ASPARAGINE DERIVATIVE AND ITS USE

摘要

PURPOSE:To provide a new asparagine derivative having retrovirus protease- inhibiting activity and low toxicity and useful as an agent for treating retroviral diseases. CONSTITUTION:The compound of formula I [ring A is 5 to 7-membered ring; R<1> and R<2> are H or together form a condensed ring; R<3> is carboxyl which may be esterified or amidated; R<4> is H or acyl; X is C(OH)H or C(C=0)] and its salt, e.g. 1-[(3S)--3-(N-benzyloxycarbonyl-L-asparaginyl) amino-2-hydroxy-4- phenylbutyryl]-N-t-butyl-L-prolinamide. The compound can be produced by condensing a compound of formula II with a compound of formula III (R<4>' is acyl).