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US 2022/0089620 A1Published application
Inhibitors of the enzyme enolase for precision oncology
AssigneeBoard of Regents, The University of Texas System
InventorsFlorian MULLER, Victoria YAN, Kristine YANG, Elliot BALLATO, Cong-dat PHAM
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Abstract
Provided herein are compounds of the formula: wherein the variables are defined herein. The present disclosure also provides pharmaceutical compositions comprising the compounds disclosed herein as well as methods of treatment using the compounds and/or compositions disclosed herein. Such compounds and compositions may be used, for example, for the inhibition of enolase enzymes.
Claims103
A compound of the formula:
- wherein:
- X is —O— or —NRa—, wherein:
- Ra is hydrogen, alkyl(C≤12), or substituted alkyl(C≤12);
- R1 is hydrogen, acyl(C≤12), or substituted acyl(C≤12);
- R2 is hydrogen;
- or
- alkyl(C≤12), acyl(C≤12), aralkyl(C≤12), heteroaralkyl(C≤12), or a substituted version of any of these groups;
- or
- -L1-R4;
- wherein:
- L1 is alkanediyl(C≤8) or substituted alkanediyl(C≤8);
- and
- R4 is acyl(C≤12), acyloxy(C≤12), acylthio(C≤12), —C(O)-alkoxy(C≤12), —OC(O)-heterocycloalkanediyl(C≤12)-heterocycloalkyl(C≤12), or a substituted version of any of these groups;
- or
- R2 and R3 are taken together as defined below;
- R3 is aralkyl(C≤12), heteroaralkyl(C≤12), -alkanediyl(C≤12)-alkoxy(C≤18), cycloalkyl(C≤12), -alkanediyl(C≤12)-cycloalkyl(C≤12), or a substituted version of any of these groups;
- or
- R3 and R2 are taken together as defined below;
- R2 and R3 are taken together and are -alkanediyl(C≤12)-arenediyl(C≤12)- or substituted -alkanediyl(C≤12)-arenediyl(C≤12)—;
- or a pharmaceutically acceptable salt thereof.
17 more elements
Dependencies are inferred from the claim text.