ANTAGONISTS OF ENDOTHELIAL RECEPTORS, PHARMACEUTICAL COMPOSITION, METHOD OF SYNTHESIS, METHOD OF INHIBITION OF ENDOTHELIAL RECEPTORS

摘要

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention describes new indane- and indene-derivatives that are antagonists of endothelial receptors. Derivatives have a general formula (I): where R₁ is -X(CH₂)_n--Ar or -X(CH₂)_nCO₂H (tetrazole); R₂ is Ar; P₁,P₂ are X(CH₂)_nCO₂H or -X(CH₂)_n-tetrazole; Z₁,Z₂,Z₃ are H, OH, C_1-8-alkoxy, N(R₆)₂,NHCOR₆,, phenyl, benayl; R₆ is H or lower alkyl. Invention describes also a method of their synthesis by an interaction of the corresponding ester and organomagnesium compound, pharmaceutical composition and a method of endothelial receptor blocking. EFFECT: improved method of synthesis, enhanced effectiveness of compounds. 12 cl, 85 ex, 1 tbl