IP Library › Granted Patent US 9,518,032
Granted Patent B2
US 9,518,032 · App. 13/695,036 · Granted Dec 13, 2016

Small molecule inhibitors of USP1 deubiquitinating enzyme activity

Inventors: Alan D. D'Andrea (Winchester, MA); Gregory D. Cuny (Houston, TX); Ross L. Stein (Cambridge, MA); Marcie Glicksman (Winchester, MA); April Case (Watertown, MA); Jun Xian (Sharon, MA); David Wilson (Lawrence, KS); Min Huang (Pudong, CN)
Assignees: Dana-Farber Cancer Institute, Inc.; The Brigham and Women's Hospital, Inc.
C07D263/60A61K31/136A61K31/423A61K31/472A61K31/4725A61K45/06C07C225/30C07D217/24C07D405/06
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Quick Facts
Patent No.
US 9,518,032
App. No.
13/695,036
Granted
Dec 13, 2016
Kind
B2
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.

Claims (9)

1. A pharmaceutical composition comprising:

a small molecule inhibitor of ubiquitin specific protease 1 (USP1) of Formula IV (527):

or a pharmaceutically acceptable salt thereof; and

a DNA cross-linking agent.

2. The pharmaceutical composition of claim 1 , further comprising a poly (adenosine diphosphate (ADP)-ribose) polymerase (PARP) inhibitor.

3. A pharmaceutical composition comprising:

a small molecule inhibitor of ubiquitin specific protease 1 (USP1) of Formula IV (527):

or a pharmaceutically acceptable salt thereof; and

a poly (adenosine diphosphate (ADP)-ribose) polymerase (PARP) inhibitor.

Assignments (3)
CONFIRMATORY LICENSE Recorded Feb 13, 2015
From: BRIGHAM AND WOMEN'S HOSPITAL
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 034995/0403 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 10, 2013
From: CUNY, GREGORY D.; STEIN, ROSS L.; GLICKSMAN, MARCIE; CASE, APRIL; XIAN, JUN; WILSON, DAVID
To: THE BRIGHAM & WOMEN'S HOSPITAL, INC.
Reel/Frame 030765/0226 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 10, 2013
From: D'ANDREA, ALAN D.; HUANG, MIN
To: DANA-FARBER CANCER INSTITUTE, INC.
Reel/Frame 030765/0285 →
Continuity (2)
Provisional Application 61329984 · Apr 30, 2010
Related Publication 20130253005A1 · Sep 26, 2013