TRICYCLIC CONDENSED DERIVATIVES OF PYRIDIN-2-ONE AND USE THEREOF AS BRD4 INHIBITORS Russian patent published in 2020 - IPC C07D471/14 C07D491/14 C07D495/14 C07D513/14 A61K31/55 A61P35/00 

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to a compound having formula (I),

formula (I),

or its tautomeric forms, stereoisomers or pharmaceutically acceptable salts. In formula 1: ---- is absent or is a single bond, X is selected from -O- or -N-, n equals 0–6, R1 is C1-6 alkyl, where C1-6 alkyl is optionally substituted with one or more groups, selected from a hydrogen atom, C1-6 alkyl, a halogen atom, OH, R2 and R3 are independently selected from a hydrogen atom, a hydroxy group, C1-6 alkyl, C1-6 haloalkyl, C1-6 alkoxy group or C1-6 haloalkoxy- group, R4 is selected from a group consisting of C1-6 alkyl, haloalkyl, C3-8 cycloalkyl, C3-8 cycloalkyl(C1-6 alkyl), C6 aryl, or alkoxyalkyl, where C1-6 alkyl, C3-8 cycloalkyl, C3-8 cycloalkyl(C1-6 alkyl), C6 aryl are optionally substituted with one or more groups selected from a hydrogen atom, C1-6 alkyl, a halogen atom, OH and a cyano group, cycle A is C1-6 heteroaryl with heteroatoms selected from N, O, S, Z is selected from -CH2OR5, -COOR5, -CONR5R6, -NR5R6, -NR5CO-OR6, -NR5CO-NR6R7, -NR5COR6 or -O-CO-NR5R6, R5, R6 and R7 are independently selected from a hydrogen atom or substituted or unsubstituted C6 aryl, C3-8 cycloalkyl and C1-6 alkyl, where when R5, R6 and R7 are substituted, substitutes are selected from a hydrogen atom or a hydroxy group. Also disclosed are a pharmaceutical composition, a BRD4 protein inhibition method, a method of treating a BRD4 mediated condition, method for treating and/or preventing a proliferative disorder or cancer and using the compound of formula 1 or a pharmaceutical composition.

EFFECT: compounds of the present invention can be used as medicinal agents and in production of medicinal agents for treating, preventing or suppressing diseases and conditions mediated by one or more bromodomains of the BET family.

18 cl, 1 tbl, 43 ex