DERIVATIVES OF AZETIDINE, METHODS FOR THEIR PREPARING, PHARMACEUTICAL COMPOSITION AND MEDICINAL AGENT BASED ON THEREOF Russian patent published in 2004 - IPC

FIELD: organic chemistry, pharmacy.

SUBSTANCE: invention relates to new derivatives of azetidine of the formula: wherein R means a link of the formula:

or,wherein R₁ means radical methyl or ethyl; R₂ means radical naphthyl, quinolyl, phenyl possibly substituted with one or some halogen atoms, radicals alkyl, alkoxyl, hydroxyl and so on; R₃ and R₄ are similar or different and mean radical phenyl possibly substituted with one or some halogen atoms, alkyl, alkoxyl, formyl, trifluoromethyl and so on; R₅ means radical alkyl or phenyl substituted with one or some halogen atoms; R₆ and R₇ are similar or different and mean hydrogen atom or radical alkyl; or R₆ and R₇ in common with nitrogen atom to which they are bound form piperidine or piperazine cycle substituted with alkyl; R'₆ and R'₇ are similar or different and mean hydrogen atom or radical alkyl; or R'₆ and R'₇ in common with nitrogen atom to which they are bound form pyrrolidine or piperazine cycle possibly substituted with one or some radicals alkyl, -CO-alk, -COO-alk and so on; R''₆ and R''₇ are similar or different and mean radical alkyl, cycloalkyl, -alk-O-alk, hydroxyalkyl; or R''₆ and R''₇ in common with nitrogen atom to which they are bound form cycle imidazole, piperazinone, thiomorpholine and so on; R₈ means alkyl; R₉ means hydrogen atom, radical alkyl or alkyl substituted with dialkylamine, phenyl and so on; R₁₀ and R₁₁ are similar or different and mean hydrogen atom or alkyl; R₁₂ and R₁₃ in common with nitrogen atom to which they are bound form morpholine cycle; R ₁₆ and R₁₇ in common with nitrogen atom to which they are bound form piperidine cycle; R' means hydrogen atom or radical -CO-alk wherein alk means alkyl or alkylene being alkyl or alkylene radicals or their moieties and alkoxyl radicals or their moieties are direct or branched chains comprising from 1 to 6 carbon atoms, and to their optic isomers or their salts with mineral or organic acid. Invention relates to a method for preparing compounds of the formula (I) wherein R represents a chain of the formula A by dehydration of compound of the formula (Ia):

wherein R₁, R₂, R₃ and R₄ have values indicated for the formula (I) and R'' means radical hydroxy-, methanesulfonyloxy- or acetyloxy- with the following isolation of the end compound that if necessary is converted to salt with mineral or organic acid. Invention relates to a pharmaceutical composition eliciting antagonistic effect and containing at least one compound of the formula (I) as an active component taken in the dose from 1 to 1000 mg. Invention relates to a medicinal agent eliciting antagonistic effect and comprising at least one compound of the formula (I) as an active substance. Invention provides preparing new derivatives of azetidine eliciting an antagonistic effect.

EFFECT: improved preparing methods, valuable medicinal properties of compounds.

28 cl, 1 tbl, 163 ex