BASIC TYPE TERTIARY AMIDES, METHODS OF PREPARING THEREOF, AND PHARMACEUTICAL COMPOSITION COMPRISING SAID COMPOUNDS Russian patent published in 1998 - IPC

FIELD: pharmaceutical industry. SUBSTANCE: present invention concerns basic type tertiary amides of formula I: Ar-T-CO-NR-CH₂-CQAr′-CH₂-CH₂-Am^⊕•A^⊖, wherein Ar is mono-or biocyclic aromatic group optionally substituted by Ar alkyl, halogen, OH or (C₁-C₁₀) alkoxy: T is direct bond or (C₁-C₄) alkylene: C₁-C₅ is phenyl optionally substituted by halogen; or naphtyl; R is hydrogen, Ar′ alkyl or C₁-C₄ alkynoyloxy w-(C₂-C₄) alkyl; Q is hydrogen or Q and R together form 1,2-ethylene or 1,3- propylene; (C₂-C₄) is Am^⊕ is X₁X₂X₃N^⊕ wherein X₁, X₂, X₃ together with nitrogen atom from azabicyclic system optionally substituted by phenyl or benzyl; A^⊖ is pharmaceutically acceptable anion. The present invention also describes method of preparing compounds I by reacting compound of formula: X₁X₂X₃N with compound of formula: Ar-T-CO-NR-CH₂-QA′C-CH₂-CH₂-OY in aprotic polar solvent at temperatures ranging room temperature up to 120 C. Compounds are useful as active ingredient in pharmaceutical composition having antagonistic properties with respect to neurokinine receptors. EFFECT: improved properties of the pharmaceutical composition. 15 cl, 36 ex, 1 tbl