Aniline derivative having polyunsaturated fatty acid residue and

Details Aniline derivative having polyunsaturated fatty acid residue and Aniline derivative having polyunsaturated fatty acid residue and

1996-02-07

1998-09-01

Bernhardt, Emily

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514596, 514598, 514627, 544388, 554 35, 554 56, 554 58, 554 62, 554 65, 554 67, A61K 31495, A61K 31165, C07C23309, C07D295185

Patent

active

058011781

ABSTRACT:
An aniline derivative of the formula (1) ##STR1## wherein R.sup.1 is an eicosapentaenoyl or docosahexaenoyl; R.sup.2 and R.sup.3 are each independently an alkyl or alkoxy having 1 to 6 carbon atoms, or a halogen atom; R.sup.4 is a hydrogen atom, an alkyl or alkoxy having 1 to 6 carbon atoms, or a halogen atom; and A is a single bond, --C(.dbd.O)NH--(CH.sub.2).sub.n --NH-- wherein n is 2 or 3, or a bivalent group of the following formula ##STR2## wherein m and p are each independently 0 or 1. The aniline derivative of the present invention has high inhibitory activity against and high selectivity for ACAT derived from macrophage and is useful as an agent for the prophylaxis and treatment of arteriosclerosis.

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Roth et al., Inhibitors of Acyl-CoA:Cholesterol Acyltransferase. 1. Identification and Structure-Activity Relationships of a Novel Series of Fatty Acid Anilide Hypocholesterolemic Agents; J. Med. Chem. 1992, 35, 1609-1617.
Protein, Nucleic Acid and Enzyme, vol. 39, No. 9, 1532-1547 (1994) (Article Not Translated).
Roark et al., Inhibitors of Acyl-CoA: Cholesterol Acyltransferase (ACAT). 2. Modification of Fatty Acid Anilide ACAT Inhibitors: Bioisosteric Replacement of the Amide Bond, Journal of Medicinal Chemistry, vol. 36, No. 11, May 28, 1993, pp. 1662-1668.

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