Inhibitors of kynureninase

Details Inhibitors of kynureninase Inhibitors of kynureninase

1994-01-21

1995-08-15

Dees, Josee G.

Organic compounds -- part of the class 532-570 series

Organic compounds

Carboxylic acids and salts thereof

560 12, 560 13, C07C31710, C07C31714, C07C31728

Patent

active

054421047

ABSTRACT:
The present invention provides inhibitors of kynureninase having the formula ##STR1## where X is CHOH, S, SO.sub.2, SO, SONH.sub.2, PO.sub.2 H or PONH.sub.2, R.sub.a and R.sub.b, independently of one another are H, a halogen, CF.sub.3 or a small alkyl group having one to three carbon atoms; R.sub.1 is H, NH.sub.2, NR.sub.6 RT, 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. In particular, compounds of this formula in which X is CHOH, S or SO.sub.2 are provided. 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.

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