Patent RU-2569298-C2 (RU)
Inventor: BIAN Khajan
IPC: C07D495/04
Filed: 2010-04-22
Granted: 2015-11-20
Abstract: 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 Caryl; ii) Ccycloalkyl, 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 Caryl is substituted, and heteroaryl is optionally substituted with one substituent, selected from the group, consisting of fluorine, chlorine, bromine, Calkyl, Calkoxy and Calkylcarbonylamino; group b) represents i)Caryl; 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 Caryl, 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, Calkyl, Calkoxy and trifluoromethyl; and where Caryl and heteroaryl are substituted with one additional substituent, selected from the group, consisting of i) C-aryl; 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 Caryl and heteroaryl are optionally independently substituted with one or two substituents, selected from the group, consisting of Calkyl; cyanomethyl; Calkoxy; from one to three substituents, representing fluorine or chlorine; trifluoromethy; trifluoromethoxy; Calkylcarbonyl; Calkoxycarbonyl(C)alkenyl; cyano(C)alkenyl; (2-cyano)ethylaminocarbonyl; cyano; carboxy; aminocarbonyl, formyl, nitro, bromine, hydroxyl; and NRR, in which Rrepresents hydrogen or Calkyl and in which Rrepresents hydrogen,Calkyl, di(Calkyl)aminosulphonyl and Calkylsulphonyl; s equals 0, 1 or 2; Rrepresents Caryl, Calkyl; 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