Peptider med foermaoga att inhibera effekten av HIV-proteas, deras framstaellning och terapeutiska anvaendning

摘要

Compounds of formula (I) : [wherein: R<1> is hydrogen, alkyl, aralkyl, -COR, -COR, -CSR, -CSR, -SO2R, -CONHR, -CSNHR, -CONRR or -CSNRR; R<2> is hydrogen or alkyl; R<3> is hydrogen, alkylidene, substituted alkyl, or R; R<4> is optionally substituted alkyl, cycloalkyl, or aryl; R<5> is RO-, RRN-, RHN-, aralkyloxycarbonyloxy or aralkyloxycarbonylamino, or R<5> is -(CH2)p-D-(CH2)r- [where D is a single bond, carbonyl, oxygen, sulphur, -NH-, -(CH2=CH2)- or -NHCO-; and p and r are each 0 or an integer from 1 to 5]; A is -(CH2)m-B-(CH2)n- [where B is a single bond, carbonyl, oxygen, sulphur, -NH-, -(CH2=CH2)- or -NHCO-; and m and n are each 0 or an integer from 1 to 5]; R is alkoxy, aralkyloxy, aryloxy or alkoxycarbonyl; R is optionally substituted alkyl, cycloalkyl, heterocyclic, aryl or arylalkenyl]; and pharmaceutically acceptable salts and esters thereof and pro-drugs therefor, have the ability to inhibit the activity of HIV protease and may thus be used for the treatment and prophylaxis of AIDS.