Sulfanyl substituted phenyl methanones as glycine...

Details Sulfanyl substituted phenyl methanones as glycine... Sulfanyl substituted phenyl methanones as glycine...

C - Chemistry, Metallurgy

07

D

C07D 295/18 (2006.01) A61K 31/495 (2006.01) A61K 31/496 (2006.01) A61K 31/506 (2006.01) A61P 25/28 (2006.01) C07D 213/74 (2006.01) C07D 239/42 (2006.01)

Patent

CA 2593453

The present invention relates to compounds of the general formula (I) wherein R1 is lower alkyl or lower alkyl substituted by halogen; R2 is -S(O)2-lower alkyl, -S(O)2NH-lower alkyl, NO2 or CN; R3 is halogen, CN, lower alkyl, lower alkyl substituted by halogen, NO2, -C(O)-lower alkyl or S(O)2-lower alkyl; X/X1 are independently from each other CR4 or N; R4 is hydrogen or halogen; 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 (G1yT-1) for the treatment of schizophrenia.

L'invention concerne des composés de formule générale (I), dans laquelle R1 désigne un alkyle inférieur ou un alkyle inférieur substitué par un halogène; R2 désigne un alkyle inférieur -S(O)2-, un alkyle inférieur -S(O)2NH-, NO2 ou CN; R3 désigne un halogène, CN, un alkyle inférieur, un alkyle inférieur substitué par un halogène, NO2, un alkyle inférieur -C(O)- ou un alkyle inférieur S(O)2-; X/X1 désignent, indépendamment l'un de l'autre, CR4 ou N; R4 désigne un hydrogène ou un halogène; n est égal à 0, 1 ou 2. L'invention concerne en outre des sels d'addition acides pharmaceutiquement acceptables de ces composés. On a trouvé que les composés de formule générale (I) sont de bons inhibiteurs du transporteur de glycine 1 (GlyT-1) pour le traitement de la schizophrénie.

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