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Piperidin-1-yl-ethanesulfonyl- phenyl ester, process for its preparation and medicament containing thereof
专利权人:
F. HOFFMANN-LA ROCHE AG
发明人:
ALANINE ALEXANDER,Alanine@Alexander,BUETTELMANN BERND,Buettelmann@Bernd,FISCHER HOLGER,Fischer@Holger,HEITZ NEIDHART MARIE-PAULE,Heitz Neidhart@Marie-Paule,HUWYLER JOERG,Huwyler@Joerg,JAESCHKE GEORG,J
申请号:
CZ20030492
公开号:
CZ303319B6
申请日:
2001.08.20
申请国别(地区):
CZ
年份:
2012
代理人:
摘要:
(Piperidin-1-ylethan)sulfonylfenylester vzorce I, kde R je a) -C(O)(CH.sub.2.n.).sub.n.n.C(O)OH, b) (R.sup.2.n.)(R.sup.3.n.)N-methylfenylkarbonyl-, kde každý z R.sup.2 .n.a R.sup.3.n. je H nebo alkyl s 1 až 7 atomy C nebo cyklická terciární aminoskupina zvolená z pyrrol-1-ylové, imidazol-1-ylové, piperidin-1-ylové, piperazin-1-ylové a morfolin-4-ylové skupiny, z nichž každá je poprípade substituována alkylem s 1 až 7 atomy C, c) -P(O)(OH).sub.2 .n.nebo d) -C(O)(CH.sub.2.n.).sub.n.n.NHC(O)(CH.sub.2.n.).sub.n.n.-N(R.sup.2.n.)(R.sup.3.n.), kde R.sup.2.n. a R.sup.3.n. mají výše uvedený význam a n je císlo 1, 2, 3 nebo 4 a jeho farmaceuticky prijatelné adicní soli s kyselinami. Zpusob jeho prípravy a lécivo s jeho obsahem. Toto lécivo je vhodné pro lécení chorob souvisejících se selektivním blokátorem receptoru subtypu NMDA, jako jsou neurodegenerativní choroby, zvlášte pak pro lécení nebo prevenci mrtvice.The present invention relates to piperidin-1-yl-ethanesulfonyl- phenyl ester of the general formula I in which R represents a) -C(O)(CHi2)inC(O)OH, b) (Re2)(Re3) N-methylphenylcarbonyl-, wherein each Re2a and Re3 are independently from each other hydrogen or alkyl containing 1 to 7 carbon atoms or a cyclic tertiary amine group being selected from the group consisting of pyrrol-1-yl, imidazol-1-yl, piperidin-1-yl, piperazin-1-yl and morpholin-4-yl group being each optionally substituted by an alkyl containing 1 to 7 carbon atoms, c) -P(O)(OH)i2 or d) -C(O)(CHi2)inNHC(O)(CHi2)inN(Re2)(Re3), wherein Re2 and Re3 are as defined above and n is 1, 2, 3 or 4 and to pharmaceutically acceptable acid addition salts thereof. The invention also relates to a process for preparing the above-describe compound as well a medicament in which the compound is comprised wherein the medicament is suitable for the treatment of diseases associated with the NMDA-receptor-subtypes blockers, such as neurodegenerative diseases, especially for the treatment or prevention of stroke.
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