NEW AZETIDINE COMPOUNDS Russian patent published in 2009 - IPC C07D205/04 C07D417/02 A61K31/397 A61K31/54 A61P9/00 A61P25/00 

FIELD: chemistry, pharmacology.

SUBSTANCE: present invention relates to new azetidine compounds with general formula (I): where Het is piperadino, substituted with hydroxyl, oxo, cyano, 1,3-dioxolan-2-yl, fluorine atom; or Het is morpholino or thiomorpholino, possibly substituted on its sulphur atom with one or two oxygen atoms; or Het is piperazino, substituted on its nitrogen atom in position 4 with C₁-C₄alkyl, C₃-C₄cycloalkyl or C₁-C₄acyl; R1 represents hydrogen; R2 represents fluoro, bonded in position four; R3 is hydrogen; R4 is C₁-C₄alkyl or C₃-C₄cycloalkyl; Ar is phenyl, substituted in its positions 3 and 5 with groups, independently chosen from halogen and C₁-C₄alkyl, where one or more hydrogen atoms of the alkyl group can be substituted with a fluorine atom. The invention also relates to the new compound's enantiomer or its pharmaceutically used salt.

EFFECT: compounds I exhibit antagonistic activity towards NK₁ and NK₂, which allows for their use in pharmaceutical compositions for making medicine for curing respiratory, cardiovascular, neurotic, painful, oncological, inflammatory and/or gastroenteric upsets.

20 cl, 6 dwg, 54 ex