| 摘要 |
The compound of formula I wherein: W is A-B-D A is aryl(CH2)n, heteroaryl(CH2)n, alkyl having from 1 to 14 carbons, alkenyl having from 2 to 14 carbons, or cycloalkyl from 3 to 10 carbons. The A group may be optionally substituted with 1 or more J groups. B is a bond or CO, SO, SO2, OCO, NR5CO, NR5SO2 or NR5SO D is a bond, an amino acid residue or a peptide composed of 2 to 5 amino acid residues. The amino acids are independently defined by the formula -NH-**CH(R6)-CO-, in which ** denotes the a carbon of an a-amino acid residue possessing when R6 is other than hydrogen, the D-configuration, the L-configuration or a mixture of D-and L-. n is an integer from 0 to 6 R1, R2, R3, R4, R5 and R6 are independently hydrogen, alkyl having 1 to 14 carbons or cycloalkyl having 3 to 10 carbons. The alkyl and cycloalkyl groups being optionally substituted with 1or more J groups. J is halogen, lower alkyl, aryl, heteroaryl, haloaryl, amino optionally substituted with 1 to 3 aryl or lower alkyl groups, guanidine, alkoxycarbonyl, amido, lower alkylamido, sulfonamido, lower alkyl sulfonamido, lower alkylsulfonyl, lower alkylsulfoxy, lower alkylthio, lower alkoxy, aryloxy, arylalkyloxy, hydroxy, carboxy, cyano or nitro. *denotes the a carbon of an a-amino acid residue possessing when R2 is other than hydrogen, the D-configuration, the L-configuration or a mixture of D-and L- configurations. The compound of formula 1 are useful for neurodegeneration, stroke, Alzheimer's, amytrophy, motor neuron damage, acute central nervous system injury, muscular dystrophy, bone resorption, platelet aggregation, cataracts, inflammation and for inhibiting serine proteases and cysteine protease. Also described are pharmaceutical compositions comprising the compound of formula I.
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