Broadspectrum substituted benzimidazole sulfonamide hiv protease inhibitors

Abstract

The present invention concerns the compounds having the formula N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein Rand Reach are H, optionally substituted Calkyl, Calkenyl, Ccycloalkyl, aryl, Het, Het; Rmay also be a radical of formula (RR)NC(RR)CR—; t is 0, 1 or 2; Ris H or Calkyl; L is —C(═O)—, —O—C(═O)—, —NR—C(═O)—, —O—Calkanediyl-C(═O)—, —NR—Calkanediyl-C(═O)—, —S(═O)—, —O—S(═O)—, —NR—S(═O); Ris Calkyl, aryl, Ccycloalkyl, CcycloalkylCalkyl, or arylCalkyl; Ris H, CalkylOC(═O), carboxyl, aminoC(═O), mono- or di(Calkyl)aminoC(═O), Ccycloalkyl, Calkenyl, Calkynyl or optionally substituted Calkyl; A is Calkanediyl, —C(═O)—, —C(═S)—, —S(═O)—, Calkanediyl-C(═O)—, Calkanediyl-C(═S)— or Calkanediyl-S(═O)—; Ris H, OH, Calkyl, HetCalkyl, HetCalkyl, optionally substituted amino-Calkyl; Ris CalkylO, Het, HetO, Het, HetO, aryl, arylO, Calkyloxy-carbonylamino or amino; and in case -A- is other than Calkanediyl then Rmay also be Calkyl, HetCalkyl, HetOCalkyl, HetCalkyl, HetOCalkyl, arylCalkyl, arylOCalkyl or aminoCalkyl; whereby each of the amino groups in the definition of Rmay optionally be substituted; Rand -A-Rtaken together with the nitrogen atom to which they are attached may also form Hetor Het' Ris H, —NH, —NRAR, —Calkyl or alkyl-W—R, wherein said alkyl is optionally substituted with halogen, hydroxy, aryl, heteroaryl, Het, Het, or amino wherein said amino is optionally mono- or di-substituted with Calkyl and Ris H, C-alkyl, optionally substituted by aryl, Het, Het, hydroxy, halogen, amino whereby the amino group may be optionally be mono- or di-substituted with Calkyl.