The Brigham and Women's Hospital, Inc.

Dana-farber-cancer Institute Inc.

Duke University

Ross L Stein

Gregory D Cuny

Marcie A Glicksman

Jun Xian

Min Huang

Alan D D'Andrea

David Wilson

David Cohen

Neil Wagle

Ekaterina Y Shishova

April Case

Lixin Qiao

Kai W Wucherpfennig

Donald C Lo

Li-An Yeh

Melissa Call

Thomas Gainer

Sungwoon Choi

Alan D D'andrea

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.

Small molecule inhibitors of USP1 deubiquitinating enzyme activity

This invention relates to compounds of Formulas I, II, and III, and their use as inhibitors of phosphatidylcholine transfer protein (PC-TP). The invention further relates to pharmaceutical compositions and methods of treatment of disorders related to the inhibition of PC-TP using the compounds of Formulas I, II, and III. Such disorders include obesity and disorders associated with obesity.

Phosphatidylcholine transfer protein inhibitors

This invention relates to compounds of Formulas I, II, and III, and their use as inhibitors of phosphatidylcholine transfer protein (PC-TP). The invention further relates to pharmaceutical compositions and methods of treatment of disorders related to the inhibition of PC-TP using the compounds of Formulas I, II, and III. Such disorders include obesity and disorders associated with obesity. 

EphB3 kinase inhibitor compounds, including certain pyrazolo[1,5-a]pyridine and imidazo[1,2-a]pyridine compounds, inhibit EphB3 kinase. The EphB3 kinase inhibitor compounds can have greater potency for the inhibition of EphB3 kinase than general kinase inhibitors. Pharmaceutical compositions, such as neuroprotective agents, comprising the EphB3 kinase inhibitor compounds are also provided. The EphB3 kinase inhibitor compounds and pharmaceutical compositions are useful, for example, to provide neuroprotection and/or repair of neuronal tissue damaged during an ischemic event, such as a stroke.

Inhibiting Eph B-3 kinase

Compounds of formula (I), compositions, methods and kits are provided. The compounds and compositions may be particularly useful for modulating immunological responses. Formula (I) wherein, Ris alkyl, aryl, or heterocyclyl; Ris H, alkyl, aryl, heterocyclyl, ORor N(R), Ris H, alkyl, aryl, or heterocyclyl; Ris H, CN, halogen, CF, COR, or C(O)N(R); X is S, SO, O, or NR; and Y is S, O, or NR. 

Thiophene derivatives for up-regulating HLA-DM activity

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Cambridge, MA, United States of America

Ross L Stein