C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 207/12 (2006.01) A61K 31/397 (2006.01) A61K 31/40 (2006.01) A61K 31/445 (2006.01) A61P 25/28 (2006.01) C07D 205/04 (2006.01) C07D 211/46 (2006.01) C07D 401/12 (2006.01)
Patent
CA 2601326
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 or -S(O)2NH-lower alkyl; R3 is aryl or heteroaryl, which are unsubstituted or substituted by one to three substituents, selected from the group consisting of lower alkyl, lower alkoxy, CN, NO2, -C(O)-lower alkyl, - C(O)O-lower alkyl, halogen or lower alkyl substituted by halogen; n is 1 or 2; m is 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 (GIyT-I).
La présente invention concerne des composés de la formule générale (I) dans laquelle R1 est -OR1 , -SR1 ou est un groupe hétérocycloalkyle; R1 est alkyle inférieur, alkyle inférieur substitué par halogène, ou est -(CH2)n-cycloalkyle; R2 est -S(O)2-alkyle inférieur ou -S(O)2NH-alkyle inférieur ; R3 est aryle ou hétéroaryle, qui sont non substitués ou substitués par un à trois substituants, sélectionnés parmi le groupe composé de alkyle inférieur, alkoxy inférieur, CN, NO2, -C(O)-alkyle inférieur, -C(O)O-alkyle inférieur, halogène ou alkyle inférieur substitué par halogène; n est 1 ou 2; m est 1 ou 2; l'invention concerne aussi des sels d~addition d~acide pharmaceutiquement acceptables de ceux-ci. Il s~est avéré que les composés de formule générale (I) sont de bons inhibiteurs du transporteur 1 de la glycine (GIyT-I).
Jolidon Synese
Narquizian Robert
Norcross Roger David
Pinard Emmanuel
Borden Ladner Gervais Llp
F.hoffmann-La Roche Ag
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