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    • 6. 发明公开
    • Cholesterol ester hydrolase inhibitors
    • 胆固醇酯水解酶抑制剂
    • EP0428385A1
    • 1991-05-22
    • EP90312382.6
    • 1990-11-13
    • AMERICAN HOME PRODUCTS CORPORATION
    • Mewshaw, Richard EricCommons, Thomas JosephStrike, Donald Peter
    • C07C271/40C07D295/205A61K31/325A61K31/33
    • C07D295/205C07C271/40C07C2601/14C07C2603/93
    • The compounds of the formula:
      in which R¹ is alkyl of 4 or more carbon atoms, cycloalkyl, 1-adamantyl, 2-adamantyl, 3-noradamantyl, 3-methyl-1-adamantyl, 1-fluorenyl, 9-fluorenyl, cycloalkylalkyl, phenyl, substituted phenyl, alkyl, alkoxy, halo, nitro, cyano or trifluoromethyl, phenylalkyl or substituted phenylalkyl, where the substituent on the benzene ring is alkyl, alkoxy, halo, nitro, cyano, trifluoromethyl or phenyl; R² is hydrogen, alkyl or R¹ taken with R² and the nitrogen atom to which they are attached form a heterocyclic moiety of the formula:
      wherein
      in which R⁷ is hydrogen, alkyl, hydroxy, alkanoyloxy, hydroxyalkyl, hydroxycarbonyl, alkoxycarbonyl, phenyl or substituted phenyl, in which the substituent is alkyl, alkoxy, halo, nitro, cyano, haloalkyl, perhaloalkyl or dialkylaminoalkyl; R⁸ is hydrogen or alkyl or R⁷ and R⁸ taken together are polymethylene; R⁹ is hydrogen, alkyl, phenyl or substituted phenyl, in which the substituent is alkyl, alkoxy, halo, nitro, cyano or perhaloalkyl; R¹⁰ is hydrogen, alkyl or gemdialkyl; n is one of the integers 0, 1 or 2; and R³, R⁴, R⁵ and R⁶ are, independently, hydrogen, alkyl, alkoxy, halo, nitro, cyano or perhaloalkyl, alkoxycarbonyl or hydroxycarbonyl; and when X is -NR⁹- or R⁷ is an amino alkyl group, a pharmaceutically acceptable salt thereof; useful as inhibitors of cholesterol ester hydrolase.
    • 下式化合物:其中R 1是4个或更多个碳原子的烷基,环烷基,1-金刚烷基,2-金刚烷基,3-金刚烷基,3-甲基-1-金刚烷基,1-芴基,9-芴基,环烷基烷基, 苯基,取代的苯基,烷基,烷氧基,卤素,硝基,氰基或三氟甲基,苯基烷基或取代的苯基烷基,其中苯环上的取代基为烷基,烷氧基,卤素,硝基,氰基,三氟甲基或苯基; R 2为氢,烷基或R 1与R 2和它们所连接的氮原子一起形成下式的杂环部分:其中R 7为氢,烷基,羟基,烷酰氧基,羟烷基,羟基羰基,烷氧基羰基,苯基或取代的苯基 其中取代基是烷基,烷氧基,卤素,硝基,氰基,卤代烷基,全卤代烷基或二烷基氨基烷基; R 7是氢或烷基或R 7和R 7一起是聚亚甲基; R 7是氢,烷​​基,苯基或取代的苯基,其中取代基是烷基,烷氧基,卤素,硝基,氰基或全卤代烷基; R 10是氢,烷基或偕二烷基; n是整数0,1或2中的一个; 和R 3,R 4,R 5和R 6独立地是氢,烷基,烷氧基,卤素,硝基,氰基或全卤代烷基,烷氧基羰基或羟基羰基; 当X是-NR 8 - 或R 7是氨基烷基时,其药学上可接受的盐; 用作胆固醇酯水解酶的抑制剂。