Claims
- 1. A compound of the formula (Ia) whereineach of the groups X and Y is, independently, hydrogen; halogen; nitro; C1-C6 alkyl; C2-C4 alkenyl; C2-C4 alkynyl; C1-C6 alkoxy; C1-C6 alkylthio; SOR2 or SO2R2 in which R2 is C1-C6 alkyl, phenyl or benzyl; or SO2N(R3)2 in which each of the groups R3 is, independently, hydrogen, C1-C6 alkyl, C2-C4 alkenyl, C2-C4 alkynyl, phenyl or benzyl; R is hydroxy; —OR5 in which R5 is C1-C6 alkyl, C2-C4 alkenyl, C2-C4 alkynyl or benzyl; —N(R3)2 or —N(R3)OR3 in which each of R3 is as defined above; W is —SO2R4 in which R4 is C1-C6 alkyl, an optionally substituted C2-C4 alkenyl, an optionally substituted phenyl or benzyl; —CONHR5 or —CSNHR5 in which R5 is as defined above; or a pharmaceutically acceptable salt thereof.
- 2. The compound of the formula (Ia) according to claim 1 wherein W is SO2R4 in which R4 is C1-C4 alkyl and X and Y, which may be the same or different are hydrogen or halogen, or a pharmaceutically acceptable salt thereof.
- 3. The compound of the formula (Ia) according to claim 1 which is N-methylsulphonyl-2-amino-4-oxo-4-(3′,4′-dichlorophenyl)butanoic acid, either as single enantiomer or as a mixture thereof, or a pharmaceutically acceptable salt thereof.
- 4. A method of inhibiting kynurenine-3-hydroxylase enzyme in a mammal in need thereof, comprising administering to said mammal a kynurenine-3-hydroxylase enzyme-inhibiting effective amount of a compound of formula (I) as defined in claim 1, or a pharmaceutically acceptable salt thereof.
- 5. A pharmaceutical composition for inhibiting kynurenine-3-hydroxylase, which comprises, as an active ingredient, an effective amount of one or more compounds of the formula (I) of claim 1, or a pharmaceutically acceptable salt thereof, in association with a pharmaceutically acceptable carrier.
- 6. A pharmaceutical composition for inhibiting kynurenine-3-hydroxylase, which comprises, as an active ingredient, an effective amount of one or more compounds of the formula (Ia) of claim 1, or a pharmaceutically acceptable salt thereof, in association with a pharmaceutically acceptable carrier.
- 7. The method of claim 4, wherein said mammal is a human.
Priority Claims (1)
Number |
Date |
Country |
Kind |
9618349 |
Sep 1996 |
GB |
|
Parent Case Info
This application is a 371 of PCT/EP97/04271 filed Jul. 31, 1997.
PCT Information
Filing Document |
Filing Date |
Country |
Kind |
102e Date |
371c Date |
PCT/EP97/04271 |
|
WO |
00 |
2/24/1999 |
2/24/1999 |
Publishing Document |
Publishing Date |
Country |
Kind |
WO98/09938 |
3/12/1998 |
WO |
A |
US Referenced Citations (2)
Number |
Name |
Date |
Kind |
4758661 |
Melilo et al. |
Jul 1988 |
|
5495044 |
Phillips et al. |
Feb 1996 |
|
Foreign Referenced Citations (1)
Number |
Date |
Country |
WO9503271 |
Feb 1995 |
WO |
Non-Patent Literature Citations (2)
Entry |
Sahoo, P S et al. “Inhibition of Matrix Metalloproteinases by N-Carboxyalkyl Dipeptides” Bioorganic & Med. Chem. Lett. vol. 5 No. 20 pp. 2441-2446. See Scheme 1 and Table 1, 1995.* |
Yato, M. et al “Reduction of Aromatic Ketones into Methylenes using Triethylsilane and Titanium Tetrachloride. Synethesis of 2-Aminobutanoic Acids” Heterocycles vol. 41 No. 1 pp. 17-20. See Table 1, 1995. |