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:
Apr. 30, 2019

Filed:

May. 16, 2018
Applicant:

President and Fellows of Harvard College, Cambridge, MA (US);

Inventors:

Matthew D. Shair, Lexington, MA (US);

Juergen Ramharter, Vienna, AT;

Henry Efrem Pelish, Newton, MA (US);

Brian Bor-Jen Liau, Belmont, MA (US);

Jae Young Ahn, Boston, MA (US);

Assignee:
Attorney:
Primary Examiner:
Int. Cl.
CPC ...
C07D 493/08 (2006.01); C07D 519/00 (2006.01); C07K 16/26 (2006.01); C07D 493/22 (2006.01); C07K 14/575 (2006.01);
U.S. Cl.
CPC ...
C07D 493/08 (2013.01); C07D 493/22 (2013.01); C07D 519/00 (2013.01); C07K 14/575 (2013.01); C07K 16/26 (2013.01);
Abstract

Provided herein are compounds of Formula (A), (B), (C), (D) and (E), pharmaceutically acceptable salts, quaternary amine salts, and N-oxides thereof, and pharmaceutical compositions thereof. Compounds of Formula (A), (B), (C), (D), and (E) are contemplated useful as therapeutics for treating a wide variety of conditions, e.g., including but not limited to, conditions associated with angiogenesis and with CDK8 and/or CDK19 kinase activity. Further provided are methods of inhibiting CDK8 and/or CDK19 kinase activity, methods of modulating the-catenin pathway, methods of modulating STAT1 activity, methods of modulating the TGFβ/BMP pathway, methods of modulating HIF-1-alpha activity in a cell, and methods of increasing BIM expression to induce apoptosis, using a compound of Formula (A), (B), (C), (D), or (E). Further provided are CDK8 and CDK19 point mutants and methods of use thereof.


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