Inhibitors of bromodomains
The present disclosure relates to compounds capable of acting as covalent inhibitors of bromodomains and the therapeutic use of these inhibitors.
1. A compound selected from:
5-(Dimethyl-1,2-oxazol-4-yl)-1-(3-fluoro-4-(oxiran-2-yl)benzyl)pyridin-2(1H)-one;
5-(Dimethyl-1,2-oxazol-4-yl)-1-{[4-(oxiran-2-yl)phenyl]methyl}-1,2-dihydropyridin-2-one;
3-Amino-5-(3,5-dimethylisoxazol-4-yl)-1-(4-(oxiran-2-yl)benzyl)pyridin-2(1H)-one;
6-(Dimethyl-1,2-oxazol-4-yl)-1-{[4-(oxiran-2-yl)phenyl]methyl}-1H-1,3-benzodiazol-4-amine;
4-(1-{[4-(2-Chloroethyl)phenyl]ethyl}-2-methyl-1H-imidazo[4,5-b]pyridin-6-yl)-3,5-dimethyl-1,2-oxazole;
2-Chloro-1-(4-{[6-(dimethyl-1,2-oxazol-4-yl)-2-methyl-1H-imidazo[4,5-b]pyridin-1 yl]methyl}phenyl)ethan-1-one;
3,5-Dimethyl-4-(2-methyl-1-{[4-(oxiran-2-ylmethyl)phenyl]methyl}-1H-imidazo[4,5-b]pyridin-6-yl)-1,2-oxazole; and
stereoisomers, tautomers, pharmaceutically acceptable salts, and hydrates thereof.
2. A pharmaceutical composition comprising the compound of claim 1 , and a pharmaceutically acceptable carrier.
3. A method for inhibition of BET protein function comprising administering a therapeutically effective amount of the compound of claim 1 .