DERIVATIVES OF AZETIDINE, METHODS FOR THEIR PREPARING, PHARMACEUTICAL COMPOSITION AND MEDICINAL AGENT BASED ON THEREOF
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, ra...
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Zusammenfassung: | 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 for |
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