Michael Lazarus

US Patent:

20140163079, Jun 12, 2014

Filed:

Jul 6, 2012

Appl. No.:

14/131024

Inventors:

Suzanne Walker Kahne - Brookline MA, US
Jiaoyang Jiang - Boston MA, US
Michael Block Lazarus - West Newton MA, US

Assignee:

President and Fellows of Harvard College - Cambridge MA

International Classification:

C07D 263/58

US Classification:

514375, 548221, 435184

Abstract:

The present invention provides compounds of Formulae (I)-(V), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. In one aspect, compounds of the present invention are useful as glycosyltransferase inhibitors, in particular, O-linked N-acetylglucosamine (O-GlcNAc) transferase (OGT) inhibitors. In another aspect, compounds of the present invention are useful as kinase inhibitors, in particular, PLK1 inhibitors, GSK3P inhibitors, or MAPKAPK2 inhibitors. The present invention further provides methods of using the inventive compounds, e.g., as biological probes to study the inhibition of OGT and/or kinase activity and as therapeutics, e.g., for the treatment of OGT-associated and/or kinase-associated conditions.

US Patent:

20120108605, May 3, 2012

Filed:

Jun 1, 2010

Appl. No.:

13/375036

Inventors:

Suzanne Walker Kahne - Brookline MA, US
Michael Block Lazarus - W. Newton MA, US
Benjamin J. Gross - Philadelphia PA, US

Assignee:

President and Fellows of Harvard College - Cambridge MA

International Classification:

A61K 31/496
C07D 401/12
C07D 409/14
C07D 215/36
C07D 417/12
C07D 405/14
C07D 405/12
A61K 31/4709
A61K 31/4725
C12N 5/071
A61P 25/00
A61P 35/00
A61P 3/10
A61P 29/00
A61P 37/00
C07D 401/14

US Classification:

51425307, 544363, 546158, 546157, 546141, 546143, 514312, 514310, 435375

Abstract:

The present invention provides inhibitors of O-GIcNAc transferase. Typically, the inhibitors are quinolinone-6-sulfonamides. The invention also provides pharmaceutical compositions thereof and methods for using the same in diabetes and complications thereof, neurodegenerative diseases, cancers, autoimmune diseases, and inflammatory diseases.