DERIVATIVES OF PIPERAZINE, METHOD FOR THEIR PREPARING, PHARMACEUTICAL COMPOSITION AND METHOD FOR VOMITING INHIBITION

FIELD: organic chemistry, medicine, pharmacy. ^ SUBSTANCE: invention describes derivatives of piperazine of the general formula (I): wherein Y represents lower alkylene; R1 represents phenyl substituted with one or two similar or different substitutes taken among a group including lower alkoxy-group...

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Hauptverfasser: TAKE KAZUKHIKO, AZAMI KHIDENORI, KAJAKIRI NATSUKO, NAKAI KAZUO, SIGENAGA SINDZI, KONISI NOBUKIJO, ISIDA DZUNIJA, EHJKIJU JOSITERU, MORITA MASATAKA
Format: Patent
Sprache:eng ; rus
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Zusammenfassung:FIELD: organic chemistry, medicine, pharmacy. ^ SUBSTANCE: invention describes derivatives of piperazine of the general formula (I): wherein Y represents lower alkylene; R1 represents phenyl substituted with one or two similar or different substitutes taken among a group including lower alkoxy-group, mono- (or di-, or tri-)-halogen-lower)-alkyl, nitro-, amino-, lower alkylamino-, di-(lower)-alkylamino-, lower alkylthio-group,alkylsulfonyl, lower alkylaminosulfonyl, di-(lower)-alkylaminosulfonyl, and pyrrolyl; R2 means phenyl substituted with hydroxy-group at position 3 and with lower alkyl and halogen atom additionally; R3 means hydrogen atom; R4 represents (2,6-dimethylmorpholino)-(lower)-alkyl, (2-methoxymethylmorpholino)-(lower)-alkyl, (3-methoxymethylmorpholino)-(lower)-alkyl. Also, invention relates to their pharmaceutically acceptable salts, to method for their preparing, pharmaceutical composition and a method for vomiting inhibition. Proposed compounds are antagonists of tachykinin and can be used for vomiting inhibition. ^ EFFECT: improved preparing method, valuable medicinal properties of compounds. ^ 9 cl, 47 ex