NOVEL DERIVATIVES OF 3-HYDROXY ANTHRANILIC ACID, METHODS ANDINTERMEDIATES FOR THEIR PREPARATION, NOVEL PHARMACEUTICAL COMPOSITIONS AND THE USE THEREOF

摘要

The present invention relates to novel derivatives of 3-hydroxyanthranilic acid, 3-HANA, of general formula (I) wherein R1 and R2 are the same or different and selected from H, alkyl, aryl and arylalkyl; X and Y are the same or different and selected from alkoxy, aryloxy, alkyl, alkylthio, arylthio, fluoroalkyl, halogen, cyano, OSO2CH3, OSO2CF3, OCF3 and SCF3 with the proviso that the compound of formula (I) wherein R1 and R2 = H, X = Br and Y = Me is excluded; or a pharmaceutically acceptable salt thereof, methods and intermediates for their preparation, novel pharmaceutical compositions and the use thereof for inhibiting the enzyme 3-hydroxyanthranilate oxygenase, 3- HAO, responsible for the production of the endogenous neurotoxin quinolinic acid, QUIN.