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US 2016/0102055 A1Published application
Indolinone compounds and uses thereof
AssigneeTokalas, Inc.
InventorJean-Michel Vernier
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Abstract
Indolinone derivative compounds that act as EWS-FLI1 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.
Claims20
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;
- wherein A is selected from the group consisting of H and C1-6 alkyl;
- wherein D is selected from the group consisting of —OH and —O(C1-6 alkyl);
- wherein R5 and R6 are independently selected from the group consisting of H, F, and C1-6 alkyl, or wherein R5 and R6 taken together form a substituted or unsubstituted cycloalkyl ring;
- wherein R12 is independently selected from the group consisting of C3-8 cycloalkyl and
- wherein 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, 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 C3-8 heterocycloalkyl.
3 more elements
Dependencies are inferred from the claim text.