HIV-PROTEASE INHIBITOR USEFUL FOR MEDICAL TREATMENT OF AIDS

摘要

The present invention provides novel HIV protease inhibitors, of formula I wherein: Z is hydrogen, formyl, carbamoyl, C2-C6 alkanoyl, C1-C4 alkoxycarbonyl, -C(O)CF3 or -S(O)2-R, where R is C1-C6 alkyl, amino, trifluoromethyl, C1-C4 alkylamino, di(C1-C4)alkylamino, aryl, aryl(C1-C4)alkyl, heterocycle, unsaturated heterocycle or C5-C7 cycloalkyl; R<1> is aryl, C5-C7 cycloalkyl or -S-R<1x>, where R<1x> is aryl or C5-C7 cycloalkyl; R<2> is an amino acid side chain, -(CH2)y-X-R<2a>, cyano(C1-C4)alkyl or -(CH2)y-S(O)w-[1-N(R<2c>)-tetrazol-5-yl], where y is 0, 1, 2 or 3; X is a bond, divalent(C2-C4)alkenyl, divalent(C2-C4)alkynyl, -C(O)-O-, -O-C(O)-, -C(O)-NR<2b>-, -NR<2b>-C(O)-, -NR<2b>-, -C(O)-, -O-, -S(O)w-; w is 0, 1 or 2; R<2a> is C1-C6 alkyl, aryl, unsaturated heterocycle, heterocycle, aryl(C1-C4)alkyl, unsaturated heterocycle(C1-C4)alkyl or heterocycle(C1-C4)alkyl; R<2b> is hydrogen or C1-C4 alkyl; R<2c> is hydrogen, C1-C6 alkyl, aryl, unsaturated heterocycle, aryl(C1-C4)alkyl or unsaturated heterocycle(C1-C4)alkyl; Y is aryl or unsaturated heterocycle; R<3> is a group having the structure: where: p is 4 or 5; l is 3, 4 or 5; R<4> at each occurrence is independently hydrogen, C1-C6 alkyl or hydroxy(C1-C4)alkyl; R<5> and R<6> are independently selected from hydrogen, hydroxy, C1-C6 alkyl, C1-C6 alkoxy, amino, C1-C4 alkylamino, hydroxy(C1-C4)alkyl, carboxy, C1-C4 alkoxycarbonyl, carbamoyl, N-(C1-C4)alkylcarbamoyl, aryl, heterocycle or unsaturated heterocycle; o