Inhibitors of kynureninase

Details Inhibitors of kynureninase Inhibitors of kynureninase

C - Chemistry, Metallurgy

07

C

C07C 229/36 (2006.01) A61K 31/195 (2006.01) A61K 31/66 (2006.01) C07C 233/47 (2006.01) C07C 313/06 (2006.01) C07C 317/48 (2006.01) C07C 323/58 (2006.01) C07F 9/30 (2006.01)

Patent

CA 2108670

2108670 9218003 PCTABS00016 The present invention provides inhibitors of kynureninase having formula (I), where X is CHOH, S, SO2, SO, SONH, PO2H or PONH2, RA and RB, independently of one another, are H, a halogen CF3 or a small alkyl group having one to three carbon atoms; A is a H or an acetyl group; R1 is H, NH2, NR6R7, NO2, halogen, CF3 or a small alkyl group having from one to three carbon atoms, wherein: R6 and R7, 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 R6 or R7 can be a formyl group; R2 is OH, H, halogen, CF3 or a small alkyl group having from one to three carbon atoms; and R3, R4 and R5, independently of one another, are H, halogen, CF3, NO2, NH2, or small alkyl group having from one to three carbon atoms. In particular, compounds of this formula in which X is CHOH, S or SO2 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 RA or RB is a hydrogen, are more potent inhibitors of kynureninase. Inhibitors or mammalian kynureninase are of particular use in therapy for certain neurological disorders.

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