AMINOBENZOPHENONES AS INHIBITORS OF INTERLEUKIN IL-1BETA AND TUMOR NECROSIS FACTOR TNF-ALPHA

摘要

FIELD: organic chemistry.;SUBSTANCE: invention relates to compounds of the formula (1):; ; wherein R₁, R₂ and R₃ represent independently one or more similar or different substitutes taken among the group consisting of hydrogen, halogen atom, hydroxy-group, mercapto-group, trifluoromethyl, amino-group, (C₁-C₃)-alkyl, (C₂-C₃)-olefin group, (C₁-C₃)-alkoxy-group, (C₁-C₃)-alkylthio-group, (C₁-C₆₎-alkylamino-group, (C₁-C₃)-alkoxycarbonyl, cyano-group, carbamoyl or phenyl; R₁ and R₂ are represented by nitro-group and R₃ - by carboxy-group additionally; R₄ represents hydrogen atom, (C₁-C₃)-alkyl or allyl; Q represents a bond or -C(R₆)(R₇)(-O-C=O)- wherein R₆ and R₇ mean independently hydrogen atom, trifluoromethyl or (C₁-C₄)-alkyl; Y represents either (C₅-C₁₅)-alkyl, (C₂-C₁₅)-olefin group, (C₃-C₁₀)-monocyclic hydrocarbon or phenyl being each of that can be substituted optionally with one or more similar or different substituted represented by the formula R₅; or Y represents (C₅-C₆)-alkyl, (C₂-C₆)-alkenyl, (C₃-C₆)-cycloalkyl, (C₅-C₈)-cycloalkene group or phenyl bein each can be substituted optionally with one or more similar or different substituted taken among the group including halogen atom, hydroxy-group, amino-group, (C₁-C₂)-alkoxy-group, (C₁-C₄)-alkylamino-group, (C₁-C₃)-alkoxycarbonyl, cyano-group, azido-group, -COOH, -CONH₂, -CONHR' or -CONRR', wherein R and R' mean (C₁-C₂)-alkyl; or Y represents (C₁-C₄)-alkyl substituted with at least one or more substituted of the formula R₅ or -CONRR' wherein R and R' mean (C₁-C₂)-alkyl; or Y represents group of the formula -CH₂-(Z-O)_n-Z wherein Z represents (C₁-C₃)-alkyl and wherein n represents a whole number 1 being without continuous linear sequence of atoms in the group Y 15; R₅ represents halogen atom, hydroxy-group, mercapto-group, trifluoromethyl, amino-group, (C₁-C₃)-alkoxy-group, (C₁-C₃)-alkylthio-group, (C₁-C₆)-alkylamino-group, (C₁-C₃)-alkoxycarbonyl, cyano-group, azido-group, nitro-group, -COOH, -CONH₂, -CONHR', -COONR'R' wherein R' means (C₁-C₃)-alkyl; X means oxygen or sulfur atom; or pharmaceutically acceptable salts of this compound, or hydrates of this compound, or solvates of this compound that can be used for treatment of humans in veterinary science.;EFFECT: valuable medicinal and veterinary properties of compounds.;8 cl, 2 tbl, 31 ex