FIELD: chemistry.
SUBSTANCE: invention relates to a compound represented by general formula (I) or a pharmaceutically acceptable salt thereof, wherein A1 is a group selected from the group consisting of the following items a) to c), where a) C6 aryl, where the ring is unsubstituted or substituted with 1 or 2 substituents independently selected from the group comprising a halogen atom, hydroxy, C1-6 alkyl, C1-6 alkoxy, halogen-C1-6 alkyl, C1-6 alkoxycarbonyl, cyano, hydroxy-C1-6 alkyl, carbamoyl, nitro, amino, C1-6 alkoxycarbonylamino-C1-6 alkyl, mono(di)C1-6 alkylamino, (C1-6 alkyl)carbonylamino, C1-6 alkylsulphonylamino and C1-6 alkylsulphonyl; b) thiazolyl, and c) a group selected from the group consisting of pyridyl, pyrimidinyl, pyrazinyl and pyridazinyl, where the ring is unsubstituted or substituted with 1 or 2 substituents independently selected from the group comprising a halogen atom, hydroxy, C1-6 alkyl, C1-6 alkoxy, halogen-C1-6 alkyl, cyano and halogen-C1-6 alkoxy; A2 is a group selected from the group including the following items d) to f), where d) C6-10 aryl, in which the ring is unsubstituted or substituted with 1 or 2 substituents independently selected from the group including: halogen atom, hydroxy, C1-6 alkyl, C1-6 alkoxy, hydroxy-C1-6 alkoxy, halogen-C1-6 alkyl, halogen-C1-6 alkoxy, cyano, amino, nitro, carboxy, (C1-6 alkyl)carbonylamino, (C1-6 alkyl) carbonyloxy, (C1-6 alkyl)carbonyl and (C7-10 aralkyloxy)carbonyl; e) a group consisting of thienyl, pyrrolyl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyranyl, pyridyl, 1-oxidopyridyl, pyridazinyl, pyrimidinyl, pyrazinyl, furazanyl, morphonyl, benzothiazolyl, isoquinolyl, quinolyl, 2,3-dihydrobenzofuranyl, imidazo[1,2-a]pyridyl, imidazo[1,2-a]pyrazinyl, benzo[1,3]dioxolyl, benzothienyl, 5,6,7,8-tetrahydroimidazo[1,2- a]pyrazinyl, where the ring is unsubstituted or substituted with 1 or 2 substituents independently selected from the group comprising a halogen atom, hydroxy, C1-6 alkyl, C1-6 alkoxy, halogen-C1-6 alkyl, halogen-C1-6 alkoxy, cyano, mono(di)C1-6 alkylamino, C1-6 alkylsulphanyl, amino, (C7-10 aralkyloxy)carbonyl, hydroxy-C1-6 alkyl, hydroxy-C1-6 alkoxy, C2-6 alkenyl, morpholino and (C1-6 alkyl)carbonyl, and f) C3-6 cycloalkyl; X is CH or N; Y is -CR1R2- or an oxygen atom; R1 and R2, independently represent a hydrogen atom, a halogen atom or C1-6 alkyl; R3 and R4, independently represent a hydrogen atom, a halogen atom, C1-6 alkyl, C1-6 alkoxy, halogen-C1-6 alkyl, halogen-C1-6 alkoxy, hydroxy-C1-6 alkoxy, C3-6 cycloalkyl, C2-6 alkenyl or cyano with the proviso that when X is CH and R1 and R2 are hydrogen atoms, R3 and R4 do not represent hydrogen atoms; and n is 1 or 2. Invention also relates to a pharmaceutical composition having inhibitory activity against TRPM8, containing a compound of formula (I) or a pharmaceutically acceptable salt thereof and a carrier.
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EFFECT: compounds of the invention are intended for the prevention or treatment of a disease or symptom caused by increased excitability or a disorder of afferent neurons, selected from the group consisting of lower urinary tract symptoms (LUTS), algia and pruritus.
16 cl, 47 tbl, 358 ex
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