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    High affinity small molecule C5a receptor modulators
    1.
    发明授权
    High affinity small molecule C5a receptor modulators 失效
    高亲和力小分子C5a受体调节剂

    公开(公告)号：US06723743B1

    公开(公告)日：2004-04-20

    申请号：US09672071

    申请日：2000-09-28

    申请人： Andrew Thurkauf ,  Xiao-shu He ,  He Zhao ,  John Peterson ,  Xiaoyan Zhang ,  Robbin Brodbeck ,  James Krause ,  George Maynard ,  Alan Hutchison

    发明人： Andrew Thurkauf ,  Xiao-shu He ,  He Zhao ,  John Peterson ,  Xiaoyan Zhang ,  Robbin Brodbeck ,  James Krause ,  George Maynard ,  Alan Hutchison

    IPC分类号： A61K31415

    CPC分类号： C07D207/327 ,  C07C233/11 ,  C07C233/22 ,  C07C233/65 ,  C07C233/66 ,  C07C233/73 ,  C07C233/78 ,  C07C235/46 ,  C07C235/48 ,  C07C235/54 ,  C07C235/60 ,  C07C235/62 ,  C07C235/66 ,  C07C237/20 ,  C07C323/62 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/08 ,  C07C2602/10 ,  C07C2603/18 ,  C07D213/38 ,  C07D213/82 ,  C07D215/12 ,  C07D217/04 ,  C07D217/06 ,  C07D217/14 ,  C07D217/16 ,  C07D231/12 ,  C07D233/64 ,  C07D233/68 ,  C07D235/02 ,  C07D235/14 ,  C07D235/18 ,  C07D317/58 ,  C07D333/24 ,  C07D333/28 ,  C07D333/54 ,  C07D401/06 ,  C07D401/12 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12 ,  C07D471/04

    摘要： This invention relates to low molecular weight, non-peptidic, non-peptidomimetic, organic molecules that act as modulators of mammalian complement C5a receptors, preferably ones that act as high affinity C5a receptor ligands and also to such ligands that act as antagonists or inverse agonists of complement C5a receptors, preferably human C5a receptors, Preferred compounds of the invention possess one or more, and preferably two or more, three or more, four or more, or all of the following properties in that they are; 1) multi-aryl in structure (having a plurality of un-fused or fused aryl groups), 2) heteroaryl in structure, 3) orally available in vivo (such that a sub-lethal or preferably a pharmaceutically acceptable oral dose can provide a detectable in vitro effect such as a reduction of C5a-induced neutropenia), 4) comprised of fewer than four, preferably fewer than three, or fewer than two, or no amide bonds, and 5) capable of inhibiting leukocyte chemotaxis at nanomolar concentrations and preferably at sub-nanomolar concentrations. Specifically exemplified representative compounds include, but are not limited to optionally substituted arylimidazoles, optionally substituted arylpyridyls, optionally substituted aryl-substituted cycloalkylimidazoles, optionally substituted arylpyrazoles, optionally substituted benzimidazoles, optionally substituted aryl-substituted tetrahydroisoquinolines, and optionally substituted biaryl carboxamides. This invention also relates to pharmaceutical compositions comprising such compounds. It further relates to the use of such compounds in treating a variety of inflammatory and immune system disorders. Additionally, this invention relates to the use such compounds as probes for the localization of C5a receptors.

    摘要翻译： 本发明涉及作为哺乳动物补体C5a受体调节剂的低分子量，非肽，非拟肽，有机分子，优选用作高亲和力C5a受体配体的调节剂，还涉及作为拮抗剂或反向激动剂的这些配体 的补体C5a受体，优选人C5a受体。本发明的优选化合物具有一个或多个，优选两个或更多个，三个或更多个，四个或更多个或全部以下性质： 1）结构上的多芳基（具有多个未稠合或稠合芳基），2）结构上的杂芳基，3）在体内可口服（使得亚致死或优选药学上可接受的口服剂量可提供 可检测的体外效应，例如C5a诱导的中性粒细胞减少的减少），4）由少于4个，优选少于3个，或少于2个或不存在的酰胺键组成，以及5）能够以纳摩尔浓度抑制白细胞趋化性， 优选亚纳摩尔浓度。 具体示例的代表性化合物包括但不限于任选取代的芳基咪唑，任选取代的芳基吡啶基，任选取代的芳基取代的环烷基咪唑，任选取代的芳基吡唑，任选取代的苯并咪唑，任选取代的芳基取代的四氢异喹啉和任选取代的双芳基甲酰胺。 本发明还涉及包含这些化合物的药物组合物。 它还涉及这些化合物在治疗各种炎性和免疫系统疾病中的应用。 此外，本发明涉及使用这些化合物作为C5a受体定位的探针。

    Chimeric neuropeptide Y receptors
    3.
    发明申请
    Chimeric neuropeptide Y receptors 审中-公开
    嵌合神经肽Y受体

    公开(公告)号：US20050221428A1

    公开(公告)日：2005-10-06

    申请号：US11029242

    申请日：2005-01-04

    申请人： Michele Kinrade ,  Robbin Brodbeck ,  James Krause

    发明人： Michele Kinrade ,  Robbin Brodbeck ,  James Krause

    IPC分类号： C12N15/09 ,  A61K45/00 ,  A61P9/00 ,  A61P25/00 ,  A61P25/22 ,  C07K14/705 ,  C07K19/00 ,  C12N5/10 ,  C12Q1/02 ,  C12R1/91 ,  C07H21/04

    CPC分类号： C07K14/70571

    摘要： Novel chimeric G-protein coupled receptors are provided as isolated polypeptides, membrane preparations containing such chimeric receptors, nucleic acids encoding such chimeric receptors, and cells expressing such receptors. The chimeric receptors are NPY5 receptors with most or all of either one or both of the third cytoplasmic loop domain or the C-terminal intracellular domain of NPY5 replaced with the corresponding region(s) of another NPY receptor, preferably an NPY1 receptor.

    摘要翻译： 提供了新的嵌合G蛋白偶联受体作为分离的多肽，含有这种嵌合受体的膜制剂，编码这种嵌合受体的核酸和表达这种受体的细胞。 嵌合受体是NPY5受体，其中NPY5的第三细胞质环结构域或C末端胞内结构域中的大多数或全部都被另一个NPY受体，优选NPY1受体的相应区域取代。