# US 9,518,032 B2 · Small molecule inhibitors of USP1 deubiquitinating enzyme activity

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- Number: US 9,518,032 B2
- Document ID: US9518032B2
- Status: Granted
- Kind: B2
- Application number: 13/695,036
- Filed: 2011-04-29
- Published: 2013-09-26
- Granted: 2016-12-13
- Earliest claimed: 2010-04-30
- Assignees: Dana-Farber Cancer Institute, Inc.; The Brigham and Women's Hospital, Inc.
- Applicants: Alan D. D'Andrea; Gregory D. Cuny; Ross L. Stein; Marcie Glicksman; April Case; Jun Xian; David Wilson; Min Huang
- Inventors: Alan D. D'Andrea; Gregory D. Cuny; Ross L. Stein; Marcie Glicksman; April Case; Jun Xian; David Wilson; Min Huang
- Web page: https://patentgrep.com/patent/US9518032B2

## CPC

- A61K 31/423: condensed with carbocyclic rings
- A61K 31/136: having the amino group directly attached to the aromatic ring, e.g. benzeneamine
- A61K 31/472: Non-condensed isoquinolines, e.g. papaverine
- A61K 31/4725: containing further heterocyclic rings
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 35/00: Antineoplastic agents
- C07C 225/30: of condensed quinone ring systems formed by two rings
- C07D 217/24: Oxygen atoms
- C07D 263/60: Naphthoxazoles; Hydrogenated naphthoxazoles
- C07D 405/06: linked by a carbon chain containing only aliphatic carbon atoms
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07C: ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)

## 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

### Claim 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.

### Claim 2 (depends on 1)

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

### Claim 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.