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    Peptidyl inhibitors of viral proteases
    7.
    发明授权
    Peptidyl inhibitors of viral proteases 失效
    肽基蛋白酶抑制剂

    公开(公告)号：US5866684A

    公开(公告)日：1999-02-02

    申请号：US971036

    申请日：1997-11-14

    申请人： Michael Richard Attwood ,  David Nigel Hurst ,  Philip Stephen Jones ,  Paul Brittain Kay ,  Tony Michael Raynham ,  Francis Xavier Wilson

    发明人： Michael Richard Attwood ,  David Nigel Hurst ,  Philip Stephen Jones ,  Paul Brittain Kay ,  Tony Michael Raynham ,  Francis Xavier Wilson

    IPC分类号： C12N15/09 ,  A01N43/34 ,  A01N43/36 ,  A61K38/00 ,  A61P31/12 ,  A61P31/14 ,  C07C205/04 ,  C07C205/45 ,  C07C271/18 ,  C07D207/12 ,  C07D207/20 ,  C07D211/70 ,  C07D223/04 ,  C07D227/04 ,  C07D405/10 ,  C07D407/10 ,  C07D409/10 ,  C07K7/06 ,  A61K38/08

    CPC分类号： C07K7/06 ,  A61K38/00

    摘要： The invention provides amino acid derivatives of the formula ##STR1## wherein E represents CHO or B(OH).sub.2 ;R.sup.1 represents lower alkyl (optionally substituted by halo, cyano, lower alkylthio, aryl-lower alkylthio, aryl or heteroaryl), lower alkenyl or lower alkynyl;R.sup.2 represents lower alkyl optionally substituted by hydroxy, carboxy, aryl, aminocarbonyl or lower cycloalkyl; andR.sup.3 represents hydrogen or lower alkyl; orR.sup.2 and R.sup.3 together represent di- or trimethylene optionally substituted by hydroxy;R.sup.4 represents lower alkyl (optionally substituted by hydroxy, lower cycloalkyl, carboxy, aryl, lower alkylthio, cyano-lower alkylthio or aryl-lower alkylthio), lower alkenyl, aryl or lower cycloalkyl;R.sup.5 represents lower alkyl (optionally substituted by hydroxy, lower alkylthio, aryl, aryl-lower alkylthio or cyano-lower alkylthio) or lower cycloalkyl;R.sup.6 represents hydrogen or lower alkyl;R.sup.7 represent lower alkyl (optionally substituted by hydroxy, carboxy, aryl or lower cycloalkyl) or lower cycloalkyl;R.sup.8 represents lower alkyl optionally substituted by hydroxy, carboxy or aryl; andR.sup.9 represents lower alkylcarbonyl, carboxy-lower alkylcarbonyl, arylcarbonyl, lower alkylsulphonyl, arylsulphonyl, lower alkoxycarbonyl or aryl-lower al koxycarbonyl,and salts of acidic compounds of formula I with bases, which are viral proteinase inhibitors useful as antiviral agents, especially for the treatment or prophylaxis of infections caused by Hepatitis C, Hepatitis G and human GB viruses.

    摘要翻译： 本发明提供式（I）的氨基酸衍生物，其中E表示CHO或B（OH）2; R 1表示低级烷基（任选被卤素，氰基，低级烷硫基，芳基 - 低级烷硫基，芳基或杂芳基取代），低级烯基或低级炔基; R 2表示任选被羟基，羧基，芳基，氨基羰基或低级环烷基取代的低级烷基; 并且R 3表示氢或低级烷基; 或R 2和R 3一起表示任选被羟基取代的二 - 或三亚甲基; R4代表低级烷基（任选被羟基，低级环烷基，羧基，芳基，低级烷硫基，氰基 - 低级烷硫基或芳基 - 低级烷硫基取代），低级烯基，芳基或低级环烷基; R5代表低级烷基（任选被羟基，低级烷硫基，芳基，芳基 - 低级烷硫基或氰基 - 低级烷硫基取代）或低级环烷基; R6代表氢或低级烷基; R7代表低级烷基（任选被羟基，羧基，芳基或低级环烷基取代）或低级环烷基; R8代表任选被羟基，羧基或芳基取代的低级烷基; 并且R 9表示低级烷基羰基，羧基 - 低级烷基羰基，芳基羰基，低级烷基磺酰基，芳基磺酰基，低级烷氧基羰基或芳基 - 低级烷氧基羰基，以及式I酸性化合物与碱的碱，其为用作抗病毒剂的病毒蛋白酶抑制剂， 治疗或预防丙型肝炎，丙型肝炎和人类GB病毒引起的感染。