Patent ID: 6387908
Filing Date: 2002-05-14
Classification: A61P,C07D

Abstract:
An epoxysuccinamide derivative having the following formula (1) and its physiologically acceptable salt: whereinR1 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, or an aralkyl group consisting of an aryl group having 6 to 20 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, or an aralkyl group consisting of an aryl group having 6 to 20 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 consisting of 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 heterocyclic-alkyl group consisting of a heterocyclic group having 3 to 12 carbon atoms and an alkyl group having 1 to 6 carbon atoms; X represents â€”Oâ€” or â€”NR4â€” 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 consisting of 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 heterocyclic-alkyl group consisting of a heterocyclic group having 3 to 12 carbon atoms 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 consisting of an aryl group having 6 to 20 carbon atoms and an alkyl group having 1 to 6 carbon atoms; and Y2 represents a hydrogen atom or an alkyl group having 1 to 10 carbon atoms; provided that the aryl group for R1 to R4 may 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, alkoxy-carbonyl having 2-7 carbon atoms, â€”CONH2, alkylaminocarbonyl having 2-7 carbon atoms, dialkylaminocarbonyl having 3-13 carbon atoms in total, amidino, and guanidino; and provided that the heterocyclic group for R3 and R4 is selected from the group consisting of pyridyl, pyrrolidinyl, piperidinyl, furyl, thienyl, piperazinyl, indolyl and benzimidazolyl.