Claims
- 1. A quinoline derivative of the formula (I): ##STR24## wherein each phenyl ring of A and B has one or more substituents; X is ##STR25## or ##STR26## wherein R.sup.1 is a hydrogen atom, a lower alkyl group or a lower alkoxy group and R.sup.2 is a hydrogen atom or a lower alkyl group; Y is --(CH.sub.2).sub.m -- or --CH.dbd.CH-- wherein m is 0, 1 or 2; Z is a group of the formula: ##STR27## wherein the phenyl ring of Z has two to four substituents, R.sup.3 and R.sup.4 are each a hydrogen or halogen atom, or a lower alkyl, lower alkoxy, lower acyloxy, lower alkoxycarbonyloxy, N,N-di-lower alkylcarbamoyloxy, optionally esterified carboxy or hydroxyl group, R.sup.5 is a halogen atom, or a lower alkyl, lower alkoxy, lower acyloxy, lower alkoxycarbonyloxy, N,N-di-lower alkylcarbamoyloxy, optionally esterified carboxy or hydroxyl group, and n and o are each 1 or 2; l is 0 or 1, or its salt.
- 2. The compound of claim 1 wherein the phenyl ring A is substituted by one or two lower alkyl groups, the phenyl ring B is substituted by one or two halogen atoms, X is ##STR28## wherein (R.sup.1 =hydrogen atom) Y is --(CH.sub.2).sub.m -- or --CH.dbd.CH--wherein m is 0, 1 or 2, or its salt.
- 3. The compound of claim 2 wherein the phenyl ring A is substituted by two methyl groups and the phenyl ring B is substituted by a chlorine atom.
- 4. The compound of claim 1 wherein R.sup.3 is a hydroxyl group, a lower alkoxy group, a hydrogen atom or a halogen atom, R.sup.4 an R.sup.5 are a lower alkyl group, a lower alkoxy group, a hydroxyl group or a halogen atom, and o and n are 1 or 2.
- 5. The compound of claim 1 which is 4-(2-chlorophenyl)-3-(4-hydroxy-2,3,5-trimethylbenzamido)-6,8-dimethylquinoline, 4-(2-chlorophenyl)-3-(2,4-difluorophenylacetylamino)-6,8-dimethylquinoline, 4-(2-chlorophenyl)-3-(3,4-dimethoxycinnamoylamino)-6,8-dimethylquinoline, 4-(2-chlorophenyl)-3-(3,4-dihydroxycinnamoylamino)-6,8-dimethylquinoline, 4-(2-chlorophenyl)-3-(2,3-dihydroxycinnamoylamino)-6,8-dimethylquinoline, 4-(2-chlorophenyl)-3-(4-hydroxy-3,5-dimethoxycinnamoylamino)-6,8-dimethylquinoline, or a salt thereof.
- 6. An inhibitory composition for acyl-CoA: cholesterol acyltransferase which comprises an effective inhibitory amount of a compound of the formula (I) in claim 1 or a salt thereof and a pharmaceutically acceptable carrier, diluent or excipient.
- 7. The inhibitory composition of claim 6 in which the compound is 4-(2-chlorophenyl)-3-(4-hydroxy-2,3,5-trimethylbenzamido)-6,8-dimethylquinoline; 4-(2-chlorophenyl)-3-(2,4-difluorophenylacetylamino)-6,8-dimethylquinoline, 4-(2-chlorophenyl)-3-(3,4-dimethoxycinnamoylamino)-6,8-dimethylquinoline, 4-(2-chlorophenyl)-3-(3,4-dihydroxycinnamoylamino)-6,8-dimethylquinoline, 4-(2-chlorophenyl)-3-(2,3-dihydroxycinnamoylamino)-6,8-dimethylquinoline, 4-(2-chlorophenyl)-3-(4-hydroxy-3,5-dimethoxycinnamoylamino)-6,8-dimethylquinoline, or a salt thereof.
- 8. The compound of claim 2 wherein R.sup.3 is a hydroxyl group, a lower alkoxy group, a hydrogen atom or a halogen atom, R.sup.4 and R.sup.5 are a lower alkyl group, a lower alkoxy group, a hydroxyl group or a halogen atom, and o and n are 1 or 2.
Priority Claims (1)
Number |
Date |
Country |
Kind |
1-322171 |
Dec 1989 |
JPX |
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Parent Case Info
This application is a division of Ser. No. 07/646,735, filed as PCT/JP90/01617, Oct. 12, 1990, now U.S. Pat. No. 5,362,742.
US Referenced Citations (6)
Foreign Referenced Citations (1)
Number |
Date |
Country |
2116507 |
Dec 1971 |
DEX |
Divisions (1)
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Number |
Date |
Country |
Parent |
646735 |
Feb 1991 |
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