Substituted kynurenines, a process for their preparation,...

Details Substituted kynurenines, a process for their preparation,... Substituted kynurenines, a process for their preparation,...

C - Chemistry, Metallurgy

07

C

C07C 229/36 (2006.01) A61K 31/00 (2006.01) A61K 31/16 (2006.01) A61K 31/165 (2006.01) A61K 31/195 (2006.01) A61K 31/198 (2006.01) A61K 31/215 (2006.01) A61K 31/216 (2006.01) C07C 237/20 (2006.01) C07C 259/06 (2006.01)

Patent

CA 2145178

The present invention relates to the use in the treatment of cognitive disorders associated with the aging processes of the brain and perinatal brain disorders of compounds which act as inhibitors of the enzyme kynurenine aminotransferase (KAT). The present invention also provides, as novel compounds, a selected class of KAT inhibitors which are the compounds of formula (IA), wherein R is halogen, C1- C6 alkyl, C5-C7 cycloalkyl, phenyl-C1-C4 alkyl, C1-C6 alkoxy, C6-C10 aryloxy, phenyl-C1-C4 alkoxy or trifluoromethyl, and R1 is hydroxy, C1-C6 alkoxy, amino, mono-C1-C6 alkylamino, di-C1-C6 alkylamino, hydroxylamino, C1-C4 alkoxyamino or benzyloxyamino, with the provisos that: (i) when R1 is hydroxy and, at the same time, R is halogen, then this halogen is not fluorine; and (ii) when R1 is hydroxy and, at the same time, R is C1-C6 alkyl, then this C1-C6 alkyl is not methyl, either as a single isomer or as a mixture of isomers, and the pharmaceutically acceptable salts thereof.

Cette invention concerne l'utilisation de composés qui agissent comme inhibiteurs de l'aminotransférase de Kynurénine (KAT) dans le traitement des troubles cognitifs associés aux processus de vieillissement du cerveau et aux troubles cérébraux périnatals. Cette invention utilise également comme nouveaux composés une classe sélectionnée d'inhibiteurs de KAT qui sont les composés de formule (IA). Dans cette formule, R représente halogène, alkyle C1-C6, cycloalkyle C5-C7, phényle-alkyle C1-C4, alcoxy C1-C6, aryloxy C6-C10, phényle-alcoxy C1-C4 ou trifluorométhyle, et R1 représente hydroxy, alcoxy C1-C6, amino, monoalkylamino C1-C6, dialkylamino C1-C6, hydroxylamino, alcoxyamino C1-C4 ou benzyloxyamino, à condition que : (1) lorsque R1 représente hydroxy et, qu'en même temps, R représente halogène, cet halogène ne représente pas fluor; et (ii) lorsque R1 représente hydroxy et, qu'en même temps, R représente alkyle C1-C6, cet alkyle C1-C6 ne représente pas méthyle. Les nouveaux composés se présentent sous forme d'un seul isomère ou d'un mélange d'isomères et de leurs sels pharmaceutiquement acceptables.

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