[EN] IMIDAZO-PYRAZOLES AS GPR119 INHIBITORS<br/>[FR] IMIDAZO-PYRAZOLES COMME INHIBITEURS DU GPR119
申请人:PFIZER
公开号:WO2011061679A1
公开(公告)日:2011-05-26
Compounds of formula (I) wherein: X is (A) or (B); Y is O or a bond; R1 is -C(O)-O-R3 or R2 is hydrogen, cyano, C1-C6 alkyl, or C3-C6 cycloalkyl; R5 is hydrogen, cyano, nitro, C1-C6 fluoroalkyl, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 fluoroalkoxy, or C3-C6 cycloalkyl; R6 is hydrogen, C1-C6 alkyl, C3-C6 cycloalkyl, -C(O)-NH2, or C1-C6 alkyl substituted with hydroxy or C1- C6 alkoxy; m is 1 or 2, wherein when m is 1 then R8 is hydrogen, C1-C6 alkyl, -CH2-(C1- C5)haloalkyl, C3-C6 cycloalkyl, or C1-C6 alkyl substituted with hydroxy; and when m is 2 then each R8 is independently C1-C3 alkyl or -CH2-(C1-C2)haloalkyl; modulate the activity of the G-protein-coupled receptor GPR119 and their uses in the treatment of diseases linked to the modulation of the G- protein-coupled receptor GPR119 in animals are described herein.
式(I)的化合物中:X为(A)或(B);Y为O或键;R1为-C(O)-O-R3或R2为氢、氰基、C1-C6烷基或C3-C6环烷基;R5为氢、氰基、硝基、C1-C6氟代烷基、C1-C6烷基、C1-C6烷氧基、C1-C6氟代烷氧基或C3-C6环烷基;R6为氢、C1-C6烷基、C3-C6环烷基、-C(O)-NH2或C1-C6烷基取代的羟基或C1-C6烷氧基;m为1或2,当m为1时,则R8为氢、C1-C6烷基、-CH2-(C1-C5)卤代烷基、C3-C6环烷基或C1-C6烷基取代的羟基;当m为2时,则每个R8独立地为C1-C3烷基或-CH2-(C1-C2)卤代烷基;调节G蛋白偶联受体GPR119的活性及其在治疗与动物体内G蛋白偶联受体GPR119调节相关疾病中的用途。