# US 9,750,742 B2 · Small molecular inhibitors of RAD51 recombinase and methods thereof

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- Number: US 9,750,742 B2
- Document ID: US9750742B2
- Status: Granted
- Kind: B2
- Application number: 14/928,788
- Filed: 2015-10-30
- Published: 2016-04-21
- Granted: 2017-09-05
- Earliest claimed: 2011-02-28
- Assignees: Drexel University
- Applicants: Alexander V. Mazin; Fei Huang
- Inventors: Alexander V. Mazin; Fei Huang
- Web page: https://patentgrep.com/patent/US9750742B2

## CPC

- A61K 31/517: ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
- A61K 31/365: Lactones
- A61K 31/502: ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
- A61K 31/506: not condensed and containing further heterocyclic rings
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- C07D 401/06: linked by a carbon chain containing only aliphatic carbon atoms
- A61N 2005/1098: {Enhancing the effect of the particle by an injected agent or implanted device}
- 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)
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61N: ELECTROTHERAPY; MAGNETOTHERAPY; RADIATION THERAPY; ULTRASOUND THERAPY (measurement of bioelectric currents A61B; surgical instruments, devices or methods for transferring non-mechanical forms of energy to or from the body A61B18/00; anaesthetic apparatus in general A61M; incandescent lamps H01K; infrared radiators for heating H05B)

## Abstract

The invention includes compositions comprising a selective small-molecule inhibitor of RAD51 recombinase and a pharmaceutically acceptable carrier. The invention further includes methods of treating or preventing cancer in a subject, comprising the step of administering to the subject the compositions contemplated within the invention.

## Claims

### Claim 1

A method of treating a RAD51-overexpressing cancer in a subject in need thereof, the method comprising administering to the subject a pharmaceutical composition comprising a pharmaceutically effective amount of at least one compound selected from the group consisting of Formula (1), Formula (2), Formula (3), a salt thereof, and any combinations thereof:
wherein in (1):
R1 is pyridinyl,
R2 is selected from the group consisting of C1-C6 alkyl, —(C1-C6)alkylene-phenyl, and —(C1-C6)alkylene-phenyl wherein the phenyl is substituted with a C1-C6 alkyl; and
R3 is H;
the method further comprising administering to the subject a treatment selected from the group consisting of (i) radiation therapy, and (ii) a pharmaceutically effective amount of a chemotherapeutic agent.

### Claim 2 (depends on 1)

The method of claim 1, wherein the at least one compound is selected from the group consisting of (E)-3-benzyl-2-(2-(pyridin-3-yl)vinyl)quinazolin-4(3H)-one (1a), (E)-3-ethyl-2-(2-(pyridin-3-yl)vinyl)quinazolin-4(3H)-one (1b), (E)-2-(2-(pyridin-3-yl)vinyl)-3-(m-tolyl)quinazolin-4(3H)-one (1c), 1,4,10-trihydroxy-5-(hydroxymethyl)-8-methyl-3,7-dioxo-3,7-dihydro-1H-benzo[6,7][1,4]dioxepino[2,3-e]isobenzofuran-11-carbaldehyde (2), 1,4-dihydroxy-10-methoxy-5,8-dimethyl-3,7-dioxo-3,7-dihydro-1H-benzo[6,7][1,4] dioxepino[2,3-e]isobenzofuran-11-carbaldehyde (3), a salt thereof, and mixtures thereof.

### Claim 3 (depends on 1)

The method of claim 1, wherein administering to the subject of the composition is performed at least 24 hours prior to administering to the subject the radiation therapy or the chemotherapeutic agent.

### Claim 4 (depends on 3)

The method of claim 3, wherein administering to the subject of the composition is performed at least 12 hours prior to administering to the subject the radiation therapy or the chemotherapeutic agent.

### Claim 5 (depends on 4)

The method of claim 4, wherein administering to the subject of the composition is performed at least 6 hours prior to administering to the subject the radiation therapy or the chemotherapeutic agent.

### Claim 6 (depends on 5)

The method of claim 5, wherein administering to the subject of the composition is performed at least 3 hours prior to administering to the subject the radiation therapy or the chemotherapeutic agent.

### Claim 7 (depends on 6)

The method of claim 6, wherein administering to the subject of the composition is performed at least 1 hour prior to administering to the subject the radiation therapy or the chemotherapeutic agent.

### Claim 8 (depends on 1)

The method of claim 1, wherein the composition is co-administered to the subject with the radiation therapy or the chemotherapeutic agent.

### Claim 9 (depends on 8)

The method of claim 8, wherein the composition and the chemotherapeutic agent are co-formulated.

### Claim 10 (depends on 1)

The method of claim 1, wherein the subject is a human.