摘要 |
<p>Compounds of formula (I) : <CHEM> [wherein: R<1> is hydrogen, alkyl, aralkyl, -COR<a>, -COR<b>, -CSR<a>, -CSR<b>, -SO2R<b>, -CONHR<b>, -CSNHR<b>, -CONR<b>R<b> or -CSNR<b>R<b>; R<2> is hydrogen or alkyl; R<3> is hydrogen, alkylidene, substituted alkyl, or R<b>; R<4> is optionally substituted alkyl, cycloalkyl, or aryl; R<5> is R<b>O-, R<b>R<b>N-, R<b>HN-, 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<a> is alkoxy, aralkyloxy, aryloxy or alkoxycarbonyl; R<b> 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.</p> |