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US 2026/0076941 A1Published application
Indolinone compounds and uses thereof
AssigneeGeorgetown University
InventorJean-Michel Vernier
Life of this patent
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Abstract
Indolinone derivative compounds that act as EWS-PLI1 transcription factor inhibitors are provided. Also provided are pharmaceutical compositions of the indolinone derivatives, methods of synthesizing the same, methods of treating using same, and assays for identifying the inhibitors of EWS-FLI1 oncoprotein.
Claims29
A compound having a structure of Formula (I):
- or a stereoisomer, a pharmaceutically acceptable salt, or solvate thereof, wherein
- R1, R2, R3, and R4 are independently selected from the group consisting of H, Cl, —CN and —CF3;
- A is selected from the group consisting of H and C1-6 alkyl;
- D is selected from the group consisting of —OH and —O(C1-6 alkyl);
- R5 and R6 are independently selected from the group consisting of H, F, and C1-6 alkyl, or wherein R5 and taken together form a substituted or unsubstituted cycloalkyl ring;
- R12 is independently selected from the group consisting of C3-8 cycloalkyl and
- and
- R7, R8, R9, R10 and R11 are independently selected from the group consisting of H, halogen, CN, CF3, C1-6 alkyl, aryl, heteroaryl, —O(aryl), —O(heteroaryl), —CO2H, —CO2(C1-6 alkyl), —NHSO2(C1-6 alkyl), —NHSO2(aryl), —NHCONH(C1-6 alkyl), —NHCON(C1-6 alkyl)2, —N(C1-6 alkyl)CONH2, —N(C1-6 alkyl)CONH(C1-6 alkyl), —N(C1-6 alkyl)CON(C1-6 alkyl)2, —SO2(C1-6 alkyl), —SO2NH2, —SO2NH(C1-6 alkyl), —SO2N(C1-6 alkyl)2, C3-8 cycloalkyl, and C3-8heterocycloalkyl.
5 more elements
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Dependencies are inferred from the claim text.