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    Amino acid derivatives
    2.
    发明授权
    Amino acid derivatives 失效
    氨基酸衍生物

    公开(公告)号：US06018020A

    公开(公告)日：2000-01-25

    申请号：US96570

    申请日：1998-06-12

    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 alkoxycarbonyl,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： 本发明提供下式的氨基酸衍生物，其中E代表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。

    Peptidyl inhibitors of viral proteases
    3.
    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。

    Therapeutic oxy-phenyl-aryl compounds and their use
    7.
    发明授权
    Therapeutic oxy-phenyl-aryl compounds and their use 有权
    治疗性氧 - 苯基 - 芳基化合物及其应用

    公开(公告)号：US08324226B2

    公开(公告)日：2012-12-04

    申请号：US12738808

    申请日：2008-10-23

    申请人： Ian Collins ,  John Jamieson Caldwell ,  Antony William Oliver ,  Tony Michael Raynham ,  Emma Jane Welsh ,  Cornelius Albertus Johannes Matijssen

    发明人： Ian Collins ,  John Jamieson Caldwell ,  Antony William Oliver ,  Tony Michael Raynham ,  Emma Jane Welsh ,  Cornelius Albertus Johannes Matijssen

    IPC分类号： A01N43/54 ,  A61K31/517

    CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D413/14

    摘要： The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain oxy phenyl aryl compounds (referred to herein as OPA compounds), as described herein, which, inter alia, inhibit Checkpoint Kinase 2 (CHK2) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK2 kinase function, and in the treatment of diseases and conditions that are mediated by CHK2, that are ameliorated by the inhibition of CHK2 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or II inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or TS inhibitor; (d) a microtubule targeted agent; and (e) ionising radiation.

    摘要翻译： 本发明一般涉及治疗化合物领域，更具体地涉及本文所述的某些氧苯基芳基化合物（本文称为OPA化合物），其特别地抑制了检测点激酶2（CHK2）激酶功能。 本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内的用途，以抑制CHK2激酶功能，以及用于治疗由CHK2介导的疾病和病症，即 通过抑制CHK2激酶功能等改善，包括增殖条件如癌症等，任选地与另一种试剂组合，例如（a）DNA拓扑异构酶I或II抑制剂; （b）DNA损伤剂; （c）抗代谢物或TS抑制剂; （d）微管靶向剂; 和（e）电离辐射。