PEPTIDES CAPABLE OF INHIBITING THE ACTIVITY OF HIV PROTEASE, THEIR PREPARATION AND THEIR USE

摘要

Compounds of formula (I): (I) ¢wherein: R1 is hydrogen, alkyl, aralkyl, -CORa, -CORb, -CSRa, -CSRb, -SO2Rb, -CONHRb, -CSNHRb, -CONRbRb or -CSNRbRb; R2 is hydrogen or alkyl; R3 is hydrogen, alkylidene, substituted alkyl, or Rb; R4 is optionally substituted alkyl, cycloalkyl, or aryl; R5 is RbO-, RbRbN-, RbHN-, aralkyloxycarbonyloxy or aralkyloxycarbonylamino, or R5 is -(CH2)p-D-(CH2)r-¢where D is a single bond, carbonyl, oxygen, sulfur, -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, sulfur, -NH-, -(CH2=CH2)- or -NHCO-; and m and n are each 0 or an integer from 1 to 5!; Ra is alkoxy, aralkyloxy, aryloxy or alkoxycarbonyl; Rb 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.