DERIVATIVES OF EPOXISUCCINAMIDE.

摘要

An epoxisuccinamide derivative having the following formula (1) and its physiologically acceptable salt: in which R1 represents a hydrogen atom, an alkyl group having 1 to 10 carbon atoms, an alkenyl group having 2 to 10 atoms of carbon, an alkynyl group having 2 to 10 carbon atoms, an aryl group having 6 to 20 carbon atoms, an aralkyl group comprising an aryl group having 6 to 20 carbon atoms and an alkyl group having 1 to 6 carbon atoms, a heterocyclic group having 3 to 12 carbon atoms, or a heterocycle-alkyl group comprising a heterocyclic group having 3 to 12 carbon atoms and an alkyl group having 1 to 6 carbon atoms; R2 represents an alkyl group having 1 to 10 carbon atoms, an alkenyl group having 2 to 10 carbon atoms, an alkynyl group having 2 to 10 carbon atoms, an aryl group having 6 to 20 carbon atoms, an aralkyl group comprising an aryl group having 6 to 20 carbon atoms and an alkyl group having 1 to 6 carbon atoms, a heterocyclic group having 3 to 12 carbon atoms, or a heterocycloalkyl group comprising a heterocyclic group that it has 3 to 12 carbon atoms and an alkyl group having 1 to 6 carbon atoms; R3 represents a hydrogen atom, an alkyl group having 1 to 10 carbon atoms, an alkenyl group having 2 to 10 carbon atoms, an alkynyl group having 2 to 10 carbon atoms, an aryl group having 6 to 20 carbon atoms, an aralkyl group comprising an aryl group having 6 to 20 carbon atoms and an alkyl group having 1 to 6 carbon atoms, a heterocyclic group having 3 to 12 carbon atoms, or a heterocycle group - alkyl comprising a heterocyclic group having 3 to 12 carbon atoms and an alkyl group having 1 to 6 carbon atoms; X represents -O- or -NR4-, in which R4 is a hydrogen atom, an alkyl group having 1 to 10 carbon atoms, an aryl group having 6 to 20 carbon atoms, an aralkyl group comprising a group aryl having 6 to 20 carbon atoms and an alkyl group having 1 to 6 carbon atoms, a heterocyclic group having 3 to 12 carbon atoms, or a heterocycloalkyl group comprising a heterocyclic group having 3 to 12 atoms of carbon and an alkyl group having 1 to 6 carbon atoms; Y1 represents a hydroxyl group, an alkoxy group having 1 to 6 carbon atoms, an acetoxy group, or an aralkyloxy group comprising an aryl group having 6 to 20 carbon atoms and an alkyl group having 1 to 6 atoms of carbon; and Y2 represents a hydrogen atom or an alkyl group having 1 to 10 carbon atoms; wherein each of the aryl groups and the heterocyclic groups for R1 to R4 can have one or more substituents selected from the group consisting of alkyl having 1-6 carbon atoms, hydroxyl, amino, alkylamino having 1-6 carbon atoms , dialkylamino having 2-12 carbon atoms in total, alkoxy having 1-6 carbon atoms, halogen, haloalkyl having 1-6 carbon atoms, cyano, nitro, carboxyl, alkoxycarbonyl having 27 carbon atoms, carbamoyl , alkylaminocarbonyl having 2-7 carbon atoms, dialkylaminocarbonyl having 3-13 carbon atoms in total, amidino and guanidino.