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公开(公告)号：EP0428385A1
公开(公告)日：1991-05-22
申请号：EP90312382.6
申请日：1990-11-13
IPC分类号： C07C271/40 , C07D295/205 , A61K31/325 , A61K31/33
CPC分类号： C07D295/205 , C07C271/40 , C07C2601/14 , C07C2603/93
摘要： 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.摘要翻译： 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。
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公开(公告)号：EP0283168A3
公开(公告)日：1989-06-14
申请号：EP88301853.3
申请日：1988-03-03
IPC分类号： C07D303/48 , A61K31/335
CPC分类号： C07D303/48
摘要： There are disclosed compounds of the formula
wherein R¹ and R² are each, independently, hydrogen, hydroxy, lower alkyl, lower alkoxy, haloloweralkyl, haloloweralkyl sulfonyl, halo or nitro;
R³ is hydrogen, lower alkyl, or aryl or 7-12 carbon atoms;
A is -CH₂-, -O- or -S-;
m is 1 - 8;
n is 0 - 7, with the proviso that m + n ≦ 8;
or a pharmacologically acceptable salt thereof, and their use as fatty acid oxidation inhibitors possessing a significantly reduced potential for impairment of normal cardiac function, and having particular utility in the treatment of glucose and fatty acid metabolism disorders, such as diabetes.-
公开(公告)号：EP0283168A2
公开(公告)日：1988-09-21
申请号：EP88301853.3
申请日：1988-03-03
IPC分类号： C07D303/48 , A61K31/335
CPC分类号： C07D303/48
摘要： There are disclosed compounds of the formula
wherein R¹ and R² are each, independently, hydrogen, hydroxy, lower alkyl, lower alkoxy, haloloweralkyl, haloloweralkyl sulfonyl, halo or nitro;
R³ is hydrogen, lower alkyl, or aryl or 7-12 carbon atoms;
A is -CH₂-, -O- or -S-;
m is 1 - 8;
n is 0 - 7, with the proviso that m + n ≦ 8;
or a pharmacologically acceptable salt thereof, and their use as fatty acid oxidation inhibitors possessing a significantly reduced potential for impairment of normal cardiac function, and having particular utility in the treatment of glucose and fatty acid metabolism disorders, such as diabetes.摘要翻译： 公开了式CHEM的化合物，其中R 1和R 2各自独立地为氢，羟基，低级烷基，低级烷氧基，卤代低级烷基，卤代烷基磺酰基，卤素或硝基; R 3是氢，低级烷基或芳基或7-12个碳原子;
A是-CH 2 - ， - O-或-S-; m为1〜8; n为0-7，条件是m + n = 8; 或其药理学上可接受的盐，以及它们作为脂肪酸氧化抑制剂的用途，具有显着降低正常心脏功能损害的潜力，并且在治疗葡萄糖和脂肪酸代谢紊乱如糖尿病中具有特别的用途。
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