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57 条记录 (耗时 0.044 秒)

    1H-pyrrolo [3,2-b] pyridine-3-carboxylic acid amines as GABAA receptor ligands
    52.
    发明授权
    1H-pyrrolo [3,2-b] pyridine-3-carboxylic acid amines as GABAA receptor ligands 失效
    1H-吡咯并[3,2-b]吡啶-3-甲酸胺作为GABA A受体配体

    公开(公告)号：US06673811B1

    公开(公告)日：2004-01-06

    申请号：US10299199

    申请日：2002-11-19

    申请人： George D. Maynard ,  Manuka Ghosh ,  Christopher J. O'Donnell

    发明人： George D. Maynard ,  Manuka Ghosh ,  Christopher J. O'Donnell

    IPC分类号： A61K314965

    CPC分类号： C07D471/04

    摘要： Disclosed are 1H-Pyrrolo[3,2-b]pyridine-3-carboxylic acid amides that bind to the benzodiazepine site of GABAA receptors. Such compounds can be used to modulate ligand binding to GABAA receptors in vivo and in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) disorders in humans, domesticated companion animals, and livestock animals.

    摘要翻译： 公开了结合GABA A受体的苯并二氮杂位点的1H-吡咯并[3,2-b]吡啶-3-羧酸酰胺。 这些化合物可用于体内和体外调节配体与GABA A受体的结合，并且特别可用于治疗人类，驯养的伴侣动物和家畜中的各种中枢神经系统（CNS）紊乱。

    4-Substituted quinoline derivatives
    53.
    发明授权
    4-Substituted quinoline derivatives 失效
    4-取代的喹啉衍生物

    公开(公告)号：US06624175B2

    公开(公告)日：2003-09-23

    申请号：US10140693

    申请日：2002-05-07

    申请人： Jun Yuan ,  George D. Maynard ,  Alan Hutchison ,  Stanislaw Rachwal

    发明人： Jun Yuan ,  George D. Maynard ,  Alan Hutchison ,  Stanislaw Rachwal

    IPC分类号： A61K3147

    CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D413/04 ,  C07D487/04 ,  G01N33/9426 ,  G01N2333/70571

    摘要： Disclosed are compounds of the Formula where R1, R2, R3, R4, X, Y1, and Y2 are defined herein. These compounds bind with high affinity to NK-3 receptors and/or GABAA receptors. Also provided are pharmaceutical compositions comprising these compounds, and methods of treating patients suffering from various central nervous system and peripheral diseases or disorders with these pharmaceutical compositions. This invention also relates to the use of such compounds in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. The compounds of this invention are also useful as probes for the localization of NK-3 receptors and GABAA receptors.

    摘要翻译： 公开了本文定义的化学式R 1，R 2，R 3，R 4，X，Y 1和Y 2的化合物。 这些化合物以高亲和力结合NK-3受体和/或GABA A受体。 还提供了包含这些化合物的药物组合物，以及用这些药物组合物治疗患有各种中枢神经系统和外周疾病或病症的患者的方法。 本发明还涉及这样的化合物与一种或多种其它CNS剂组合用于增强其它CNS剂的作用的用途。 本发明的化合物也可用作NK-3受体和GABA A受体定位的探针。

    2-Aminoquinolinecarboxamides: neurokinin receptor ligands
    54.
    发明授权
    2-Aminoquinolinecarboxamides: neurokinin receptor ligands 失效
    2-氨基喹啉甲酰胺：神经激肽受体配体

    公开(公告)号：US06369053B1

    公开(公告)日：2002-04-09

    申请号：US09560160

    申请日：2000-04-28

    申请人： Jun Yuan ,  George D. Maynard ,  Alan Hutchison

    发明人： Jun Yuan ,  George D. Maynard ,  Alan Hutchison

    IPC分类号： C07D21550

    CPC分类号： A61K31/47 ,  C07D215/50 ,  C07D401/04 ,  C07D453/06 ,  C07D491/10 ,  Y10S206/828

    摘要： Disclosed are compounds of the formula: or pharmaceutically acceptable salts or pharmaceutically acceptable solvates thereof, wherein R1, R2, R3, X, Q1 and Q2 are defined herein, which compounds are ligands for neurokinin receptors, in particular NK-3 receptors, and are therefor useful in the treatment of a wide range of diseases or disorders including, but not limited to depression, anxiety, psychosis, obesity, pain, Parkinson's disease, Alzheimer's disease, neurodegenerative diseases, movement disorders, respiratory diseases, inflammatory diseases, neuropathy, immune disorders, migraine, biliary disfunction, and dermatitis.

    摘要翻译： 公开了下式的化合物或其药学上可接受的盐或药学上可接受的溶剂化物，其中R1，R2，R3，X，Q1和Q2如本文所定义，哪些化合物是神经激肽受体，特别是NK-3受体的配体， 用于治疗广泛的疾病或病症，包括但不限于抑郁症，焦虑症，精神病，肥胖症，疼痛，帕金森病，阿尔茨海默病，神经变性疾病，运动​​障碍，呼吸系统疾病，炎性疾病，神经病，免疫 疾病，偏头痛，胆汁功能不全和皮炎。

    Aminoalkyl substituted 9H-phridino[2,3-b] indole and 9H-pyrimidino[4,5-b] indole derivatives
    55.
    发明授权
    Aminoalkyl substituted 9H-phridino[2,3-b] indole and 9H-pyrimidino[4,5-b] indole derivatives 失效
    氨基烷基取代的9H-嘧啶并[2,3-b]吲哚和9H-嘧啶并[4,5-b]吲哚衍生物

    公开(公告)号：US06362186B1

    公开(公告)日：2002-03-26

    申请号：US09707387

    申请日：2000-11-06

    申请人： Raymond F. Horvath ,  James W. Darrow ,  George D. Maynard

    发明人： Raymond F. Horvath ,  James W. Darrow ,  George D. Maynard

    IPC分类号： C07D23970

    CPC分类号： C07D471/04 ,  C07D487/04

    摘要： Disclosed are compounds of the formula: wherein Ar, R1, W and X are substituents as defined herein, which compounds are (1) antagonists at CRF1 receptors and are, therefore, useful in the diagnosis and treatment of stress related disorders such as post traumatic stress disorder (PTSD) as well as depression, headache and anxiety; and (2) are neuropeptide Y1, receptor antagonists, and are therefore useful in the treatment of a variety of clinical conditions which are characterized by the presence of an excess of neuropeptide Y.

    摘要翻译： 公开了下式的化合物：其中Ar，R 1，W和X是如本文所定义的取代基，该化合物是（1）CRF1受体的拮抗剂，因此可用于诊断和治疗应激相关疾病如创伤后 压力障碍（PTSD）以及抑郁，头痛和焦虑; 和（2）是神经肽Y1，受体拮抗剂，因此可用于治疗以过量神经肽Y的存在为特征的各种临床病症。