5-DEMETHOXYFUMAGILLOL DERIVATIVES AND PREPARATION PROCESS THEREOF

摘要

PURPOSE: 5-demethoxyfumagillol derivatives useful as angiogenesis inhibiting agents and a preparation process thereof are provided. CONSTITUTION: 5-demethoxyfumagillol derivatives represented by the formula(1) and pharmaceutically acceptable salts thereof are provided, wherein X is hydroxy; Y is halogen and a compound represented by the formula, wherein R1 and R2 are independently hydrogen, or substituted or unsubstituted lower alkyl, Z- is counter ion, provided that R1 and R2 are not hydrogen simultaneously, and X and Y form an oxirane ring together; A is compounds represented by the formulae, wherein R3 is substituted or unsubstituted lower alkyl or alkanoyl, substituted or unsubstituted aryl or arylalkyl, or arylalkanoyl.