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.sub.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; -A-R.sub.6 is
hydroxyC.sub.1-6alkyl; R.sub.5 and -A-R.sub.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.
