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    • 28. 发明授权
    • Cholesterol ester hydrolase inhibitors
    • 胆固醇酯水解酶抑制剂
    • US5602151A
    • 1997-02-11
    • US572993
    • 1995-12-15
    • Richard E. MewshawThomas J. CommonsDonald P. Strike
    • Richard E. MewshawThomas J. CommonsDonald P. Strike
    • C07C271/40C07D295/205A61K31/445C07D211/06
    • C07D295/205C07C271/40C07C2101/14C07C2103/93
    • The compounds of the formula: ##STR1## in which X is ##STR2## where R.sup.7 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; R.sup.8 is hydrogen or alkyl or R.sup.7 and R.sup.8 taken together are polymethylene; R.sup.9 is hydrogen, alkyl, phenyl or substituted phenyl, in which the substituent is alkyl, alkoxy, halo, nitro, cyano or perhaloalkyl; R.sup.10 is hydrogen, alkyl or gemdialkyl; n is one of the integers 0, 1 or 2; and R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are, independently, hydrogen, alkyl, alkoxy, halo, nitro, cyano or perhaloalkyl, alkoxycarbonyl or hydroxycarbonyl; and when X is --NR.sup.9 -- or R.sup.7 is an amino alkyl group, a pharmaceutically acceptable salt thereof; are useful as inhibitors of cholesterol ester hydrolase.
    • 其中X为的化合物,其中R 7为氢,烷基,羟基,烷酰氧基,羟基烷基,羟基羰基,烷氧基羰基,苯基或取代的苯基,其中取代基为烷基,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; R8是氢或烷基或R7和R8一起是聚亚甲基; R9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; R10为氢,烷基或偕二烷基; n是整数0,1或2之一; 并且R 3,R 4,R 5和R 6独立地为氢,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-NR9-或R7是氨基烷基时,其药学上可接受的盐; 可用作胆固醇酯水解酶的抑制剂。