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Azetidinyldiamides as monoacrylic glycerol lipase inhibitors
专利权人:
JANSSEN PHARMACEUTICA N.V.
发明人:
BIAN, HAIYAN,CHEVALIER, KRISTEN M.,CONNOLLY, PETER J.,FLORES, CHRISTOPHER M.,LIN, SHU-CHEN,LIU, LI,MABUS, JOHN,MACIELAG, MARK J.,MCDONNELL, MARK E.,PITIS, PHILIP M.,ZHANG, SUI-PO,ZHANG, YUE-MEI,ZHU, B
申请号:
ES10716205
公开号:
ES2455744T3
申请日:
2010.04.22
申请国别(地区):
ES
年份:
2014
代理人:
摘要:
A compound of formula (1) ** Formula ** in which Y and Z are independently selected from a) or b) so that one of Y and Z is selected from group a) and the other is selected from group b); group a) is i) substituted C6-10 aryl, ii) C3-8 cycloalkyl optionally substituted with one to two fluorine substituents, iii) trifluoromethyl, or iv) heteroaryl selected from the group consisting of thienyl, furanyl, thiazolyl, isothiazolyl , oxazolyl, pyrrolyl, pyrimidinyl, isoxazolyl, benzothienyl, thieno [3,2-b] thiophene-2-yl, pyrazolyl, triazolyl, tetrazolyl and [1,2,3] thiadiazolyl; wherein C6-10 aryl is substituted with; and the heteroaryl is optionally substituted with; a substituent selected from the group consisting of fluorine, chlorine, bromine, C 1-4 alkyl, C 1-4 alkoxy, cyano, C 1-4 alkylcarbonylamino and trifluoromethyl; group b) is i) C6-10 aryl; ii) heteroaryl selected from the group consisting of thiazolyl, pyridinyl, indolyl, indazolyl, benzoxazolyl, benzothiazolyl, benzofuranyl, benzothienyl, 1 H -pyrrolo [3,2-b] pyridin-5-yl, 1 H -thieno [2,3- c ] pyrazol-5-yl, 1H-pyrrolo [2,3-b] pyridin-5-yl, 1H-pyrazolo [3,4-b] pyridin-5-yl, furo [2,3-b] pyridin-2 -yl, quinolinyl, quinazolinyl, furanyl, [1,2,3] triazolyl, thienyl, oxazolyl, [1,3,4] oxadiazol-2-yl, pyrrolyl, pyrazolyl and benzimidazolyl; iii) 2,3-dihydro-1H-indolyl; iv) 2,3 diphenyl indolyl; v) diphenyl imidazolyl; vi) 1- (2,4-dichlorophenyl) -4,5,6,7-tetrahydro-1H-indazol-3-yl; vii) 3- (4-chlorophenyl) -4,5,6,7-tetrahydro-indazol-2-yl; viii) 1- (4-fluorophenyl) -1H-pyrrolo [3,2-b] pyridin-6-yl; or ix) diphenyl-1H-pyrazol-3-yl; wherein each phenyl is optionally substituted with one to two chlorine substituents; and wherein said pyrazolyl is optionally substituted with a methyl substituent; wherein C6-10 aryl, 2,3-dihydro-1H-indolyl and heteroaryl of group b) are optionally independently substituted with one to two substituents selected from the group consisting of bromine, chlorine, fluorine, iodine, C1-4 alky
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