# US 10,308,656 B2 · Small molecule inhibitors of Ku70/80 and uses thereof

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- Number: US 10,308,656 B2
- Document ID: US10308656B2
- Status: Granted
- Kind: B2
- Application number: 15/753,513
- Filed: 2016-08-16
- Published: 2018-08-30
- Granted: 2019-06-04
- Earliest claimed: 2015-08-18
- Assignees: Arizona Board of Regents on Behalf of the University of Arizona
- Applicants: Arizona Board of Regents On Behalf of the University of Arizona
- Inventors: Eric Weterings; Daruka Mahadevan; Josef Vagner
- Web page: https://patentgrep.com/patent/US10308656B2

## CPC

- C07D 487/04: Ortho-condensed systems
- A61K 31/496: Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
- A61K 31/519: ortho- or peri-condensed with heterocyclic rings
- A61K 31/55: having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 35/00: Antineoplastic agents
- C07D 413/12: linked by a chain containing hetero atoms as chain links
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- 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

## Abstract

Provided herein are methods for identifying and treating subjects having conditions involving aberrant Ku70/80 activity. In particular, the invention relates to small-molecules which function as inhibitors of Ku70/80 protein and the non-homologous end-joining (NHEJ) pathway, and their use as therapeutics for the treatment of cancer and other diseases.

## Claims

### Claim 1

A compound selected from the group consisting of:
or a pharmaceutically acceptable salts, and/or solvates thereof.

### Claim 2 (depends on 1)

A pharmaceutical composition comprising the compound of claim 1 and a pharmaceutically acceptable carrier.

### Claim 3 (depends on 1)

A kit comprising a compound of claim 1 and instructions for administering said compound to a patient having a hyperproliferative disease, wherein said hyperproliferative disease is cancer.

### Claim 4 (depends on 3)

The kit of claim 3, wherein the cancer is one or more selected from glioblastoma, prostate cancer, a solid cancer, and a hematologic cancer.

### Claim 5 (depends on 3)

The kit of claim 3, wherein the cancer is characterized by aberrant Ku70/80 activity.

### Claim 6 (depends on 3)

The kit of claim 3, wherein said cancer is any type of cancer having NHEJ pathway related activity.

### Claim 7 (depends on 3)

The kit of claim 3, wherein the cancer is characterized by aberrant of DNA-PKcs activity.

### Claim 8 (depends on 3)

The kit of claim 3, further comprising one or more anticancer agents.

### Claim 9 (depends on 8)

The kit of claim 8, wherein said compound is to be administered together with one or more anticancer agents.