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 NK-, NK- AND NK-RECEPTORS OR IN THEIR COMBINATION Russian patent published in 2000 - IPC

Abstract RU 2150468 C1

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

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RU 2 150 468 C1

Authors

Makenzi Aleksandr Roderik

Marchington Alan Patrik

Middlton Donal'D Stjuart

Midouz Sandra Dora

Dates

2000-06-10Published

1995-07-29Filed