CONDENSED TRICYCLIC IMIDAZOLE DERIVATIVES AS MODULATORS OF TNF ACTIVITY Russian patent published in 2019 - IPC C07D471/04 C07D471/14 C07D491/147 A61K31/437 A61K31/506 A61P1/06 A61P17/06 A61P19/02 

FIELD: chemistry.

SUBSTANCE: invention relates to organic chemistry, specifically to a compound of formula (I)

or a pharmaceutically acceptable salt thereof, in which n denotes an integer equal to 1 or 2; Y denotes aryl, thiazole, pyrimidine, pyrazine, where any of these groups can optionally contain one or two substitutes selected from a difluoromethoxy group, trifluoromethoxy group, methyl, trifluoromethyl, methylsulphonyl, halogen, methoxy group, cyano; X and Z are independently denoted by a heteroatom selected from N or O; or unsubstituted linear C₁-C₄-alkylene chain; R¹ denotes aryl, C₃-C₇-heterocycloalkyl selected from piperidine, piperazine, azetidine or pyrrolidine, heteroaryl selected from pyridine, pyrimidine or pyrazole, heteroaryl (C₁-C₆) alkyl, where heteroaryl is selected from pyridine, pyrimidine or pyrazole, heteroaryl (C₃-C₇) heterocycloalkyl-, where heteroaryl is selected from pyrimidine and pyridine, and heterocycloalkyl is selected from morpholine, piperazine, piperidine, tetrahydrofuran, pyrrolidine, dioxydotetetrahydrothiophene, (C₃-C₇)cycloalkyl-heteroaryl-, where heteroaryl is selected from pyrazole and pyridine, heteroaryl-aryl-, selected from dihydroisoindolyl and triazolyl, where any of these groups may optionally contain one or two substitutes selected from C₁-C₆-alkyl, methoxy groups, methoxy(C₁-C₆)alkyl, methylsulphonyl, phenylsulphonyl, acetamide, methylcarboxylate, tert-butyl carboxylate, cyano, hydroxyalkyl, ethoxycarbonyl, carboxy groups, methylpropane nitrile, propanol, halogen (C₁-C₆)alkyl; R² denotes hydrogen, halogen, trifluoromethyl or cyano; or C₁-C₆-alkyl, optionally substituted C₂-C₆-alkoxycarbonyl; R³ and R⁴ independently denote hydrogen; R^5a and R^5b independently denote hydrogen, hydroxy group; or R^5a and R^5b together with carbon atom to which they are attached, denote carbonyl; and R⁶ independently denotes hydrogen, hydroxy group. Invention also relates to a pharmaceutical composition based on formula (I), use of the compound of formula (I) and a method of treatment based on using the compound of formula (I).

EFFECT: technical result is obtaining novel heterocyclic compounds which are active modulators of TNFα activity human and are useful for treating and/or preventing rheumatoid arthritis, psoriasis or inflammatory bowel disease.

20 cl, 108 ex