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118 条记录 (耗时 0.065 秒)

    4-Substituted quinoline derivatives
    76.
    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
    78.
    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。

    Certain fused pyrrolecarboxamides; a new class of GABA brain receptor
    79.
    发明授权
    Certain fused pyrrolecarboxamides; a new class of GABA brain receptor 失效
    某些融合的吡咯甲酰胺; 一类新的GABA脑受体

    公开(公告)号：US06353109B2

    公开(公告)日：2002-03-05

    申请号：US09088522

    申请日：1998-06-01

    申请人： Pamela Albaugh ,  Gang Liu ,  Alan Hutchison

    发明人： Pamela Albaugh ,  Gang Liu ,  Alan Hutchison

    IPC分类号： C07C23359

    CPC分类号： C07D401/12 ,  C07D209/42 ,  C07D409/12 ,  C07D471/04

    摘要： Disclosed are compounds of the formula or the pharmaceutically acceptable non-toxic salts thereof wherein: W represents substituted or unsubstituted aryl or heteroaryl; T is hydrogen, halogen, hydroxyl, amino or alkyl; X is hydrogen, hydroxy, or lower alkyl; m is 0, 1, or 2; n is 0, 1, or 2; and R3 and R4 represent substituted or unsubstituted organic residues. These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.

    摘要翻译： 公开了下式的化合物或其药学上可接受的无毒盐，其中：W表示取代或未取代的芳基或杂芳基; T是氢，卤素，羟基，氨基或烷基; X是氢，羟基或低级烷基; m是0 ，1或2; n为0,1或2; R 3和R 4代表取代或未取代的有机残基。这些化合物是GABAa脑受体的高选择性激动剂，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。 这些化合物可用于诊断和治疗焦虑，睡眠和癫痫发作，用苯二氮卓类药物过量并用于记忆增强。