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21 条记录 (耗时 0.043 秒)

    Reverse-turn mimetics and compositions and methods relating thereto
    1.
    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。

    Reverse-turn mimetics and compositions and methods relating thereto
    2.
    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。

    Reverse-turn mimetics and methods relating thereto
    4.
    发明授权
    Reverse-turn mimetics and methods relating thereto 有权
    反转模拟物及其相关方法

    公开(公告)号：US06294525B1

    公开(公告)日：2001-09-25

    申请号：US09388854

    申请日：1999-09-01

    申请人： Marcin Stasiak ,  Michael Kahn

    发明人： Marcin Stasiak ,  Michael Kahn

    IPC分类号： A61K2133

    CPC分类号： C07D487/04 ,  A61K38/00 ,  C07K5/06139 ,  C40B40/00 ,  G01N2333/70546

    摘要： Conformationally constrained compounds which mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins having the following structure are disclosed: wherein A, R1, R2, R2a, R3, R3a and R4 are as defined herein. Such compounds have utility over a wide range of fields, including use as diagnostic and therapeutic agents. In particular, compounds of this invention are useful in pharmaceutical compositions as anti-inflammatory agents. Libraries containing the compounds of this invention are also disclosed, as well as methods for screening the same to identify biologically active members.

    摘要翻译： 公开了具有以下结构的模拟具有生物活性肽和蛋白质的反向转转区域的二级结构的构象约束化合物：其中A，R1，R2，R2a，R3，R3a和R4如本文所定义。 这些化合物可用于广泛的领域，包括用作诊断和治疗剂。 特别地，本发明的化合物可用作药物组合物作为抗炎剂。 还公开了含有本发明化合物的文库，以及筛选该文库以鉴定生物活性成员的方法。