2-amino-4-phenyl-4-oxo-butyric acid derivatives with...

Details 2-amino-4-phenyl-4-oxo-butyric acid derivatives with... 2-amino-4-phenyl-4-oxo-butyric acid derivatives with...

C - Chemistry, Metallurgy

07

C

C07C 229/36 (2006.01) A61K 31/165 (2006.01) A61K 31/195 (2006.01) A61K 31/215 (2006.01) C07C 237/20 (2006.01) C07C 259/06 (2006.01) C07C 317/48 (2006.01) C07C 323/63 (2006.01)

Patent

CA 2144521

Use in the prevention and/or in the treatment of neurodegenerative diseases of 2-amino-4-phenyl-4- oxobutyric acid derivatives (I) which act as kynureninase enzyme inhibitors and/or kynurenine-3-hydroxylase enzyme inhibitors. In formula (I), each of the groups X and Y is, independently, hydrogen, halogen, trifluromethyl, hydroxy, C1-C6 alkyl, benzyl, C6-C10 aryl, -OR', -SR', (a) or (b), in which R' is C1-C6 alkyl or benzyl; and R is hydroxy, amino, hydroxylamine, -OR', -NHR', (c) or -NHOR', in which R' is as defined above. Several of these derivatives are new and, as such, constitute a further object of this invention, together with the process for their preparation and the pharmaceutical compositions containing them.

Utilisation, dans la prévention et/ou le traitement des maladies neurodégénératives, des dérivés de l'acide 2-amino-4-phényl-4-oxobutyrique (I), qui exercent une activité inhibitrice de la cynuréninase et/ou de la cynurénine-3-hydroxylase. Dans la formule (I), chacun des groupes X et Y représente, indépendamment, de l'hydrogène, de l'oxygène, du trifulorométhyle, un groupe hydroxy, alkyle C1-C6, benzyle, aryle C6-C10, -OR', -SR', (a) ou (b), où R' représente un benzyle ou un alkyle C1-C6; et R représente un groupe hydroxy, amino, hydroxylamine, -OR', -NHR', (c) ou -NHOR', où R' est tel qu'il est défini ci-dessus. Plusieurs de ces dérivés sont nouveaux et, en tant que tels, constituent un autre objet de l'invention, ainsi que le procédé permettant de les préparer et que les compositions pharmaceutiques qui les contiennent.

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