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    • 1. 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。
    • 2. 发明授权
    • Cholesterol ester hydrolase inhibitors
    • 胆固醇酯水解酶抑制剂
    • US5512565A
    • 1996-04-30
    • US413559
    • 1995-03-30
    • Richard E. MewshawThomas J. CommonsDonald P. Strike
    • Richard E. MewshawThomas J. CommonsDonald P. Strike
    • C07C271/40C07D295/205A61K31/54C07D279/12
    • C07D295/205C07C271/40C07C2101/14C07C2103/93
    • The compounds of the formula: ##STR1## in which ##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R7是氢,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; 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。
    • 6. 发明授权
    • Cholesterol ester hydrolase inhibitors
    • 胆固醇酯水解酶抑制剂
    • US5391571A
    • 1995-02-21
    • US62026
    • 1993-05-13
    • Richard E. MewshawThomas J. CommonsDonald P. Strike
    • Richard E. MewshawThomas J. CommonsDonald P. Strike
    • C07C271/40C07D295/205A61K31/325C07C271/02
    • C07D295/205C07C271/40C07C2101/14C07C2103/93
    • The compounds of the formula: ##STR1## in which R.sup.1 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; R.sup.2 is hydrogen, alkyl or R.sup.1 taken with R.sup.2 and the nitrogen atom to which they are attached form a heterocyclic moiety of the formula: ##STR2## wherein ##STR3## in which 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, R5 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; useful as inhibitors of cholesterol ester hydrolase.
    • 下式的化合物:其中R1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-降金刚烷基,3-甲基-1-金刚烷基,1-芴基,9-芴基 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是烷基,烷氧基,卤素,硝基,氰基,三氟甲基或苯基; R 2是氢,烷基或R 1与R 2取代,并且与它们相连的氮原子形成下式的杂环部分:其中R7是氢,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; 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。