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DÉRIVÉS DE TÉTRAHYDROPYRANE DIRIGÉS CONTRE DES MALADIES NEUROLOGIQUES
专利权人:
F.Hoffmann-La Roche AG
发明人:
申请号:
EP11700964.7
公开号:
EP2531190A1
申请日:
2011.01.28
申请国别(地区):
EP
年份:
2012
代理人:
摘要:
The present invention relates to a compound of formula I wherein R1/R2 are independently from each other hydrogen, (CR2)o-cycloalkyl, optionally substituted by lower alkyl or hydroxy, or are lower alkyl or heterocycloalkyl, and o is 0 or 1; and R may be the same or different and is hydrogen or lower alkyl; or R1 and R2 may form together with the N atom to which they are attached a heterocycloalkyl group, selected from the group consisting of pyrrolidinyl, piperidinyl, 3-aza-bicyclo[3.1.0]hex-3-yl or 2-aza-bicyclo[3.1.0]hex-2-yl, which are optionally substituted by hydroxy; R3 is S-lower alkyl, lower alkyl, lower alkoxy or cycloalkyl; R3' is hydrogen, lower alkyl substituted by halogen, lower alkyl or lower alkoxy R4 is lower alkyl substituted by halogen, lower alkyl or lower alkoxy; X is -O- or -CH2-; X' is -O- or -CH2-; with the proviso that one of X or X' is always -O- and the other is -CH2-; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer thereof. It has been found that the compounds of formula I are good inhibitors of the glycine transporter 1 (GlyT-1) and therefore they may be used for the treatment of schizophrenia.La présente invention concerne un composé de formule générale (I) dans laquelle X représente -O- ou -CH2- ; X' représente -O- ou -CH2- ; à condition que l'un de X ou X' représente toujours -O- et l'autre représente -CH2-.Il a été découvert que les composés de formule générale (I) sont de bons inhibiteurs du transporteur 1 de la glycine (GlyT-1) et ils peuvent donc être utilisés pour le traitement de la schizophrénie, des psychoses et d'autres affections neurologiques, y compris la douleur.
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中国工程科技知识中心
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