Patent number: 5516936
Abstract: The present invention provides inhibitors of kynureninase having the formula ##STR1## where X is CHOH, S, SO.sub.2, SO, SONH, 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; 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. In particular, compounds of this formula in which X is CHOH, S or SO.sub.
Type:
Grant
Filed:
December 27, 1993
Date of Patent:
May 14, 1996
Assignee:
University of Georgia Research Foundation, Inc.
Inventors:
Robert S. Phillips, Rajesh K. Dua
Patent number: 5442104
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.
Type:
Grant
Filed:
January 21, 1994
Date of Patent:
August 15, 1995
Assignee:
University of Georgia Research Foundation, Inc.
Inventors:
Robert S. Phillips, Rajesh K. Dua