IP Library Granted Patent US 10,973,819
Granted Patent B2
US 10,973,819 · App. 16/081,662 · Granted Apr 13, 2021

Small molecules inhibitors of RAD51

Inventors: Philip Connell (Chicago, IL); Wei Lv (Chicago, IL); Brian Budke (Chicago, IL); Alan Kozikowski (Chicago, IL)
Assignee: The University of Chicago
A61K31/4985A61K31/5377A61K45/06A61P35/00C07D487/04
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Quick Facts
Patent No.
US 10,973,819
App. No.
16/081,662
Granted
Apr 13, 2021
Kind
B2
Abstract

Embodiments concern methods and small molecule compositions for selectively inhibiting RAD51-mediated D-loop formation while preserving RAD51's ability to form nucleoprotein filaments. The selective RAD51 D-loop formation activity inhibitors DNA repair while minimizing replication-associated toxicity in normal tissue.

Claims (16)

1. A method for inhibiting RAD51 D-loop-formation activity in a ovarian cell comprising providing to said cell an effective amount of a RAD51 inhibitor, wherein the RAD51 inhibitor is a compound of formula (I):

wherein R 1 is hydrogen, hydroxyl, ether, halo-alkyl ether, nitro, amine, alkylamine, dialkylamine, or heterocycle;

R 2 is hydrogen, nitro, or amine;

R 3 and R 4 are independently selected from hydrogen, halogen, hydroxyl, ether, halo-alkyl ether, alkoxyalkyl, or 2-oxy-2-methylpropanamide;

W is C or CH;

X is C, CH, or N;

Y is C, CH, or N;

Z is C or CH; and

A and B are H or join to form a carbocyclic ring;

or a salt, or enantiomer thereof.

2. The method of claim 1 , wherein the cancer cell is resistant to chemotherapy or radiation.

3. The method of any of claim 1 , wherein the cell is in a patient.

4. The method of claim 3 , wherein the patient is a cancer patient.

5. The method of claim 3 , wherein the patient has been determined to have chemotherapy- or radiation-resistant cancer.

6. The method of claim 1 , wherein the cells have been treated or will be treated with a DNA damaging agent.

7. The method of claim 6 , wherein the DNA damaging agent is a cross linking agent, an alkylating agent, nitrosourea, anti-metabolite, plant alkaloid, plant extract, radiation, or radioisotope.

Assignments (2)
CONFIRMATORY LICENSE Recorded Sep 1, 2020
From: UNIVERSITY OF CHICAGO
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 053656/0781 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 31, 2018
From: CONNELL, PHILIP; LV, WEI; BUDKE, BRIAN; KOZIKOWSKI, ALAN
To: THE UNIVERSITY OF CHICAGO
Reel/Frame 046768/0335 →
Continuity (2)
Provisional Application 62302569 · Mar 2, 2016
Related Publication 20190083491A1 · Mar 21, 2019