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. 23, 2020

Filed:

Oct. 31, 2017
Applicants:

Cornell University, Ithaca, NY (US);

Dana-farber Cancer Institute, Inc., Boston, MA (US);

Inventors:

Ari M. Melnick, New York, NY (US);

Lorena Fontan Gabas, New York, NY (US);

Nathanael S. Gray, Boston, MA (US);

David A. Scott, Newton, MA (US);

John Hatcher, Marlborough, MA (US);

Guangyan Du, Jamaica Plain, MA (US);

Assignees:

Cornell University, Ithaca, NY (US);

Dana-Farber Cancer Institute, Inc., Boston, MA (US);

Attorney:
Primary Examiner:
Int. Cl.
CPC ...
C07D 401/14 (2006.01); A61P 35/00 (2006.01); A61K 31/4439 (2006.01); A61K 31/519 (2006.01); C07D 417/14 (2006.01); C07D 471/04 (2006.01); C07D 487/04 (2006.01);
U.S. Cl.
CPC ...
C07D 401/14 (2013.01); A61K 31/4439 (2013.01); A61K 31/519 (2013.01); A61P 35/00 (2018.01); C07D 417/14 (2013.01); C07D 471/04 (2013.01); C07D 487/04 (2013.01);
Abstract

Provided herein are bifunctional compounds that inhibit MALT1 and/or promote targeted ubiquitination for the degradation of MALT1. In particular, provided are compounds that can bind MALT1, a protein whose activity is responsible for constitutive NF-KB signaling in certain cancers (e.g., activated B-cell diffuse large B-cell lymphoma (ABC-DLBCL)), and can assist in its degradation by recruiting an E3 ubiquitin ligase (e.g., Cereblon, VHL), which can ubiquitinate MALT1, marking it for proteasome degradation. Also provided are pharmaceutical compositions comprising the bifunctional compounds, methods of treating cancer with the bifunctional compounds, methods of promoting the degradation of MALT1, and methods of binding E3 ubiquitin ligase activity in a subject by administering a compound or composition described herein.


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