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US 2017/0360756 A1Published application
Substituted heterocycles as bromodomain inhibitors
AssigneeZenith Epigenetics Ltd.
InventorsSamuel David BROWN, Craig Alan COBURN, Oiesya KHARENKO
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Abstract
The present application relates to substituted heterocycles compound of Formula I and pharmaceutical compositions thereof useful for the inhibition of BET protein function by binding to bromodomains (Formula I).
Claims33
1-76. (canceled)
A compound of Formula I:
- or a stereoisomer, tautomer, pharmaceutically acceptable salt, or hydrate thereof,
- wherein:
- X is selected from CH and N;
- Y is selected from —NH, —N—R1b and oxygen;
- Z is selected from N, and —CH—;
- R1a and R1b are independently selected from alkyl (C1-C6), carbocycle (C3-C10), heterocycle (C2-C10) optionally substituted with 1 to 3 groups selected from R4;
- R2 is selected from aryl (C5-C10) and heteroaryl (C5-C10) optionally substituted with 1 to 5 groups selected from R5;
- R3 is selected from carbocycle (C3-C10) and heterocycle (C2-C10) optionally substituted with 1 to 5 groups selected from R5;
- each R4 is independently selected from deuterium, alkyl (C1-C6), cycloalkyl (C3-C8), alkoxy (C1-C6), amino, —NHC(O)NH-alkyl(C1-C6), halogen, amide, —CF3, —CN, —N3, ketone, —S(O)-alkyl(C1-C4), —SO2-alkyl(C1-C6), thioalkyl(C1-C6), —COOH, and ester, each of which may be optionally substituted with hydrogen, F, Cl, Br, —OH, —NH2, —NHMe, —OMe, —SMe, oxo, and/or thio-oxo;
- and
- each R5 is independently selected from deuterium, alkyl (C1-C6), alkoxy (C1-C6), amino, —NHC(O)NH-alkyl(C1-C6), halogen, amide, —CF3, —CN, —N3, ketone, —S(O)-alkyl(C1-C4), —SO2-alkyl(C1-C6), thioalkyl(C1-C6), —COOH, and ester, each of which may be optionally substituted with hydrogen, F, Cl, Br, —OH, —NH2, —NHMe, —OMe, —SMe, oxo, and/or thio-oxo.
8 more elements
Dependencies are inferred from the claim text.