ACETAMIDE DERIVATIVE AND ITS USE

PROBLEM TO BE SOLVED: To obtain the novel subject acetamide derivative which has a strong cholesterol acyl transferase (Co-A) inhibitory action, particularly high effective for arteriosclerosis. SOLUTION: This acetamide derivative is represented by formula I [R1 and R2 are H, a halogen, a lower alhy...

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Hauptverfasser: MAEDA KOJI, YAMAGUCHI KATSUSHI, SUZUKI TOMOO, FUCHIGAMI MASAHIRO, KATOU NORIYASU, KIMURA HIROMOTO, MITANI TAKAHIKO, TASHIMO SATOSHI
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Sprache:eng
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Zusammenfassung:PROBLEM TO BE SOLVED: To obtain the novel subject acetamide derivative which has a strong cholesterol acyl transferase (Co-A) inhibitory action, particularly high effective for arteriosclerosis. SOLUTION: This acetamide derivative is represented by formula I [R1 and R2 are H, a halogen, a lower alhyl, a lower alkoxy; X is a single bond, O, s, -CH=CH-, -N=CH-; Y is a single bond, >C=O, >CH-R3 (R3 is a lower alkyl); m is 0-4; n is 0 or 1], typically 3, 4-dihydro-N-(2,6-diisopropylphenyl)-1(2H)- quinolineacetoamide. The compound is prepared, for example, by formulating compounds of formula II and formula III at a molar ratio of 1/2-2/1 and allowing them to react with each other in a solvent such as toluene at a temperature of -70-+150 deg.C. The daily dose of this compound is usually about 0.1-100mg in the case of oral administration.