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    • 4. 发明申请
    • OXADIAZOLE DERIVATIVES AS DGAT INHIBITORS
    • 氧化氮衍生物作为DGAT抑制剂
    • WO2009024821A3
    • 2009-04-09
    • PCT/GB2008050716
    • 2008-08-15
    • ASTRAZENECA ABASTRAZENECA UK LTDBIRCH ALAN MARTINBUTLIN ROGER JOHNGILL ADRIAN LIAMGROOMBRIDGE SAMUEL DAVIDPLOWRIGHT ALLEYNWARING MICHAEL JAMES
    • BIRCH ALAN MARTINBUTLIN ROGER JOHNGILL ADRIAN LIAMGROOMBRIDGE SAMUEL DAVIDPLOWRIGHT ALLEYNWARING MICHAEL JAMES
    • C07D413/12A61K31/4245A61P3/00
    • C07D413/12
    • Compounds of formula (I), or pharmaceutically-acceptable salts and/or pro-drugs thereof, which inhibit acetyl CoA(acetyl coenzyme A):diacylglycerol acyltransferase (DGAT1) activity are provided, wherein n is 0 to 3; p is 0 or 1; q is 0 to 2; R1and R2are, for example, independently fluoro, chloro, bromo, cyano or (1-4C)alkyl; X is -O-, -S- or -NRa- wherein Ra is hydrogen or (1-4C)alkyl; RA1 and RA2 are, for example, independently hydrogen or (1-4C)alkyl; Ring A is a di-linked ring or ring system chosen from (4-6C)cycloalkane, (7- 10C)bicycloalkane and (8-12C)tricycloalkane each optionally substituted, for example, by one substituent selected from (1-4C)alkyl, (1-4C)alkoxy and (1-4C)alkoxy(1-4C)alkyl; or Ring A is phenylene optionally substituted, for example, by up to four substituents selected from fluoro, chloro, bromo, cyano, (1-4C)alkyl, (1-4C)alkoxy and (1- 4C)alkoxy(1-4C)alkyl; togetherwith processes for their preparation, pharmaceutical compositions containing them and their use as medicaments.
    • 提供了抑制乙酰CoA(乙酰辅酶A):二酰基甘油酰基转移酶(DGAT1)活性的式(I)化合物或其药学上可接受的盐和/或前药,其中n为0-3; p为0或1; q为0〜2; R 1和R 2例如独立地为氟,氯,溴,氰基或(1-4C)烷基; X是-O - , - S-或-NRa-,其中R a是氢或(1-4C)烷基; RA1和RA2例如独立地为氢或(1-4C)烷基; 环A是选自(4-6C)环烷烃,(7-10C)双环烷烃和(8-12C)三环烷烃的二联环或环系,其各自任选被例如选自(1-4C)的一个取代基取代, 烷基,(1-4C)烷氧基和(1-4C)烷氧基(1-4C)烷基; 或环A是任选取代的亚苯基,例如至多四个选自氟,氯,溴,氰基,(1-4C)烷基,(1-4C)烷氧基和(1-4C)烷氧基(1-4C) )烷基; 以及其制备方法,含有它们的药物组合物及其作为药物的用途。