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23 条记录 (耗时 0.023 秒)

    Alpha-helix mimetics and methods relating thereto
    12.
    发明授权
    Alpha-helix mimetics and methods relating thereto 失效
    α-螺旋模拟物及其相关方法

    公开(公告)号：US5859184A

    公开(公告)日：1999-01-12

    申请号：US846431

    申请日：1997-04-30

    申请人： Michael Kahn ,  Hwa-Ok Kim ,  Jan Urban

    发明人： Michael Kahn ,  Hwa-Ok Kim ,  Jan Urban

    IPC分类号： C07K5/12 ,  C07K7/02 ,  C07K14/575 ,  C07K1/04 ,  C07K1/113 ,  C07K2/00

    CPC分类号： C07K7/02 ,  C07K14/57545 ,  C07K5/123

    摘要： There are disclosed alpha-helix mimetics and methods relating to the same for imparting or stabilizing alpha-helicity to a peptide or protein. In one aspect, the alpha-helix mimetics contain eleven- to fourteen-membered rings covalently attached at the end or within the length of the peptide or protein. The alpha-helix mimetics render the resulting peptide or protein more stable with regard to thermal stability, as well as making the peptide or protein more resistant to proteolytic degradation. In addition, the alpha-helix mimetics may be used in standard peptide synthesis protocols.

    摘要翻译： 已经公开了α-螺旋模拟物和涉及赋予或稳定肽或蛋白质的α-螺旋性的方法。 在一个方面，α-螺旋模拟物含有在肽或蛋白质的末端或长度内共价连接的十一至十四元环。 α-螺旋模拟物使所得肽或蛋白质在热稳定性方面更稳定，以及使肽或蛋白质对蛋白水解降解更具抗性。 此外，α-螺旋模拟物可用于标准肽合成方案中。

    Reverse-turn mimetics and compositions and methods related thereto
    14.
    发明申请
    Reverse-turn mimetics and compositions and methods related thereto 有权
    反转模拟物及其组合物和方法

    公开(公告)号：US20050245528A1

    公开(公告)日：2005-11-03

    申请号：US11175920

    申请日：2005-07-06

    申请人： Gangadhar Nagula ,  Jan Urban ,  Hwa-Ok Kim ,  Christopher Lum ,  Hiroshi Nakanishi

    发明人： Gangadhar Nagula ,  Jan Urban ,  Hwa-Ok Kim ,  Christopher Lum ,  Hiroshi Nakanishi

    IPC分类号： C07D487/04 ,  A61K31/498

    CPC分类号： C07D487/04

    摘要： Conformationally constrained compounds that 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 and R3 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 as well as inhibitors of central nervous disorders. 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转转区的二级结构的构象约束的化合物：其中A，R 1，R 2，R 2a和R 3'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作为抗炎剂的药物组合物以及中枢神经障碍的抑制剂。 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。

    Reverse-turn mimetics and composition and methods relating thereto
    15.
    发明授权
    Reverse-turn mimetics and composition and methods relating thereto 有权
    反转模拟物及其组合和方法

    公开(公告)号：US06943157B2

    公开(公告)日：2005-09-13

    申请号：US10268062

    申请日：2002-10-09

    申请人： Gangadhar Nagula ,  Jan Urban ,  Hwa-Ok Kim ,  Christopher Lum ,  Hiroshi Nakanishi

    发明人： Gangadhar Nagula ,  Jan Urban ,  Hwa-Ok Kim ,  Christopher Lum ,  Hiroshi Nakanishi

    IPC分类号： C07D487/04 ,  A61K31/519 ,  A61K31/55

    CPC分类号： C07D487/04

    摘要： Conformationally constrained compounds that 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 and R3 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 as well as inhibitors of central nervous disorders. 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转转区的二级结构的构象约束的化合物：其中A，R 1，R 2，R 2a和R 3'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作为抗炎剂的药物组合物以及中枢神经障碍的抑制剂。 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。

    Beta-sheet mimetics and composition and methods relating thereto
    17.
    发明申请
    Beta-sheet mimetics and composition and methods relating thereto 审中-公开
    β-折叠模拟物及其组合和方法

    公开(公告)号：US20060084653A1

    公开(公告)日：2006-04-20

    申请号：US11295833

    申请日：2005-12-06

    申请人： Cyprian Ogbu ,  Hwa-Ok Kim ,  Mark Blaskovich

    发明人： Cyprian Ogbu ,  Hwa-Ok Kim ,  Mark Blaskovich

    IPC分类号： A61K31/503 ,  A61K31/4745 ,  A61K31/454 ,  C07D487/04

    CPC分类号： C07D487/04 ,  C40B40/00

    摘要： Compounds having the following structure: including pharmaceutically acceptable salts and stereoisomers thereof, wherein A, A′, B, X, Y, R2, R3, R4 and R5 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 tryptase antagonists.

    摘要翻译： 具有以下结构的化合物：包括其药学上可接受的盐和立体异构体，其中A，A'，B，X，Y，R 2，R 3， 4和R 5 5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类胰蛋白酶拮抗剂。