[4-(heteroaryl) piperazin-1-yl]-(2,5-substituted...

C - Chemistry – Metallurgy – 07 – D

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C07D 277/42 (2006.01) A61K 31/496 (2006.01) A61P 25/28 (2006.01) C07D 277/56 (2006.01) C07D 285/08 (2006.01) C07D 285/135 (2006.01)

Patent

CA 2593463

The present invention relates to compounds of the general formula (I) wherein R1 is-OR1~,-SR1~ or is a heterocycloalkyl group; R1~ is lower alkyl, lower alkyl substituted by halogen or is -(CH2)n-cycloalkyl; R2 is-S(O)2-lower alkyl, -S(O)2NH-lower alkyl, NO2 or CN; X1 is CR3 or N; X2 is CR3~ or N; R3/R3~ are independently from each other hydrogen, halogen, lower alkyl, CN, NO2,-S(O)2-phenyl, -S(O)2-lower alkyl, -S(O)2-pyridin-2, 3 or 4-yl, phenyl, optionnally substituted by one or two substituents selected from the group consisting of NO2 or halogen, or is lower alkyl substituted by halogen or is - C(O)-lower alkyl; n is 0, 1 or 2; and to pharmaceutically acceptable acid addition salts thereof. It has been found that the compounds of general formula (I) are good inhibitors of the glycine transporter 1 (GlyT-1). They may be used in the treatment of schizophrenia.

L'invention concerne des composés de formule (I), dans laquelle R1 représente OR1',-SR1' ou un groupe hétérocycloalkyle ; R1' représente un alkyle inférieur, un alkyle inférieur substitué par halogène ou cycloalkyle (CH2)n ; R2 représente un alkyle inférieur S(O)2, un alkyle inférieur S(O)2NH, NO2 ou CN ; X1 représente CR3 ou N ; X2 représente CR3' ou N ; R3/R3' représentent indépendamment l'un de l'autre hydrogène, halogène, alkyle inférieur, CN, NO2, phényle S(O)2, alkyle inférieur S(O)2, pyridine S(O)2 2, 3 ou 4, phényle, éventuellement substitué par un ou deux substituants sélectionnés parmi le groupe constitué de NO2 ou halogène ou un alkyle inférieur substitué par halogène ou un alkyle inférieur C(O) ; n représente 0, 1 ou 2 ; des sels supplémentaires d'acide pharmaceutiquement acceptables. Il a été démontré que les composés de formule (I) sont de bons inhibiteurs du transporteur de la glycine 1 (GlyT-1). Ils peuvent être utilisés dans le traitement de la schizophrénie.

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