| 摘要 |
PROBLEM TO BE SOLVED: To obtain the subject new compound having an inhibiting action which is strong against gelatinase and has high selectivity, and useful as a carcinostatic medicine, a vascularization-inhibiting medicine, a cancer infiltration- inhibiting medicine and a cancer metastasis-inhibiting medicine. SOLUTION: A compound of formula I R<1> is 2-thienyl; R<2> is a 1-4C alkyl, a 4-12C cycloalkyl-alkyl, etc.; R<3> is a 1-4C alkyl [substituted with one to six groups of (substituted)OH, (substituted)amino, etc.], and R<4> is H, or R<3> , R<4> and N atom connected to the groups together form a heterogeneous ring [substituted with a (protected)hydroxyl(alkyl) group], or its salt. For example, [4-hydroxyamino-2-(R)-nonyl-3-(2-thienylthiomethyl)succinyl]-L-phenyla lanine}-[2- hydroxy-1-(hydroxymethyl)ethyl]amide. The compound of formula I is obtained by subjecting a compound of formula II (Bn is benzyl) and a compound of formula III to a condensation-reaction, converting the product intoα-methylene carboxylic acid compound, addition-reacting a compound of formula: R<1> SH to the producedα-methylene carboxylic acid compound and subsequently amidating the reaction product.
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