HYDROXYINDOLES, THEIR APPLICATION AS INHIBITORS OF PHOSPHODIESTERASE-4 AND METHOD FOR THEIR PREPARING Russian patent published in 2003 - IPC

FIELD: organic chemistry, biochemistry, pharmacy. SUBSTANCE: invention relates to new hydroxyindoles of the general formula (I): wherein R¹ means linear or branched C₁-C₁₂-alkyl that can be monosubstituted if necessary with monocyclic saturated or polyunsaturated carbocyclene with 6 ring members being C₆-aryl group and closed carbocyclic substituents can be mono- or polysubstituted if necessary with R⁴; R⁵ means monocyclic polyunsaturated carbocyclene with 6 ring members mono- or polysubstituted with halogen atoms or monocyclic polyunsaturated heterocyclene with 6 ring members one of that is nitrogen atom as heteroatom mono- or polysubstituted with halogen atom; R², R³ can be hydrogen atom or OH being at least one or both substituents must be OH; R⁴ means -H, -OH, -F, -Cl, -J, -Br, -O- C₁-C₆-alkyl, -NO₂; A means or a bons either -(CHOZ)_m, -(C=0)-; m = 0-3; Z means hydrogen atom; B means carbon atom; D means oxygen atom; E means (N-Z)- being Z has above mentioned value, and also their physiologically acceptable salts and isomers with asymmetric carbon atom as D-forms, L-forms and D, L-mixtures and in the case of asymmetric carbon atoms diastereomeric forms. Compounds are inhibitors of phosphodiesterase-4 that allows their using as medicinal agent. Invention describes also methods for preparing the compound. EFFECT: improved preparing method, valuable biochemical and medicinal properties of compounds. 11 cl, 1 tbl, 4 ex