AZETIDINYL DIAMIDES AS MONOACYLGLICEROL LIPASE INHIBITORS Russian patent published in 2015 - IPC C07D205/04 C07D401/14 C07D403/12 C07D405/12 C07D405/14 C07D409/12 C07D409/14 C07D413/12 C07D413/14 C07D417/12 C07D417/14 C07D495/04 A61K31/496 A61P25/00 A61P29/00 

FIELD: chemistry.

SUBSTANCE: invention relates to formula (I) compounds, where Y and Z are independently selected from group a) or b) in such a way that one of Y or Z is selected from group a) and the other is selected from group b); group a) represents i) substituted C_6-10aryl; ii) C_3-8cycloalkyl, optionally substituted with one or two substituents, representing fluorine; iii) trifluoromethyl; or iv) heteroaryl, selected from the group, consisting of thienyl, furanyl, thiazolyl, isothiazolyl, oxazolyl, pyrrolyl, pyrimidinyl, isoxazolyl, benzothienyl, thieno[3,2-b]thiophen-2-yl, pyrazolyl, triazolyl and [1,2,3]thiadiazolyl; where C_6-10aryl is substituted, and heteroaryl is optionally substituted with one substituent, selected from the group, consisting of fluorine, chlorine, bromine, C_1-4alkyl, C_1-4alkoxy and C_1-4alkylcarbonylamino; group b) represents i)C_6-10aryl; ii) heteroaryl, selected from the group, consisting of thiazolyl, pyridinyl, indolyl, indazolyl, benzoxazolyl, benzothiazolyl, benzofuranyl, benzothienyl, 1H-pyrrolo[3,2-b]pyridin-5-yl, 1H-thieno[2,3-c]pyrazol-5-yl, 1H-pyrrolo[2,3-b]pyridine-5-yl, 1H-pyrazolo[3,4-b]pyridine-5-yl, furo[2,3-b]pyridine-2yl, furanyl, [1,2,3]triazolyl, thienyl, oxazolyl, [1,3,4]oxadiazol-2-yl, pyrrolyl, pyrazolyl and benzimidazolyl; iii) 2,3-dihydro-1H-indolyl; vi) 1-(2,4-dichlorophenyl)-4,5,6,7-tetrahydro-1H-indazol-3-yl; or ix) diphenyl-1H-pyrazol-3-yl; in which each phenyl is optionally substituted with one or two substituents, representing chlorine, and in which said pyrazolyl is optionally substituted with one substituent, representing methyl, where C_6-10aryl, 2,3-dihydro-1H-indolyl and heteroaryl from group b) are optionally independently substituted with one or two substituents, selected from the group, consisting of bromine, chlorine, fluorine, iodine, C_1-4alkyl, C_1-4alkoxy and trifluoromethyl; and where C_6-10aryl and heteroaryl are substituted with one additional substituent, selected from the group, consisting of i) C₆-₁₀aryl; ii) heteroaryl, selected from the group, consisting of thienyl, quinolinyl, pyridinyl, isoxazolyl, benzimidazolyl, pyrrolyl, furanyl and pyrazolyl; where said heteroaryl is optionally substituted with one phenyl substituent, with said phenyl substituent being optionally substituted with one or two chlorine substituents or trifluoromethyl; and where phenyl of C_6-10aryl and heteroaryl are optionally independently substituted with one or two substituents, selected from the group, consisting of C_1-4alkyl; cyanomethyl; C_1-4alkoxy; from one to three substituents, representing fluorine or chlorine; trifluoromethy; trifluoromethoxy; C_1-4alkylcarbonyl; C_1-4alkoxycarbonyl(C_2-4)alkenyl; cyano(C_2-4)alkenyl; (2-cyano)ethylaminocarbonyl; cyano; carboxy; aminocarbonyl, formyl, nitro, bromine, hydroxyl; and NR^cR^d, in which R^c represents hydrogen or C_1-6alkyl and in which R^d represents hydrogen,C_1-6alkyl, di(C_1-4alkyl)aminosulphonyl and C_1-4alkylsulphonyl; s equals 0, 1 or 2; R¹ represents C_6-10aryl, C_1-3alkyl; or its pharmaceutically acceptable salts. Formula (I) compounds are used for manufacturing pharmaceutical composition, possessing inhibiting activity with respect to monoacylglicerol lipase (MGL), containing therapeutically effective quantity of formula (I) compound and at least one pharmaceutically acceptable carrier, pharmaceutically acceptable excipient and pharmaceutically acceptable diluent.

EFFECT: compounds, intended for treatment of inflammatory pain.

20 cl, 7 tbl, 131 ex