FIELD: organic chemistry, pharmacy. SUBSTANCE: invention describes amides of the formula (I) where X means CH2, CO, CS or SO2; Y is taken among of: direct bond, aliphatic hydrocarbylene radicals containing up to 20 carbon atoms that can be monosubstituted with hydroxy-group, (C1-C10)-alkoxy, (C1-C10)-acyl, (C1-C10)-acyloxy or (C6-C10)-aryl, NH and O at condition that if X means CH2 then Y means the direct bond; Z is taken among of the following groups: (1) H, halogen atom, cyano-group; (2) hydroxy-group, (C1-C10)-alkoxy, (C1-C10)-alkylthio, (C1-C10)-acyl, thiophenylcarbonyl, (C1-C10)-alkoxycarbonyl; (3) di-(C1-C10)-alkylamino, (C6-C10)-aryl-(C1-C10)-alkylamino at condition that Y can not be O or NH; (4) unsubstituted vinyl, (C6-C10)-aryl, (C3-C8)-cyclo-alkyl and their condensed benzoderivatives, (C7-C10)-polycyclo-alkyl, (C4-C8)-cycloalkenyl, (C7-C10)-polycycloalkenyl; (5) (C6-C10)-aryl-thio, (C6-C10)-aryl-(C1-C10)-alkoxy, (C6-C10)-aryl-(C1-C10)-alkylthio, (C3-C8)-cyclo-alkyloxy, (C4-C8)-cycloalkenyloxy; (6) heterocycle taken among of the group containing monocyclic radicals and condensed polycyclic radicals where indicated radicals have from 5 to 10 ring atoms where indicated radicals have from 1 to 4 ring heteroatoms taken independently among of oxygen, nitrogen and sulfur atoms and where separate rings of indicated radicals can be independently saturated, partially saturated or aromatic at condition that if X means CH2, Z means H or taken among of the group (4) and (6) where Z has one or more rings then each of indicated rings can has independently from 0 to 4 substituents taken independently among of halogen atom, hydroxy, cyano, nitro, oxo, thiooxo, aminosulfonyl, phenyl, phenoxy, phenylthio, halogenphenylthio, benzyl, benzyloxy, (C1-C10)-alkyl, (C1-C10)-alkoxy, -alkoxycarbonyl, (C1-C10)-alkylamino-carbonyl, di-(C1-C10)-alkylamino, di-(C1-C10)-alkylaminocarbonyl, di-(C1-C10)-alkylamino-(C1-C10)-alkoxy, (C1-C3)-perfluoroalkyl, (C1-C10)-acyl, (C1-C10)-acyloxy, (C1-C10)-acyloxy-(C1-C10)-alkyl and pyrrolidinyl, and its pharmaceutically acceptable salts. Compounds decrease the secretion of apolipoprotein B in mammals and can be used for treatment of atherosclerosis. EFFECT: enhanced curative effectiveness of compounds. 37 cl, 1 tbl, 197 ex
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Authors
Dates
1999-11-20—Published
1996-06-06—Filed