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US 2017/0360760 A1Published application
Inhibitors of Bromodomains
AssigneeZenith Epigenetics Ltd.
InventorsOlesya KHARENKO, Peter Ronald YOUNG, Samuel David BROWN, Bryan Cordell DUFFY, Shuang LIU, Peter GUZZO
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Abstract
The present disclosure relates to compounds capable of acting as covalent inhibitors of bromodomains and the therapeutic use of these inhibitors.
Claims32
1-57. (canceled)
A compound of Formula I or Formula II:
- or a stereoisomer, tautomer, pharmaceutically acceptable salt, or hydrate thereof,
- wherein:
- R1 is selected from carbocycle (C5-C10) and heterocycle (C2-C10) optionally substituted with 1 to 5 groups independently selected from R5;
- R2 and R3 are independently selected from alkyl (C1-C6) optionally substituted with halogen and hydroxyl, with the proviso that if R2 and R3 are methyls, then R1 is different from:
- wherein A is selected from hydrogen, halogen, methoxy, —CN, —NO2, —C(O)OMe, and —C(O)NMe2;
- R4 if present, is selected from hydrogen, alkyl (C1-C10), carbocycle (C3-C10), and heterocycle (C2-C10) optionally substituted with 1 to 5 groups independently selected from R5;
- each R5 is independently selected from deuterium, epoxide, alkyl (C1-C6), alkoxy (C1-C6), amino, —NHC(O)NH—alkyl(C1-C6), halogen, amide, —CF3, —CN, —N3, ketone (C1-C6), —S(O)-alkyl(C1-C4), —SO2-alkyl(C1-C6), thioalkyl(C1-C6), —COOH, and ester, each of which may be optionally substituted with oxirane, hydrogen, F, Cl, Br, —OH, —NH2, —NHMe, —OMe, —SMe, oxo, and/or thio-oxo;
- X is selected from —CH2— optionally substituted with 1 to 2 groups independently selected from R5;
- Y if present, is selected from —N—, —CH—, and —CNH2—;
- and
- Z if present, is selected from hydrogen and amino.
8 more elements
Dependencies are inferred from the claim text.