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    • 6. 发明申请
    • IMIDAZO-PYRAZOLES AS GPR119 INHIBITORS
    • 作为GPR119抑制剂的咪唑并吡唑
    • WO2011061679A1
    • 2011-05-26
    • PCT/IB2010/055194
    • 2010-11-16
    • PFIZER INC.MASCITTI, VincentMCCLURE, Kim FrancisMUNCHHOF, Michael JohnROBINSON, Ralph Pelton
    • MASCITTI, VincentMCCLURE, Kim FrancisMUNCHHOF, Michael JohnROBINSON, Ralph Pelton
    • C07D487/04A61K31/506
    • C07D487/04
    • Compounds of formula (I) wherein: X is (A) or (B); Y is O or a bond; R 1 is -C(O)-O-R 3 or R 2 is hydrogen, cyano, C 1 -C 6 alkyl, or C 3 -C 6 cycloalkyl; R 5 is hydrogen, cyano, nitro, C 1 -C 6 fluoroalkyl, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, C 1 -C 6 fluoroalkoxy, or C 3 -C 6 cycloalkyl; R 6 is hydrogen, C 1 -C 6 alkyl, C 3 -C 6 cycloalkyl, -C(O)-NH 2 , or C 1 -C 6 alkyl substituted with hydroxy or C 1 - C 6 alkoxy; m is 1 or 2, wherein when m is 1 then R 8 is hydrogen, C 1 -C 6 alkyl, -CH 2 -(C 1 - C 5 )haloalkyl, C 3 -C 6 cycloalkyl, or C 1 -C 6 alkyl substituted with hydroxy; and when m is 2 then each R 8 is independently C 1 -C 3 alkyl or -CH 2 -(C 1 -C 2 )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)化合物,其中:X为(A)或(B); Y是O或键; R 1是-C(O)-O-R 3或R 2是氢,氰基,C 1 -C 6烷基或C 3 -C 6环烷基; R5是氢,氰基,硝基,C1-C6氟代烷基,C1-C6烷基,C1-C6烷氧基,C1-C6氟烷氧基或C3-C6环烷基; R 6是氢,C 1 -C 6烷基,C 3 -C 6环烷基,-C(O)-NH 2或被羟基或C 1 -C 6烷氧基取代的C 1 -C 6烷基; m为1或2,其中当m为1时,R 8为氢,C 1 -C 6烷基,-CH 2 - (C 1 -C 5)卤代烷基,C 3 -C 6环烷基或被羟基取代的C 1 -C 6烷基; 当m为2时,各R 8独立地为C 1 -C 3烷基或-CH 2 - (C 1 -C 2)卤代烷基; 调节G蛋白偶联受体GPR119的活性及其用于治疗与动物中G-蛋白偶联受体GPR119的调节相关的疾病。