申请人:AMERICAN HOME PRODUCTS CORPORATION
公开号:EP0428385A1
公开(公告)日:1991-05-22
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.
式中的化合物
其中 R¹ 为 4 个或 4 个以上碳原子的烷基、环烷基、1-金刚烷基、2-金刚烷基、3-正金刚烷基、3-甲基-1-金刚烷基、1-芴基、9-芴基、环烷基、苯基、取代苯基、烷氧基、卤代、硝基、氰基或三氟甲基、苯基烷基或取代苯基烷基,其中苯环上的取代基为烷氧基、卤代、硝基、氰基或三氟甲基、烷基、烷氧基、卤代、硝基、氰基或三氟甲基、苯基烷基或取代苯基烷基,其中苯环上的取代基为烷基、烷氧基、卤代、硝基、氰基、三氟甲基或苯基;R² 是氢、烷基或 R¹ 与 R² 及其所连接的氮原子形成式中的杂环分子:
其中
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、苯基或取代苯基,其中取代基是烷基、烷氧基、卤代、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 合在一起是聚亚甲基;R⁹ 是氢、烷基、苯基或取代苯基,其中取代基是烷基、烷氧基、卤代、硝基、氰基或高卤烷基;R¹⁰ 是氢、烷基或二烷基;n 是整数 0、1 或 2 之一;以及 R³、R⁴、R⁵ 和 R⁶ 独立地是氢、烷基、烷氧基、卤代、硝基、氰基或高卤烷基、烷氧基羰基或羟基羰基;当 X 为-NR⁹- 或 R⁷ 为氨基烷基时,其药学上可接受的盐;可用作胆固醇酯水解酶的抑制剂。