SUCCINIMIDE AND MALEIMIDE INHIBITORS OF CYTOKINS, PHARMACEUTICAL COMPOSITION BASED ON THEREOF AND METHODS OF INHIBITION OF TUMOR NECROSIS α-FACTOR Russian patent published in 2001 - IPC

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention describes novel succinimide and maleimide inhibitors of cytokins of the general formula (I) where R¹ means -CH₂-,CH₂CO or -CO-; R² and R³ taken in common means: (i) unsubstituted ethylene or ethylene substituted with alkyl containing 1-10 carbon atoms or with phenyl; (ii) vinylene substituted with two substitutes each of that is taken independently among the group including alkyl containing from 1 to 10 carbon atoms and phenyl or (iii) bivalent unsubstituted cycloalkyl containing from 5 to 10 carbon atoms or cycloalkyl substituted with one or more substitutes each of that is taken independently among the group including the following ones: nitrogroup, cyano-group, trifluoromethyl-group, carboethoxy-group, carbomethoxy-group, carbopropoxy- group, acetyl, unsubstituted carbamoyl or carbamoyl substituted with C₁-C₃-alkyl, acetoxy-group, carboxy- group, hydroxy-group, amino-group, substituted amino-group, alkyl containing from 1 to 10 carbon atoms, alkoxy-group containing from 1 to 10 carbon atoms, norbornyl, phenyl or halogen atom; R⁴ means 3,4- disubstituted phenyl substituted with one or more number of substitutes taken independently each of other among the group including the following ones: nitro-group, cyano-group, trifluoromethyl-group, carboethoxy-group, carbomethoxy-group, carbopropoxy-group, acetyl, carbamoyl, acetoxy-group, carboxy-group, hydroxy-group, amino-group, substituted amino-group, alkyl containing from 1 to 10 carbon atoms, alkoxy-group containing from 1 to 10 carbon atoms, cycloalkyl or bicycloalkyl containing from 3 to 10 carbon atoms, cycloalkoxy-group or bicycloalkoxy-group containing from 3 to 10 carbon atoms, phenyl or halogen atom, and R⁵ means -CH₂-COX where X means NH₂, OH, NHR or OR₆ where R means lower alkyl and where R₆ means alkyl or benzyl. Compounds of the formula (I) can be used for inhibition of phosphodiesterase activity, especially phosphodiesterase-III and phosphodiesterase-IV and in treatment of patients with states mediated by these enzymes. Invention describes also a pharmaceutical composition based on thereof and methods of inhibition of tumor necrosis α-factor. EFFECT: new inhibitors indicated above, valuable medicinal properties. 17 cl, 1 tbl