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CCR2 4-azetidinyl-1-heteroaryl cyclohexanol antagonists
专利权人:
Janssen Pharmaceutica N.V.
发明人:
ZHANG, Xuqing,HUFNAGEL, Heather Rae,HOU, Cuifen,JOHNSON, Dana L.,SUI, Zhihua,FEGELY, Barry,BRESLIN, David
申请号:
ES09768584
公开号:
ES2555004T3
申请日:
2009.12.09
申请国别(地区):
ES
年份:
2015
代理人:
摘要:
Compound of Formula (I) ** Formula ** in which: R1 is ** Formula ** pyridyl, pyridyl-N-oxide, 1H-pyridin-2-onyl, indolyl, pyrazinyl, 3-H-thiazol-2- onyl, pyrimidyl, benzoxazolyl, oxazolyl, thiazolyl, isothiazolyl, pyrazolyl, imidazolyl, thiophenyl, furyl, [1,2,4] oxadiazolyl or [1,3,4] thiadiazolyl; wherein said pyridyl, pyridyl-N-oxide, pyrimidyl, pyrazolyl, imidazolyl, thiophenyl or thiazolyl is optionally substituted with a substituent selected from the group consisting of OalkylC (1-4), OccycloalkylC (3-6), OCH2CF3, OCH2Ph , F, CN, CH2CN, C (1-4) alkyl, CH2CF3, N (C (1-4) alkyl) 2, C (1-4) alkyl OH, Si (CH3) 3, -C≡CH, SCH3, S ( O) CH3, SO2CH3, pyrrolidinyl, OH, NH2, NHCN, CO2H, CONH2, NHCO2alkylC (1-4), N (SO2CH3) 2, NHSO2CH3, NHC (O) CF3, NHalkylC (1-4), NHCO2H, NHCO2alkylC ( 1-4), NHCOalkylC (1-4), NHCONH2, NHCONHalkylC (1-4) and Br; or said pyridyl may be substituted with an OCH3 group and a CH3; or wherein said pyrimidyl is optionally substituted with an N group (C (1-4) alkyl) 2 or one or two OCH3 groups; or wherein said thiazolyl is optionally substituted at two adjacent carbon atoms to form the benzothiazol-2-yl fused bicyclic system, or wherein said benzothiazol-2-yl is optionally substituted with Br or OCH3; or wherein said 1H-pyridin-2-onyl is optionally substituted with a substituent selected from the group consisting of CH2CN, C 1-4 alkyl, CH2CF3, and CH2CH2OH, or said 1H-pyridin-2-onyl may optionally be substituted with up to 2 methyl groups; or wherein said [1,2,4] oxadiazolyl is optionally substituted on any carbon atom with CCl3, or pyrrolidinyl, or alternatively both hydrogens on said carbon atom of said [1,2,4] oxadiazolyl may be substituted by an oxo group; R2 is C (1-4) alkyl, NH2, NO2, NHCH2CH2OH, N (C (1-4) alkyl) 2, N (SO2CH3) 2, CN, F, Cl, Br, CF3, C (3-6) cycloalkyl, heterocyclyl , OCF3, OCF2H, CF2H, or OalkylC (1-4); R3 is H, F, Cl, CF3, or OalkylC (1-4); alternatively, R2 and R3 can form, together with the phenyl to which they are atta
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