| 摘要 |
<p>The present invention relates to novel derivatives of 3-hydroxyanthranilic acid, 3-HANA, of general formula (I), wherein R?1 and R2¿ are the same or different and selected from H and alkyl; X is selected from alkylthio, arylthio, aryloxy, halogen and cyano; R3, R4 are the same or different and selected from halogen, methyl, fluoroalkyl, cyano and Z-R5 wherein Z is selected from CH¿n?, NHm, O, S, SO2 and CO wherein n = 1 or 2; m = 0 or 1 and R?5¿ is selected from alkyl, aryl and fluoroalkyl; or R?3 and R4¿ together form a saturated or unsaturated ring system Y-V-Z wherein Y and Z, independently of each other, are as defined for Z above and V is selected from C¿1?-C3 alkylene or alkenylene, -N = , -N = N- and (a), wherein R7 = H or alkyl; or a pharmaceutically acceptable salt thereof, methods and intermediates for their preparation, novel pharmaceutical compositions and the use thereof for inhibiting the enzyme 3-hydroxy-anthranilate oxygenase, 3-HAO, responsible for the production of the endogenous neurotoxin quinolinic acid, QUIN.</p> |
