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118 条记录 (耗时 0.047 秒)

    High affinity small molecule C5a receptor modulators
    13.
    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。

    Melanin concentrating hormone receptor ligands
    14.
    发明授权
    Melanin concentrating hormone receptor ligands 失效
    黑色素浓缩激素受体配体

    公开(公告)号：US07323478B2

    公开(公告)日：2008-01-29

    申请号：US10820344

    申请日：2004-04-08

    申请人： Rajagopal Bakthavatchalam ,  Andrew Thurkauf ,  Alan Hutchison

    发明人： Rajagopal Bakthavatchalam ,  Andrew Thurkauf ,  Alan Hutchison

    IPC分类号： A61K31/445

    CPC分类号： C07D295/096

    摘要： Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof wherein Q, X, Y, Z, and R1 R9, and R12-R19 are defined herein. These compounds are selective modulators of MCH 1 receptors that are, therefore, useful in the treatment of a variety of metabolic, feeding, and sexual disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also disclosed.

    摘要翻译： 公开了下式的化合物及其药学上可接受的盐，其中Q，X，Y，Z和R 1 R 9和R 12， 本文定义了本文所述的方法。 这些化合物是MCH 1受体的选择性调节剂，因此可用于治疗各种代谢，喂养和性功能障碍。 还公开了治疗这种病症以及包装的药物组合物的方法。

    Aryl fused 2,4-disubstituted pyridines: NK3 receptor ligands
    16.
    发明申请
    Aryl fused 2,4-disubstituted pyridines: NK3 receptor ligands 审中-公开

    公开(公告)号：US20060142324A1

    公开(公告)日：2006-06-29

    申请号：US11355439

    申请日：2006-02-15

    申请人： Jun Yuan ,  George Maynard ,  Alan Hutchison

    发明人： Jun Yuan ,  George Maynard ,  Alan Hutchison

    IPC分类号： A61K31/4745 ,  C07D471/02

    CPC分类号： C07D471/04 ,  C07D495/04

    摘要： Disclosed are compounds of formula (I) or pharmaceutically acceptable non-toxic salts or pharmaceutically acceptable solvates thereof wherein: (II) represents (a), (b), (c) or (d) and W, X, Y, A, B, C, D, E are variables as described herein. These compounds are highly selective agonists or antagonists at NK3 receptors or prodrugs thereof. The novel tachykinin NK-3 receptor antagonists contained in this invention have potential utility in the treatment of a broad array of disorders and diseases of the central nervous system (CNS) and periphery in mammals in which activation of NK-3 receptors is of importance.

    2,4-substituted quinoline derivatives
    20.
    发明授权
    2,4-substituted quinoline derivatives 失效
    2,4-取代喹啉衍生物

    公开(公告)号：US06559163B2

    公开(公告)日：2003-05-06

    申请号：US09931549

    申请日：2001-08-16

    申请人： Guolin Cai ,  Jun Yuan ,  Kevin Currie ,  Pamela Albaugh ,  Alan Hutchison

    发明人： Guolin Cai ,  Jun Yuan ,  Kevin Currie ,  Pamela Albaugh ,  Alan Hutchison

    IPC分类号： A61K314709

    CPC分类号： C07D231/12 ,  C07D215/52 ,  C07D233/56 ,  C07D249/08 ,  C07D401/06 ,  C07D401/14 ,  C07D409/04

    摘要： Disclosed are compounds of the formula or pharmaceutically acceptable salts thereof wherein: represents: and A, B, G, D, E, Ra, Rb, W, and Z are defined herein. These compounds are agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABAA receptors in tissue samples.

    摘要翻译： 公开了式或其药学上可接受的盐的化合物，其中：表示：并且A，B，G，D，E，Ra，Rb，W和Z在本文中定义。 这些化合物是GABAA脑受体的激动剂，拮抗剂或反向激动剂或GABAA脑受体的激动剂，拮抗剂或反向激动剂的前药，因此可用于诊断和治疗焦虑症，抑郁症，唐氏综合征，睡眠和癫痫发作，过量与 苯二氮卓类药物和增强记忆力。 还提供药物组合物，包括包装的药物组合物。 本发明的化合物也可用作组织样品中GABA A受体定位的探针。