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:
Feb. 09, 2021

Filed:

Nov. 23, 2016
Applicant:

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

Inventors:

James E. Bradner, Weston, MA (US);

Jun Qi, Sharon, MA (US);

Minoru Tanaka, Boston, MA (US);

Justin M. Roberts, Cambridge, MA (US);

Assignee:
Attorney:
Primary Examiner:
Int. Cl.
CPC ...
C07D 519/00 (2006.01); A61K 31/551 (2006.01); A61P 15/16 (2006.01);
U.S. Cl.
CPC ...
C07D 519/00 (2013.01); A61K 31/551 (2013.01); A61P 15/16 (2018.01); Y02A 50/30 (2018.01);
Abstract

The present invention provides bivalent inhibitors of BET bromodomains, such as compounds of Formulae (I), (II), (III), (IV), (V), and (VI). Some bromdomain-containing proteins (e.g., BRD4) have a tandem bromodomain primary structure comprising more than one bromodomain binding site (e.g., BRD4 comprises BD1 and BD2). Bivalent inhibitors of BET bromodomains provided herein can target bromodomains through advantageous multivalent interactions, and can therefore can be to treat diseases or conditions associated with bromodomain-containing proteins. The present also provides pharmaceutical compositions and kits comprising the inventive compounds, as well as methods of using the inventive compounds.


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