Alan D. D'Andrea - Winchester MA, US Gregory D. Cuny - Houston TX, US Ross L. Stein - Cambridge MA, US Marcie Glicksman - Winchester MA, US April Case - Watertown MA, US Jun Xian - Sharon MA, US David Wilson - Lawrence KS, US Min Huang - Pudong, CN
Assignee:
The Brigham and Women's Hospital, Inc. - Boston MA Dana-Farber Cancer Institute, Inc. - Boston MA
Provided are small molecule inhibitors of ubiquitin specific protease 1 (USP1) activity and methods for their use in treating and characterizing cancers. The small molecule USP1 inhibitors of the invention are particularly useful in the treatment of cancers that are resistant to DNA cross-linking agents.
Ross Stein - Sudbury MA, US April Case - Watertown MA, US Li-An Yeh - Cary NC, US Gregory Cuny - Somerville MA, US Eric Duval - Den Haag, NL
International Classification:
A61K 31/519 C07D 487/02 C07D 491/02 C07D 498/02
US Classification:
514260100, 544278000, 544280000, 514265100
Abstract:
The present invention provides novel compounds and methods useful for treating transglutaminase associated disorders such as celiac spru, Alzheimer's disease and Huntington's disease. Certain compounds of the invention are tissue transglutaminase inhibitors that comprise thiophene moieties. Methods of the invention include treatment of transglutaminase associated disorders with inhibitors of transglutaminase.
Small Molecule Inhibitors Of Usp1 Deubiquitinating Enzyme Activity
- Boston MA, US Ross L. Stein - Cambridge MA, US Marcie Glicksman - Winchester MA, US April Case - Watertown MA, US Jun Xian - Sharon MA, US David Wilson - Lawrence KS, US Min Huang - Pudong, CN
Assignee:
Dana-Farber Cancer Institute, Inc. - Boston MA The Brigham and Women's Hospital, Inc. - Boston MA
International Classification:
A61K 31/423
Abstract:
Provided are small molecule inhibitors of ubiquitin specific protease 1 (USP1) activity and methods for their use in treating and characterizing cancers. The small molecule USP1 inhibitors of the invention are particularly useful in the treatment of cancers that are resistant to DNA cross-linking agents.