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    Amino acid derivatives
    1.
    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。

    1H-[1,2,3]TRIAZOLO[4,5-c]PYRIDINE-4-CARBONITRILE DERIVATIVES
    9.
    发明申请
    1H-[1,2,3]TRIAZOLO[4,5-c]PYRIDINE-4-CARBONITRILE DERIVATIVES 有权
    1H- [1,2,3]三唑[4,5-c]吡啶-4-羰基衍生物

    公开(公告)号：US20120283239A1

    公开(公告)日：2012-11-08

    申请号：US13519924

    申请日：2011-01-13

    申请人： Jiaqiang Cai ,  David Jonathan Bennett ,  Philip Stephen Jones

    发明人： Jiaqiang Cai ,  David Jonathan Bennett ,  Philip Stephen Jones

    IPC分类号： C07D471/04 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/54 ,  A61P25/00 ,  A61P19/10 ,  A61P9/10 ,  A61P29/00 ,  A61P37/00 ,  A61P17/06 ,  A61K31/437 ,  A61K31/551

    CPC分类号： C07D471/04

    摘要： The invention relates to 1H-[1,2,3]triazolo[4,5-c]pyridine-4-carbonitrile derived Cathepsin S inhibitors of Formula (I), wherein R1 is H or (C1-3)alkyl; R2 is halogen or (C1-4)alkyl, optionally substituted with one or more halogens; n is 1-3; X is O or CH2; U, V and W are CH; or one of U, V and W is N; Y is a group capable of interacting with the Sn . . . S2 substites of the active site of Cathepsin S; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament for the treatment of cathepsin S related diseases such as atherosclerosis, obesity, inflammation and immune disorders, such as rheumatoid arthritis, psoriasis, cancer, and chronic pain, such as neuropathic pain.

    摘要翻译： 本发明涉及式（I）的1H- [1,2,3]三唑并[4,5-c]吡啶-4-腈衍生的组织蛋白酶S抑制剂，其中R 1是H或（C 1-3）烷基; R 2是卤素或任选被一个或多个卤素取代的（C 1-4）烷基; n为1-3; X是O或CH2; U，V和W是CH; 或U，V和W之一为N; Y是能够与Sn相互作用的组。 。 。 组织蛋白酶S活性位点的S2位点; 或其药学上可接受的盐用于包含其的药物组合物以及这些衍生物用于制备用于治疗组织蛋白酶S相关疾病如动脉粥样硬化，肥胖症，炎症和免疫疾病如类风湿病的药物中的用途 关节炎，牛皮癣，癌症和慢性疼痛，如神经性疼痛。