K 31/427 (2006.01); A61K 31/437 (2006.01); A61K 31/4439 (2006.01); A61K 31/454 (2006.01); A61K 31/5377 (2006.01); A61K 38/05 (2006.01); A61K 38/06 (2006.01); A61K 45/06 (2006.01); C07D 413/06 (2006.01); C07D 471/04 (2006.01); C07J 43/00 (2006.01);
U.S. Cl.
CPC ...
C07D 413/14 (2013.01); A61K 31/422 (2013.01); A61K 31/427 (2013.01); A61K 31/437 (2013.01); A61K 31/4439 (2013.01); A61K 31/454 (2013.01); A61K 31/5377 (2013.01); A61K 38/05 (2013.01); A61K 38/06 (2013.01); A61K 45/06 (2013.01); A61K 47/545 (2017.08); A61K 47/55 (2017.08); A61K 47/64 (2017.08); C07D 207/16 (2013.01); C07D 207/26 (2013.01); C07D 401/06 (2013.01); C07D 401/10 (2013.01); C07D 403/06 (2013.01); C07D 405/06 (2013.01); C07D 405/12 (2013.01); C07D 413/06 (2013.01); C07D 413/12 (2013.01); C07D 417/12 (2013.01); C07D 417/14 (2013.01); C07D 471/04 (2013.01); C07J 43/003 (2013.01); C12N 9/93 (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 that are degraded and/or otherwise inhibited by bifunctional compounds of the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand that binds to the ubiquitin ligase and on the other end a moiety that 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 of the present invention, consistent with the degradation/inhibition of targeted polypeptides.

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