The present invention concerns the compounds having the formula
##STR00001## N-oxides, salts, stereoisomeric forms, racemic mixtures,
prodrugs, esters and metabolites thereof, wherein R.sub.1 and R.sub.8
each are H, optionally substituted C.sub.1-6alkyl, C.sub.2-6alkenyl,
C.sub.3-7cycloalkyl, aryl, Het.sup.1, Het.sup.2; R.sub.1 may also be a
radical of formula (R.sub.11aR.sub.11b)NC(R.sub.10aR.sub.10b)CR.sub.9--;
t is 0, 1 or 2; R.sub.2 is H or C.sub.1-6alkyl; L is --C(.dbd.O)--,
--O--C(.dbd.O)--, --NR.sub.8--C(.dbd.O)--,
--O--C.sub.1-6alkanediyl-C(.dbd.O)--,
--NR.sub.8--C.sub.1-6alkanediyl-C(.dbd.O)--, --S(.dbd.O).sub.2--,
--O--S(.dbd.O).sub.2--, --NR.sub.8--S(.dbd.O).sub.2; R.sub.3 is
C.sub.1-6alkyl, aryl, C.sub.3-7cycloalkyl,
C.sub.3-7cycloalkylC.sub.1-4alkyl, or arylC.sub.1-4alkyl; R.sub.4 is H,
C.sub.1-4alkylOC(.dbd.O), carboxyl, aminoC(.dbd.O), mono- or
di(C.sub.1-4alkyl)aminoC(.dbd.O), C.sub.3-7cycloalkyl, C.sub.2-6alkenyl,
C.sub.2-6alkynyl or optionally substituted C.sub.1-6alkyl; A is
C.sub.1-6alkanediyl, --C(.dbd.O)--, --C(.dbd.S)--, --S(.dbd.O).sub.2--,
C.sub.1-6alkanediyl-C(.dbd.O)--, C.sub.1-6alkanediyl-C(.dbd.S)-- or
C.sub.1-6alkanediyl-S(.dbd.O).sub.2--; R.sub.5 is H, OH, C.sub.1-6alkyl,
Het.sup.1C.sub.1-6alkyl, Het.sup.2C.sub.1-6alkyl, optionally substituted
aminoC.sub.1-6alkyl; R.sub.6 is C.sub.1-6alkylO, Het.sup.1, Het.sup.1O,
Het.sup.2, Het.sup.2O, aryl, arylO, C.sub.1-6alkyloxycarbonylamino or
amino; and in case --A-- is other than C.sub.1-6alkanediyl then R.sup.6
may also be C.sub.1-6alkyl, Het.sup.1C.sub.1-4alkyl,
Het.sup.1OC.sub.1-4alkyl, Het.sup.2C.sub.1-4alkyl,
Het.sup.2OC.sub.1-4alkyl, arylC.sub.1-4alkyl, arylOC.sub.1-4alkyl or
aminoC.sub.1-4alkyl; whereby each of the amino groups in the definition
of R.sub.6 may optionally be substituted; R.sup.5 and --A--R.sup.6 taken
together with the nitrogen atom to which they are attached may also form
Het.sup.1 or Het.sup.2. It further relates to their use as broadspectrum
HIV protease inhibitors, processes for their preparation as well as
pharmaceutical compositions and diagnostic kits comprising them. It also
concerns combinations thereof with another anti-retroviral agent, and to
their use in assays as reference compounds or as reagents.
