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US 12,491,188 B2Granted
Small molecule PARG inhibitors and methods of use thereof
AssigneeBoard of Regents, The University of Texas System
InventorsJohn A. Tainer, Zamal Ahmed, Darin E. Jones, In-Kwon Kim, Tom Ellenberger, Chris Ho
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Abstract
The present disclosure provides methods of inhibiting PARG in cancer cells, including methods comprising administering a PARG inhibitor that modulates position Tyr795 in PARG. Also provided herein are methods of treating and/or preventing cancer comprising administering a PARG inhibitor. In some embodiments, the PARG inhibitors are of the formula: wherein the variables are defined herein.
Claims3
A compound of the formula:
- wherein:
- m is 0 or 1;
- R9 and R10 are each independently hydrogen, alkyl(C≤12), or substituted alkyl(C≤12);
- R11 is hydrogen;
- or
- heterocycloalkyl(C≤12), substituted heterocycloalkyl(C≤12), -alkanediyl(C≤12)-heterocycloalkyl(C≤12), or substituted -alkanediyl(C≤12)-heterocycloalkyl(C≤12);
- X7 and X9 are each independently O or S;
- X8 is a covalent bond, O, S, or NH;
- and
- Z6 and Z7 are each independently O, S, or NRa, wherein:
- Ra is hydrogen, alkyl(C≤12), or substituted alkyl(C≤12);
- or a pharmaceutically acceptable salt thereof.
9 more elements
Dependencies are inferred from the claim text.