FIELD: chemistry.
SUBSTANCE: in novel derivatives of 4-(4-alkoxy-3-hydroxyphenyl)-2-pyrrolidone of formula I 
, X represents O, R1 represents C1-C8alkyl, C3-C8cycloalkyl, C8-C16arylalkyl, C8-C16arylalkenyl, in which alkenyl fragment contains up to 5 carbon atoms, C4-C16cycloalkylalkyl, R2 represents C1-C4alkyl, unsubstituted or substituted with one or more halogens, R3 represents C3-C8cycloalkyl, C7-C16arylalkyl, substituted with one or more substituents from halogen line, C1-C8alkyl, C1-C8alkoxy, cyano or CF3, C3-C8alkoxyalkyl, -C(O)R4 or -CH2CONHR5; R4 represents C6-C14aryl, substituted with one or more substituents from halogen line, C1-C8alkoxy or nitro; R5 represents C6-C14aryl, unsubstituted or substituted with one or more substituents from halogen line, C1-C8alkyl, C1-C8alkoxy, nitro or amino, heterocyclic group, saturated, partially saturated or fully unsaturated, which contains in cycle from 5 to 6 atoms, from which one atom is N, or additionally second atom is represented with heteroatom, selected from N, O and S, heterocyclic group is unsubstituted or substituted with one or more substituents from halogen line, C1-C8alkyl, C1-C8alkoxy, or their combinations; or heterocyclylC1-C5alkyl, saturated, partially saturated or unsaturated, which contains in cycle from 5 to 6 atoms, from which one atom is N, O or S, and which is unsubstituted or substituted in heterocyclic fragment with C1-C8alkyl or C1-C8alkoxy group, and their physiologically acceptable salts, in each case compound can be in form of enantiomer mixture, such as racemate, or mixture of diastereomers, or can be in form of one enantiomer or one diastereomer; on condition that if R1 represents cyclopentyl and R2 represents methyl, R3 does not represent benzyl, 4-bromobenzyl, 3,4-dimethoxybenzyl or 4-cyanobenzyl. Compounds I inhibit activity of PDE-4 enzyme, which allows using them in pharmaceutical compositions.
EFFECT: increase of composition and treatment method efficiency.
38 cl, 11 ex
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