PURPOSE: To obtain a cis-epoxide compound useful for the treatment or prevention of diseases caused by HIV infection having a higher inhibitory effect and a lower cyto toxicity than conventional inhibitors.
CONSTITUTION: The compound of formula I [R1 is cycloalkyl or aryl-substituted alkyl; A is functional acyl of formula II (R2 is alkyl or amide-substituted alkyl; R3 is alkoxy, aryloxyalkyl, arylalkoxy, aromatic group containing N or the like; m is 0 or 1); B is functional amino or the like of formula III (R6 is alkyl, arylalkyl or amide-substituted alkyl; R7 is alkoxy, alkylamino, benzylamino, alkoxyamino, heterocyclic amino containing O; m is 1 or 2) or formula IV (R8 and R9 are each alkyl or aromatic group), e.g. N-[5-L-(N-benzyloxycarbonyl- L-asparaginyl)amino-(4R,3S)-epoxy-6-phenylhexanoyl]-L-isoleucine methylester, or the compound of formula V or formula VI.
SAI RAKUKEN
RI MASANOBU
SON EISAN
SAI KOUJITSU
KOU SHIYOUSEI
IN KOUSHIYOKU
BOKU SHIHIYO
KIN SHIYOUSHIYU