FIELD: pharmaceutics.
SUBSTANCE: invention relates to a compound of general formula (1), or a pharmacologically acceptable salt thereof, where R3 denotes a hydrogen atom, R4 denotes 5–6-membered monocyclic heterocyclic group, containing from 1 to 4 heteroatoms selected from an oxygen atom, a nitrogen atom and a sulfur atom, selected from thiazole (optionally substituted with methyl), furan, pyrazole (optionally substituted with methyl), pyridine (optionally substituted with fluorine), oxazole, isothiazole, 1,2,4-thiadiazole and pyrimidine; X denotes a group described by the following formula: -CH2-, -CH2-CH2-, -CH2-CH2-CH2- or -CH2-O-CH2-; Z denotes a hydrogen atom or a hydroxy group; R1 is selected from (i) a hydrogen atom, a halogen atom, a hydroxy group, a carboxy group, a cyano group, a sulfamoyl group and an aminocarbonyl group; and (ii) a C1-6 alkyl group; C3-7 cycloalkyl group; thiazole; tetrahydrofuran, thiomorpholine and piperidine; C1-6 acylamino groups; C1-6 alkyloxy groups; C1-6 alkyloxy-C1-6 alkyl group; C3-7 cycloalkyloxy group; 6-member monocyclic aromatic heterocyclyloxy group containing 1 heteroatom selected from an oxygen atom; C1-6 alkylthio group; C1-6 alkylsulphonyl group; C1-6 alkylsulphinyl group; mono-C1-6 alkylsulfamoyl group, di-C1-6 alkylsulfamoyl group; di-C1-6 alkylsulfamoyl group, in which two C1-6 alkyl groups can form a pyrrolidin-1-yl group or a morpholine group with an adjacent nitrogen atom; C1-6 alkylcarbonyl group and C1-6 alkyloxycarbonyl group; each of which is optionally substituted with 1–6 substitutes; and R2 is selected from (i) a hydrogen atom, a halogen atom, a hydroxygroup, a carboxygroup, a cyanogroup, a sulfamoyl group and an aminocarbonyl group; and (ii) a C1-6 alkyl group; C1-6 acylamino groups; C1-6 alkyloxy groups; C2-6 alkenyloxy groups; C1-6 alkyloxy-C1-6 alkyl group; C3-7 cycloalkyloxy group; C1-6 alkylthio group; C1-6 alkylsulphonyl group; C1-6 alkylsulphinyl group; mono-C1-6 alkylsulfamoyl group; di-C1-6 alkylsulfamoyl group; C1-6 alkylcarbonyl group and C1-6 alkyloxycarbonyl group. Invention also relates to a pharmaceutical composition having PDE4 inhibitory activity, comprising an effective amount of at least one component selected from a group consisting of a compound of formula I and a pharmacologically acceptable salt thereof as an active ingredient, and at least one component selected from a group consisting of an inert filler, a disintegrant, a binder, a lubricant and a dye.
EFFECT: novel compound and a pharmacologically acceptable salt thereof are disclosed.
6 cl, 69 tbl, 421 ex
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