Fluoro-substituted benzoylpropionic acid derivatives

C - Chemistry – Metallurgy – 07 – C

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C07C 237/20 (2006.01) A61K 31/16 (2006.01) A61K 31/21 (2006.01) C07C 229/36 (2006.01) C07C 259/06 (2006.01)

Patent

CA 2233075

A fluoro-substituted benzoyl propionic acid derivative of formula (I) either as single isomer or as mixture of isomers, wherein R is hydroxy, amino, hydroxylamine, -OR', -NHR', N(R')2 or -NHOR' in which R' is C1-C6 alkyl or benzyl, or a pharmaceutically acceptable salt thereof, which act as kynurenine- 3-hydroxylase enzyme inhibitor and can be useful in the treatment of neurodegenerative diseases. A process for preparing compounds of formula (I) and pharmaceutical compositions comprising them are also described.

On décrit un dérivé de l'acide benzoylpropionique substitué par fluoro, de la formule (I), ou un sel de celui-ci acceptable sur le plan pharmacologique, soit en tant qu'isomère seul, soit en tant que mélange d'isomères. Dans cette formule, R représente hydroxy, amino, hydroxylamine, -OR', -NHR', N(R')¿2? ou -NHOR', où R' représente alkyle C¿1?-C¿6? ou benzyle. Ce dérivé agit en tant qu'inhibiteur de la kynurénine-3-hydroxylase et il peut être utile dans le traitement des maladies neurodégénératives. On décrit encore un procédé de préparation de composés de la formule (I) ainsi que des compositions pharmaceutiques comprenant ceux-ci.

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