| 摘要 |
The invention relates to therapeutic benzamide compounds of formula (I) wherein A represents N or CH; X is selected from the following groups: (i) - C1- 6alkylene-, optionally containing one or two double bonds and optionally substituted by one or more hydroxy, C1-6 alkyl, C1-6 alkoxy, C1-6acyl or C1- 6acyloxy groups, (ii) oxo, sulfonyl, thioxo, (iii) -C1-6alkylenecarbonyl-, - C1- 6alkylenesulfonyl-, -C1-6alkylenethioxo-, (iv) -C2-6alkyleneoxy-, -C2- 6alkylenethio-, -C2-6alkylene(N-H or N-C1-6alkyl)amino-, (v) -C1- 6alkylenecarboxy-, -C1-6alkylenethioamido-, -C1-6alkylene(N-H or N-C1- 6alkyl)carboxamido-, and (vi) -C2-6alkyleneoxycarbonyl-, -C2- 6alkylenethiocarbonyl-, -C2-6 alkylene(N-H or N-C1-6alkyl)aminocarbonyl-; Z represents a direct link or -C1-6 alkylene-, optionally containing one doubl e bond and optionally substituted by one or more hydroxy, C1-6 alkyl, C1-6 alkoxy, C1-6 acyl or C1-6 acyloxy groups; R1 is selected from the following groups: (i) hydrogen, C1-3perfluoroalkyl, (ii) C6-10 aryl, C3-8cycloalkyl an d fused benz derivatives thereof, C7-10polycycloalkyl, C4-8cycloalkenyl, C7- 10polycycloalkenyl, (iii) a heterocyclyl selected from the group consisting of monocyclic radicals and fused polycylic radicals, and (iv) where either X is C1-6alkylene and Z is a direct link, or Z is C1-6alkylene, R1 additionally m ay represent a halogen, cyano, nitro or C1-6acyl group, wherein, when R1 contai ns one or more rings, said rings may each independently bear 0 to 4 substituent s. Y represents a direct or oxy link, -C1-6alkylene-, -oxyC1-6alkylene- or a heterocyclyl consisting of monocyclic radicals. R2 represents phenyl, C3- 8cycloalkyl, or a heterocyclyl consisting of monocyclic radicals, and where each R2 is optionally substituted by one or more groups independently select ed from halogen, C1-4alkyl, C1-4alkoxy, C3-8cycloalkyl, C1-3perfluoroalkyl, C1- 4perfluoroalkoxy, hydroxycarbonyl, C1-6alkoxycarbonyl, cyano, nitro, C1- 4alkylaminosulfonyl; R3 represents hydrogen or one or more groups independently selected from halogen, C1-4alkyl, C1-4alkoxy, C1-3 perfluoroalkyl or C1-3 perfluoroalkoxy; or a physiologically acceptable salt , solvate or derivative thereof, pharmaceutical compositions, to processes for their preparation and their use in the treatment of conditions mediated by ApoB-100 regulation.
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