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11 条记录 (耗时 0.023 秒)

    Reverse-turn mimetics and compositions and methods relating thereto
    3.
    发明申请
    Reverse-turn mimetics and compositions and methods relating thereto 有权
    反转模拟物及其组合物和方法

    公开(公告)号：US20050250780A1

    公开(公告)日：2005-11-10

    申请号：US11108267

    申请日：2005-04-18

    申请人： Maher Qabar ,  Marcin Stasiak ,  Jessymol Mathew ,  Thomas Little ,  Danwen Huang

    发明人： Maher Qabar ,  Marcin Stasiak ,  Jessymol Mathew ,  Thomas Little ,  Danwen Huang

    IPC分类号： A61K31/525 ,  A61P29/00 ,  C07D487/04

    CPC分类号： C07D487/04

    摘要： Reverse-turn mimetics and methods relating to the same having the following structure are disclosed: including pharmaceutically acceptable salts and stereoisomers thereof, wherein R1, R2, R3 and R4 are as defined herein. Such compounds have utility over a wide range of applications, including use as diagnostic and therapeutic agents. In particular, compounds of this invention, and pharmaceutical compositions containing such compounds, are neurokinin (tachykinin) antagonists. Libraries containing the reverse-turn mimetics of this invention are also disclosed.

    摘要翻译： 公开了具有下列结构的逆转模拟物及其相关方法：包括其药学上可接受的盐和立体异构体，其中R 1，R 2，R 2， 3＆gt;和R 4＆gt;如本文所定义。 这些化合物在广泛的应用中具有应用价值，包括用作诊断和治疗剂。 特别地，本发明的化合物和含有这些化合物的药物组合物是神经激肽（速激肽）拮抗剂。 还公开了包含本发明的反转模拟物的文库。

    Helix mimetics and composition and methods related thereto
    4.
    发明授权
    Helix mimetics and composition and methods related thereto 有权
    螺旋模拟物及其组成和方法

    公开(公告)号：US07405212B2

    公开(公告)日：2008-07-29

    申请号：US11121337

    申请日：2005-05-03

    申请人： Vincent Huber ,  Jan Urban ,  Hiroshi Nakanishi ,  Masakatsu Eguchi ,  Jessymol Mathew ,  Min Sang Lee

    发明人： Vincent Huber ,  Jan Urban ,  Hiroshi Nakanishi ,  Masakatsu Eguchi ,  Jessymol Mathew ,  Min Sang Lee

    IPC分类号： C07D498/08 ,  C07D263/00

    CPC分类号： C40B40/04 ,  C07D487/08 ,  C07D513/08 ,  C40B30/04

    摘要： Compounds which mimic the secondary structure of helical regions of biologically active peptides and proteins having the following structure: including pharmaceutically acceptable salts and stereoisomers thereof, wherein Y, A, B, R1 and R2 are as defined herein. Such compounds have utility over a wide range of applications, including use as diagnostic and therapeutic agents. In particular, compounds of this invention, and pharmaceutical compositions containing the same, are neurokinin (tachykinin) antagonists. Libraries containing the compounds of this invention are also disclosed, as well as methods for screening such libraries to identify biologically active members.

    摘要翻译： 模拟具有以下结构的生物活性肽和蛋白质的螺旋区域的二级结构的化合物：包括其药学上可接受的盐和立体异构体，其中Y，A，B，R 1和R 2 如本文所定义。 这些化合物在广泛的应用中具有应用价值，包括用作诊断和治疗剂。 特别地，本发明的化合物和含有它们的药物组合物是神经激肽（速激肽）拮抗剂。 还公开了含有本发明化合物的文库，以及筛选这些文库以鉴定生物活性成员的方法。

    Reverse-turn mimetics and compositions and methods relating thereto
    8.
    发明授权
    Reverse-turn mimetics and compositions and methods relating thereto 有权
    反转模拟物及其组合物和方法

    公开(公告)号：US07345040B2

    公开(公告)日：2008-03-18

    申请号：US11108267

    申请日：2005-04-18

    申请人： Maher N. Qabar ,  Marcin Stasiak ,  Jessymol Mathew ,  Thomas Little ,  Danwen Huang

    发明人： Maher N. Qabar ,  Marcin Stasiak ,  Jessymol Mathew ,  Thomas Little ,  Danwen Huang

    IPC分类号： A61K31/5025 ,  C07D471/04 ,  C07D487/04

    CPC分类号： C07D487/04

    摘要： Reverse-turn mimetics and methods relating to the same having the following structure are disclosed: including pharmaceutically acceptable salts and stereoisomers thereof, wherein R1, R2, R3 and R4 are as defined herein. Such compounds have utility over a wide range of applications, including use as diagnostic and therapeutic agents. In particular, compounds of this invention, and pharmaceutical compositions containing such compounds, are neurokinin (tachykinin) antagonists. Libraries containing the reverse-turn mimetics of this invention are also disclosed.

    摘要翻译： 公开了具有下列结构的逆转模拟物及其相关方法：包括其药学上可接受的盐和立体异构体，其中R 1，R 2，R 2， 3＆gt;和R 4＆gt;如本文所定义。 这些化合物在广泛的应用中具有应用价值，包括用作诊断和治疗剂。 特别地，本发明的化合物和含有这些化合物的药物组合物是神经激肽（速激肽）拮抗剂。 还公开了包含本发明的反转模拟物的文库。