US 9,802,904 B2 · Inhibitors of the USP1/UAF1 deubiquitinase complex and uses thereof

Inhibitors of the USP1/UAF1 deubiquitinase complex and uses thereof

AssigneesThe United States of America, as represented by the Secretary, Department of Health and Human Services, University of Delaware

InventorsDavid J. Maloney, Andrew S. Rosenthal, Ajit Jadhav, Thomas S. Dexheimer, Anton Simeonov, Zhihao Zhuang, Qin Liang, Diane K. Luci

Life of this patent

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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.

Claims4

Dependent claims

A compound of formula (I):

wherein Q is
wherein R1 is selected from aryl,
R2 is selected from
R3 is selected from hydrogen and alkyl,
R4 is selected from hydrogen, alkyl, alkoxy, amino, alkylamino, dialkylatnino, alkyithio, and halo, and
R5 is hydrogen or alkyl,
a deuterated derivative thereof, or a pharmaceutically acceptable salt thereof.

4 more elements

Dependencies are inferred from the claim text.

Facts

Application

14/655,538Filed 26 Dec 2013 · us provisional application

Priority

28 Dec 2012

Published

US 2015/0344443 A13 Dec 2015

Granted

31 Oct 2017

Term ends

Not estimatedThe source records don’t support an estimate.

Classification16 codes

C07D 239/94
With hetero atoms directly attached in position 4: nitrogen atoms
A61P 35/00
Antineoplastic agents
A61P 35/02
Antineoplastic agents: specific for leukemia
A61P 43/00
Drugs for specific purposes, not provided for in groups a61p1/00-a61p41/00