DERIVATIVES OF UREA, METHOD OF SYNTHESIS OF UREA DERIVATIVES, PHARMACEUTICAL COMPOSITION SHOWING INHIBITING ACTIVITY WITH RESPECT TO COA : CHOLESTEROL ACYLTRANSFERASE

摘要

FIELD: organic chemistry. SUBSTANCE: product: derivatives of urea of the formula (I): where: n = 1, 2; O - oxygen; X, Y - oxygen, sulfur; A - C₄ - C₇-aliphatic hydrocarbon chain, cyclopentyl, cyclohexyl, pyridyl, phenyl that can be substituted with C₁ - C₄-alkyl, di-C₁ - C₄-dialkylamine, halogen or methylenedihydroxy-group; or A - phenyl substituted with two adjacent substituents forming methylenedihydroxy-group possibly substituted with 1-3 C₁ - C₄-alkyls; or A - phenyl substituted with imidazolyl that can be substituted with C₁ - C₆-alkyl; C₁ - C₄ and R₁ - R₂-alkyl or they together mean C₁ - C₆-alkylene chain possibly substituted with 1-2 C₂ - C₄-alkyls; B - phenyl substituted with 1-2 substituents taken from the group involving halogen, C₁ - C₄-alkyl as separate isomers or their mixture, or their pharmaceutically acceptable salts. Synthesis: interaction of reagent 1: C₁ - C₄ and reagent 2: B - N=C=Q followed by conversion to salt, if necessary. Pharmaceutical composition inhibiting activity of enzyme CoA: cholesterol acyltransferase and containing carrier or vehicle and compound of the formula (I) taken at effective dose. Synthesized compounds were used in pharmaceutical industry. EFFECT: improved method of synthesis. 7 cl, 3 tbl