Inhibitors of kynureninase

US5254725A · kind A · utility

Assignee

• University of Georgia Research Foundation, Inc. · US

Inventors

• Robert S. Phillips · Lafayette, US
• Rajesh K. Dua · Ann Arbor, US

Key dates

• Filing date: Apr 18, 1991
• Grant date: Oct 19, 1993
• Expiry date: Apr 18, 2011

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07C323/58
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present invention provides inhibitors of kynureninase having the formula ##STR1## where 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 NH.sub.2, NR.sub.6 R.sub.7, 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 or small alkyl group having from one to three carbon atoms. In particular, compounds of formula I having the (.alpha.S,.gamma.S) configuration or (.alpha.R,.gamma.R) configuration when R.sub.A or R.sub.B is a halogen are more potent inhibitors of kynureninase. Inhibitors of mammalian kynureninase are of particular use in therapy for certain neurological disorders.