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US 2017/0320866 A1Published application
Substituted pyridinones as bromodomain inhibitors
AssigneeZenith Epigenetics Ltd.
InventorsMay Xiaowu Jiang, Bruce Francis Molino, Shuang Liu, Ruifang Wang, Bryan Cordell Duffy, John Frederick Quinn, Gregory Steven Wagner
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Abstract
The present disclosure relates to substituted pyridinones, which are useful for inhibition of BET protein function by binding to bromodomains, and their use in therapy.
Claims30
1-67. (canceled)
A compound of Formula I:
- or a stereoisomer, tautomer, pharmaceutically acceptable salt, or hydrate thereof,
- wherein:
- A is selected from aryl (C5-C10), heteroaryl (C2-C5), and heteroaryl (C5-C10) optionally substituted with 1 to 3 groups independently selected from halogen, alkyl (C1-C6), alkoxy (C1-C6), —CF3, —CN, —C(O)NHR1, —C(O)R1, —SO2R1, —S(O)R1, and —NR1R2;
- L is selected from —CH2—, —CH2CH2— and —CH(CH3)— optionally substituted with halogen;
- or
- L may be absent in which case A is connected to X via a covalent bond;
- X is selected from —O— and —NH—;
- R1 and R2 are independently selected from hydrogen and alkyl (C1-C6);
- and
- R3 and R4 are independently selected from alkyl (C1 C6) optionally substituted with halogen and hydroxyl.
7 more elements
Dependencies are inferred from the claim text.