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    Reverse-turn mimetics and compositions and methods related thereto
    1.
    发明授权
    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：US07407952B2

    公开(公告)日：2008-08-05

    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： A61P29/00 ,  A61P35/04 ,  A61P17/00 ,  A61P25/06

    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 compositions and methods related thereto
    2.
    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
    3.
    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。

    Reverse-turn mimetics and methods relating thereto
    5.
    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：US07008941B2

    公开(公告)日：2006-03-07

    申请号：US10150481

    申请日：2002-05-16

    申请人： Jan Urban ,  Hiroshi Nakanishi ,  Min S. Lee

    发明人： Jan Urban ,  Hiroshi Nakanishi ,  Min S. Lee

    IPC分类号： G01N33/53 ,  G08D498/04

    CPC分类号： C07D487/04 ,  C07D487/14

    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, B, X, R1, and R5 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向转转区域的二级结构的构象约束化合物：其中A，B，X，R 1和R 5， / SUB>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 methods relating thereto
    8.
    发明申请
    Reverse-turn mimetics and methods relating thereto 审中-公开

    公开(公告)号：US20060079517A1

    公开(公告)日：2006-04-13

    申请号：US11292611

    申请日：2005-12-02

    申请人： Jan Urban ,  Hiroshi Nakanishi ,  Min Lee

    发明人： Jan Urban ,  Hiroshi Nakanishi ,  Min Lee

    IPC分类号： A61K31/5415 ,  A61K31/498

    CPC分类号： C07D487/04 ,  C07D487/14

    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, B, X, R1, and R5 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.

    Helix mimetics and composition and methods related thereto
    9.
    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。