Inhibitors of kynureninase

Abstract

The present invention provides inhibitors of kynureninase having the formula ##STR1## where X is CO or CHOH; R.sub.A and R.sub.B, independently of one another, are H, a halogen, a halovinyl group, or a small alkyl or haloalkyl group having one to three carbon atoms; A is a H or an acetyl group; R.sub.1 is H, NH.sub.2, NR.sub.6 R.sub.7, NO.sub.2, halogen, CF.sub.3 or a small alkyl group having from one to three carbon atoms, wherein: R.sub.6 and R.sub.7, independently of one another, are H, a formyl group or a small alkyl group having from one to three carbon atoms with the exception that only one of R.sub.6 or R.sub.7 can be a formyl group; R.sub.2 is OH, H, halogen, CF.sub.3 or a small alkyl group having from one to three carbon atoms; and R.sub.3, R.sub.4 and R.sub.5, independently of one another, are H, halogen, CF.sub.3, NO.sub.2, NH.sub.2, or small alkyl group having from one to three carbon atoms, and with the proviso that when X=CO, neither R.sub.A nor R.sub.B can be CF.sub.3. In compounds of this formula in which X is CHOH, those having the (.alpha.S,.gamma.S) configuration or the (.alpha.R,.gamma.R) configuration when R.sub.A or R.sub.B is a hydrogen, are more potent inhibitors of kynureninase. Inhibitors of mammalian kynureninase are of particular use in therapy for certain neurological disorders.

Dependencies are inferred from the claim text.