DIPEPTIDE COMPOUND, ITS PREPARATION AND USE

摘要

PROBLEM TO BE SOLVED: To obtain a new dipeptide compound having excellent proteasome- inhibiting activities and useful for preventing and treating medicine of inflammatory disease, autoimmune disease, neurodegeneration disease or the like. SOLUTION: This new dipeptide compound is the compound of formula I R<1> and R<2> are each a (substituted) aryl; A is a (substituted) alkenylene; R<3> and R<4> are each a (substituted) hydrocarbon; R<5> is formyl or a group of formula II [R<6> is H or the like; R<7> and R<8> are each H or a (substituted) hydrocarbon]}, e.g. N-(5,5-diphenyl-4-pentenoyl)-(L)-valyl-(L)-phenylalaninal. The compound of formula I is obtained, for example, when the R<5> is formyl group, by oxidizing a compound of formula III by a well-known oxidation reaction (e.g. activated dimethylsulfoxide oxidation).When the R<5> is a group of formula II, the compound of formula I is obtained by subjecting a compound of formula IV to an elimination reaction of a protective group of an amino group and further reacting the product with a compound of formula V. The daily dose of the compound of formula I is preferably about 1-500 mg per adult when orally administered.