Broadspectrum 2- (substituted-amino) -benzoxazole sulfonamide HIV protease inhibitors.

The present invention concerns the compounds having the formula (I) N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R1 and R8 each are H, optionally substituted Cl-6alkyl, C2-6alkenyl, C3-7cycloalkyl, aryl, Hetl, Het2; Rl may also be a radical of formula (RIlaRllb)NC(R10aR10b)CR9-; t is 0,1 or 2; R2 is H or Cl-6alkyl; L is -C(=O)-, -O-C(=O)-, -NR8-Q=O)-, -O-Cl-6alkanediyl-C(=O)-, -NR8-Cl-6alkanediyl-C(=O-, -S(=O)2-, -O-S(=O)2-, -NR8-S(=O)2 ; R3 is Cl-6alkyl, aryl, C3-7cycloalkyl, C3-7cycloalkylCl-4alkyl, or arylCl-4alkyl; R4 is H, Cl-4.alkylOC(=O), carboxyl, aminoC(=O), mono- or di(Cl-4alkyl)aminoC(=O), C3-7cycloalkyl, C2-6alkenyl, C2-6alkynyl or optionally substituted Cl-6alkyl; A is Cl-6alkanediyl, -C(=O, -C(=S)-, -S(=O)2-, Cl-6alkanediyl-C(=O)-, Cl-6alkanediyl-C(=S)- or Cl-6alkanediyl-S(=O)2-; R5 is H, OH, Cl-6alkyl, HetlCl-6alkyl, Het2Cl-6alkyl, optionally substituted aminoCl-6aIkyl; R6 is Cl-6alkylO, Hetl, HetlO, Het2, Het2O, aryl, arylO, Cl-6alkyloxcarbonylamino or amino; and in case -A- is other than Cl-6alkanediyl then R6 may also be Cl-6alkyl, HetlCl-4alkyl, HetlOCl-4alkyl, Het2Cl-4alkyl, Het2OCl-4alkyl, arylC1-4alkyl, arylOCl-4alkyl or aminoCl-4alkyl; whereby each of the amino groups in the definition of R6 may optionally be substituted; -A-R6 is hydroxyCl-6alkyl; R5 and -A-R6 taken together with the nitrogen atom to which they are attached may also form Hetl or Het2. It further relates to their use as broadspectrum HTV 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.