Back to results
US 2017/0360765 A1Published application
SUBSTITUTED PYRIDINES 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
Life of this patent
Estimating the term…
Abstract
The disclosure relates to substituted pyridines, which are useful for inhibition of BET protein function by binding to bromodomains, and their use in therapy.
Claims31
1-70. (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), —CF 3, —CN, 13 C(O)NHR1, —C(O)R1, —S(O)R1, and —NR1R2;
- B is selected from alkyl (C1-C6), benzyl, and phenyl optionally substituted with halogen;
- L is selected from —CH2— 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—;
- Y is selected from —O— and NHMe, wherein if Y=NHMe then B is absent;
- 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/or hydroxyl. 72, (New) The compound according to claim 71, wherein A is selected from optionally substituted aryl groups.
8 more elements
Dependencies are inferred from the claim text.