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    • 10. 发明授权
    • Symmetrical diaryl and diheteroanyl cis epoxy alkanes antiviral compounds
    • 对称二芳基和二偶氮烷基顺式环氧烷烃类抗病毒化合物
    • US5578608A
    • 1996-11-26
    • US372722
    • 1995-01-17
    • William J. HornbackJohn E. Munroe
    • William J. HornbackJohn E. Munroe
    • A61K31/335A61K31/336A61K31/415A61K31/4155A61K31/44A61K31/4427A61K31/443A61K31/47A61K31/4709A61K38/00A61P31/12A61P31/18A61P43/00C07D303/36C07D405/12C07D405/14C07D407/14C07D521/00C07K5/02C07K5/078C07D215/38C07D303/08
    • C07D231/12C07D233/56C07D249/08C07D303/36C07D405/12C07K5/021C07K5/06139A61K38/00
    • An HIV protease inhibiting compound of formula I ##STR1## wherein: R is C.sub.1 -C.sub.6 alkyl, cycloalkyl, heterocycle, unsaturated heterocycle, aryl, cycloalkyl (C.sub.1 -C.sub.4)alkyl, heterocycle(C.sub.1 -C.sub.4)alkyl, unsaturated heterocycle (C.sub.1 -C.sub.4)alkyl, aryl(C.sub.1 -C.sub.4)alkyl, or --A--(CH.sub.2).sub.q --R.sup.0, where A is --O--, --NH-- or --S--; q is 0, 1, 2 or 3; and R.sup.0 is cycloalkyl, aryl, heterocycle or unsaturated heterocycle; ##STR2## where R.sup.1 is aryl, cycloalkyl, heterocycle or unsaturated heterocycle; R.sup.2 is hydrogen or C.sub.1 -C.sub.4 alkyl; R.sup.3 is an amino acid side chain, --CH.sub.2 CH.sub.3, --CH.sub.2 CH.sub.2 CH.sub.3, --CH.sub.2 (CH.sub.2).sub.2 CH.sub.3, --C(CH.sub.3).sub.3, cyano(C.sub.1 -C.sub.4)alkyl, unsaturated heterocycle (C.sub.1 -C.sub.4)alkyl, aryl(C.sub.1 -C.sub.4)alkyl, --(CH.sub.2).sub.s --A.sup.0 --(CH.sub.2).sub.r --R.sup.4, or --CH.sub.2 --C(O)--NR.sup.2 --(CH.sub.2).sub.r --R.sup.5, where s is 1, 2, 3 or 4; r is 0, 1, 2 or 3; A.sup.0 is --O--, --NH-- or --S--; R.sup.4 is C.sub.1 -C.sub.6 alkyl, cycloalkyl, aryl, heterocycle or unsaturated heterocycle; R.sup.5 is cycloalkyl, aryl, heterocycle or unsaturated heterocycle; j is 0, 1, 2, 3 or 4; k is 0 or 1; and Y is --O--, --N(R.sup.2)-- or --S--; or a pharmaceutically acceptable salt thereof.
    • 式I的HIV蛋白酶抑制化合物其中:R是C1-C6烷基,环烷基,杂环,不饱和杂环,芳基,环烷基(C1-C4)烷基,杂环(C1-C4)烷基,不饱和杂环 -C 1-4)烷基,芳基(C 1 -C 4)烷基或-A-(CH 2)q -R 10,其中A是-O - , - NH-或-S-; q为0,1,2或3; 和R 0是环烷基,芳基,杂环或不饱和杂环; 其中R1是芳基,环烷基,杂环或不饱和杂环; R2是氢或C1-C4烷基; R3是氨基酸侧链,-CH2CH3,-CH2CH2CH3,-CH2(CH2)2CH3,-C(CH3)3,氰基(C1-C4)烷基,不饱和杂环(C1-C4)烷基,芳基(C1-C4 )(CH 2)s-A 0 - (CH 2)r -R 4或-CH 2 -C(O)-NR 2 - (CH 2)r -R 5,其中s是1,2,3或4; r为0,1,2或3; A 0是-O - , - NH-或-S-; R4是C1-C6烷基,环烷基,芳基,杂环或不饱和杂环; R5是环烷基,芳基,杂环或不饱和杂环; j为0,1,2,3或4; k为0或1; 并且Y是-O - , - N(R 2) - 或-S-; 或其药学上可接受的盐。