Inhibitors of the USP1/UAF1 deubiquitinase complex and uses thereof

US9802904B2 · kind B2 · utility

Assignees

• The United States of America, as represented by the Secretary, Department of Health and Human Services · US
• University Of Delaware · US

Inventors

• David J. Maloney · Point of Rocks, US
• Andrew S. Rosenthal · Derwood, US
• Ajit Jadhav · Chantilly, US
• Thomas S. Dexheimer · Lansing, US
• Anton Simeonov · Rockville, US
• Zhihao Zhuang · Wilmington, US
• Qin LIANG · Elkton, US
• Diane K. Luci · Germantown, US

Key dates

• Filing date: Dec 26, 2013
• Grant date: Oct 31, 2017
• Expiry date: Dec 26, 2033

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D495/04
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Disclosed are inhibitors of the USP1/UAF1 deubiquitinase complex, for example. of formula (I), wherein R1, R2, and Q are as defined herein, which are useful in treating diseases such as cancer, and improving the efficacy of DNA damaging agents in cancer treatment. Also disclosed is a composition comprising a pharmaceutically suitable carrier and at least one compound of the invention, a method of method of inhibiting a heterodimeric deubiquitinase complex in a cell, and a method of enhancing the chemotherapeutic treatment of cancer in a mammal undergoing treatment with an anti cancer agent. Further disclosed is a method of preparing compounds of the invention.