DERIVATIVES OF (AZETHIDINE-1-YLALKYL)-LACTAMES, PHARMACEUTICAL COMPOSITION BASED ON THEREOF AND METHOD OF TREATMENT OF HUMANS WHEN PATIENTS ARE TREATED BY PRODUCING ANTAGONISTIC EFFECT ON TACHYKININ ACTING IN HUMAN NK₁-, NK₂- AND NK₃-RECEPTORS OR IN THEIR COMBINATION

摘要

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to derivatives of (azethidine-1-ylalkyl)-lactames of the formula (I) and their pharmaceutically acceptable salts where R is (C₁-C₆)-alkyl optionally substituted with -COOH, -COO((C₁-C₄)-alkyl), (C₃-C₇)-cycloalkyl, aryl or Het¹ and indicated (C₃-C₇)-cycloalkyl is optionally substituted with 1-2 substituents taken among (C₁-C₄)-alkyl and fluorine atom; R¹ is phenyl optionally substituted with 1-2 halogen-substituents; R² is -CONR³R⁴, -CONR⁵((C₃-C₇)-cycloalkyl), -NR³R⁴, Het³ or the group of the formula (a), (b), (c); X means (C₁-C₄)-alkylene; X¹ means directed bond X² means directed bond or CO; m = 1. Compounds are used for treatment of patients by producing antagonistic effect on tachykinin acting in human NK₁-, NK₂- and NK₃--receptor or in their combination. Invention proposes also intermediate compounds used in their synthesis, pharmaceutical composition and method of treatment of patients. EFFECT: improved method of treatment, valuable pharmacological properties. 17 cl, 1 dwg, 27 tbl, 316 ex