BENZOPHENONES AS INHIBITORS OF IL- AND TNF-, PHARMACEUTICAL COMPOSITION AND TREATMENT METHOD

摘要

FIELD: organic chemistry, medicine, pharmacy.;SUBSTANCE: invention relates to new derivatives of benzophenone of the general formula (I): or their pharmaceutically acceptable salts and N-oxides, i. e. compounds wherein nitrogen atom at heterocyclic substitute can be oxidized. Compounds show property of inhibitor of interleukin (IL-1) or alpha-tumor necrosis factor (TNF-) and can be used in treatment of inflammatory diseases and states. In compound of the general formula (I) R₁ represents (C₁-C₆)-alkyl; R₂ represents one or some similar or different substitutes taken among the group consisting of hydrogen, halogen atom, (C₁-C₆)-alkyl, (C₁-C₆)-alkoxy-group; R₃ represents one substitute at ortho-position taken among the group consisting of hydrogen, halogen atom; R₄ represents hydrogen atom; R₅ represents nitrogen-containing heteroaromatic mono- or bicyclic system comprising 1-4 heteroatoms taken among nitrogen (N), sulfur (S) or oxygen (O) atoms wherein each ring comprises 5 or 6 atoms in ring with exception for triazine being indicated mono- or bicyclic system is substituted optionally with hydrogen, halogen atom, halidealkyl, cyano-, carboxy-, nitro-group, (C₁-C₆)-alkyl, (C₁-C₆)-alkoxy-group, (C₁-C₆)-alkoxycarbonyl, -NR₉R₁₀ wherein R₉ and R₁₀ represent hydrogen atom; X represents oxygen atom. Also, invention relates to a pharmaceutical composition and to a method for treatment and prophylaxis of diseases.;EFFECT: improved treatment method, valuable medicinal properties of compounds.;20 cl, 3 tbl, 83 ex