BROAD SPECTRUM SUBSTITUTED BENZIMIDAZOLE SULFONAMIDE HIV PROTEASE INHIBITORS

摘要

The present invention concerns the compounds having the formula (I), wherein N-oxides, salts, stereoisomeric forms, racemic mixtures or esters, wherein Ris Calkyl, mono-, di- or trisubstituted phenyl, where the substituents are selected from the group comprising methyl, nitro, amino, mono- or dimethylamino, hydroxy, CN, aminomethyl, wherein at least one of said substituents is in ortho vis-a-vis the R-L bond, pyridinyl, thiazolyl, tetrahydrofuranyl, isoxazolyl substituted with Calkyl, or hexahydrofuro [2, 3-b] furanyl; Ris hydrogen; L is-O-CH-C (=O)-, -O-C (=O)-, C (=O)-, or –CH-C (=O)-, Ris phenyl substituted with Calkyl; Ris Calkyl; Ris hydrogen, NH, Calkyl optionally substituted with hydroxy, phenylamide, substituted with a methoxy group, -NH-C(=O) O-Calkyl, -NH-C(=O)-Calkyl, -NH-C(=O)-O-(CH)-, N(CH), NH-(CH)-pyrrolidine, -NH-C(=O)-O- CH)-N(CH)or a groupRis hydrogen, H, Calkyl, optionally substituted with Calkyl, phenyl, pyridinyl, pyrrolidinyl, imidazolylmethyl, hydroxy or amino, where aminogroup is disubstituted with Calkyl; or the N-oxides, salts, stereoisomeric forms, racemic mixtures or esters thereof provided the exclusion the compound which is phenylmethyl ester N-[2R-hydroxy-3-[[(2-amino benzumidazol-5-yl) sulfonyl] (2-methylpropyl) amino-1S-(phenylmethyl)propyl] carbamic acid and a compound in which Ris phenylmethyl, L is -O-C (=O)-, Ris phenylmethyl, Ris isobutyl, Ris –NH-C(=O)-O-CHand Ris hydrogen.