ZHANG, XUQING,HUFNAGEL, HEATHER RAE,CAI, CHAOZHONG,LANTER, JAMES,MARKOTAN, THOMAS P.,SUI, ZHIHUA
申请号：
ES10714148
公开号：
ES2539161T3
申请日:
2010.04.15
申请国别(地区):
ES
年份:
2015
代理人:
摘要：
Compound of Formula (I) ** Formula ** in which: X is F, NH2 or H； R1 is ** Formula ** pyridyl, pyridyl-N-oxide, pyridin-2-onyl, indolyl, pyrazinyl, 3-H-thiazol-2-onyl, pyrimidyl, benzooxazolyl, 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 Oalkyl C (1-4), Occycloalkyl C (3-6), OCH2CF3 , OCH2Ph, F, CN, Cl, OCF3, CF3, 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, NHCO2alkyl C (1-4), N (SO2CH3) 2, NHSO2CH3, NHC (O) CF3 , NHalkyl C (1-4), NHCO2H, NHCO2alkyl C (1-4), NHCOalkyl C (1-4), NHCONH2, NHCONHalkyl C (1-4) and Br； or said pyridyl may be substituted with an OCH3 group and a CH3； wherein said pyrimidyl is optionally substituted on any carbon atom with an N group (C (1-4) alkyl) 2； or said pyrimidinyl is substituted at any two carbon atoms with two substituents independently selected from the group consisting of OH, OCH3 and CH3； wherein said thiazolyl is substituted with CO2H, CONH2, NHCO2alkyl C (1-4) or OH； or said thiazolyl is optionally substituted at two adjacent carbon atoms to form a benzothiazol-2-yl fused bicyclic system, wherein said benzothiazol-2-yl is optionally substituted with Br or OCH3； wherein said 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 pyridin-2-onyl is substituted with 2 methyl groups； wherein said [1,2,4] oxadiazolyl is optionally substituted on any carbon atom with OH, CCl； or pyrrolidinyl； 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 Oalkyl C (1-4)； R3 is H, F, Cl, CF
