IP Library Granted Patent US 9,216,177
Granted Patent B2
US 9,216,177 · App. 14/001,806 · Granted Dec 22, 2015

Small molecular inhibitors of RAD51 recombinase and methods thereof

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Quick Facts
Patent No.
US 9,216,177
App. No.
14/001,806
Granted
Dec 22, 2015
Kind
B2
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 (14)

1. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a compound of Formula (1):

wherein:

R 1 is pyridinyl;

R 2 is selected from the group consisting of C 1 -C 6 alkyl, —(C 1 -C 6 )alkylene-phenyl, and —(C 1 -C 6 )alkylene-phenyl wherein the phenyl is substituted with a C 1 -C 6 alkyl;

R 3 is H or a salt thereof.

2. The pharmaceutical composition of claim 1 , wherein R2 is methyl, ethyl, n-propyl, isopropyl, benzyl, benzyl substituted on the phenyl ring with a C1-C6 alkyl.

3. A pharmaceutical composition comprising a compound selected from the group consisting of:

(E)-3-benzyl-2-(2-(pyridine-3-yl)vinyl)quinazolin-4(3H)-one(1a)

(E)-3-ethyl-2-(2-(pyrindin-3-yl)vinyl)quinazolin-4(3H)-one(1b)

and salts thereof and any mixtures thereof.

4. The pharmaceutical composition of claim 1 , further comprising a chemotherapeutic agent.

5. The pharmaceutical composition of claim 4 , wherein the agent is selected from the group consisting of an alkylating agent, antimetabolite, anthracycline, plant alkaloid, plant terpenoid, topoisomerase inhibitor, antineoplastic agent, and any combinations thereof.

6. The pharmaceutical composition of claim 3 , further comprising a chemotherapeutic agent.

7. The pharmaceutical composition of claim 6 , wherein the agent is selected from the group consisting of an alkylating agent, antimetabolite, anthracycline, plant alkaloid, plant terpenoid, topoisomerase inhibitor, antineoplastic agent, and any combinations thereof.

Assignments (4)
CONFIRMATORY LICENSE Recorded Jun 15, 2016
From: DREXEL UNIVERSITY
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 039024/0599 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 15, 2015
From: HUANG, FEI
To: DREXEL UNIVERSITY
Reel/Frame 036799/0703 →
MERGER Recorded Jan 14, 2015
From: PHILADELPHIA HEALTH & EDUCATION CORPORATION
To: DREXEL UNIVERSITY
Reel/Frame 034764/0236 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 6, 2013
From: MAZIN, ALEXANDER V.
To: PHILADELPHIA HEALTH AND EDUCATION CORPORATION D/B/A/ DREXEL UNIVERSITY COLLEGE OF MEDICINE
Reel/Frame 031555/0028 →