FIELD: medicine.
SUBSTANCE: invention relates to compounds of the general formula (I) or its pharmaceutically acceptable salts having inhibiting activity relatively to phosphodiesterase 4 (hereinafter – PDE4). In the formula (I), R1 and R4 are hydrogen; R2 and R3 are independently selected from a group consisting of hydrogen or (C1-C4)alkyl; n=0, 1 or 2; Q is selected from a group consisting of -O-C(O)-R5; R5 is selected from a group consisting of (C1-C6)alkyl, (C3-C7)cycloalkyl, 4-7-element heterocycloalkyl selected from piperidinyl, tetrahydrofuranyl, azetidinyl, tetrahydropyranyl, tetrahydrothiopyranyl and dioxothianyl, heteroaryl selected from imidazolyl, pyrazolyl, oxazolyl, pyrimidinyl, pyridyl, isothiazolyl and thiazolyl, and phenyl, where the specified heteroaryl and phenyl are optionally substituted with one or more substituents selected from R6, and where the specified (C1-C6)alkyl, (C3-C7)cycloalkyl and 4-7-element heterocycloalkyl are optionally substituted with one or more substituents selected from R7; R6 consists of halogen, cyano, (C1-C4)alkyl, halo(C1-C4)alkyl, -S(O)2Rx, -S(O)2NRaRb, C(O)NRaRb, -C(O)ORa, -C(O)Rx and -ORx; R7 consists of hydroxyl, (C1-C4)alkyl, oxo, -C(O)NRaRb, -C(O)ORa, -C(O)Rx, S(O)2Rx, -ORx and -SRx; Rx consists of (C1-C6)alkyl, (C3-C6)cycloalkyl; Ra and Rb are independently selected from a group consisting of hydrogen, (C1-C4)alkyl and phenyl(C1-C4)alkyl, or Ra and Rb, together with a nitrogen atom, to which they are attached, can form 4-6-element heterocycloalkyl selected from morpholinyl, piperazinyl, pyrrolidinyl and piperidinyl, where the specified heterocycloalkyl is optionally substituted with one or more (C1-C4)alkyl or C(O)Rx. The invention also relates to a pharmaceutical composition for PDE4 inhibition containing the specified compounds, their use for the production of a pharmaceutical composition, a method for the treatment or relief of a disease, disorder or condition reacting to PDE4 inhibition, and to a method for the treatment or relief of skin diseases.
EFFECT: obtaining PDE4 inhibitors for the treatment of skin diseases.
19 cl, 17 tbl, 316 ex
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