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    Pyrimidine and Quinoline Potentiators of Metabotropic Glutamate Receptors
    86.
    发明申请
    Pyrimidine and Quinoline Potentiators of Metabotropic Glutamate Receptors 审中-公开
    代谢型谷氨酸受体的嘧啶和喹啉电位

    公开(公告)号：US20070287716A1

    公开(公告)日：2007-12-13

    申请号：US11665422

    申请日：2005-10-24

    申请人： Essa Hu ,  Jean-Michel Vernier ,  Peter Chua ,  John Hutchinson ,  Nicholas Cosford

    发明人： Essa Hu ,  Jean-Michel Vernier ,  Peter Chua ,  John Hutchinson ,  Nicholas Cosford

    IPC分类号： A61K31/47 ,  A61P25/00 ,  C07D215/12 ,  C07D239/28

    CPC分类号： C07D239/26 ,  C07D215/06

    摘要： The present invention is directed to compounds which are potentiators of metabotropic glutamate receptors, including the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.

    摘要翻译： 本发明涉及作为代谢型谷氨酸受体的增强剂（包括mGluR2受体）的化合物，其可用于治疗或预防与谷氨酸能力障碍相关的神经和精神病学障碍以及其中涉及代谢型谷氨酸受体的疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及代谢型谷氨酸受体的疾病中的用途。

    Substituted pyridines useful as modulators of acetylcholine receptors
    87.
    发明授权
    Substituted pyridines useful as modulators of acetylcholine receptors 失效
    取代的吡啶可用作乙酰胆碱受体的调节剂

    公开(公告)号：US06194581B1

    公开(公告)日：2001-02-27

    申请号：US09218214

    申请日：1998-12-22

    申请人： Nicholas D. Cosford ,  Jean-Michel Vernier

    发明人： Nicholas D. Cosford ,  Jean-Michel Vernier

    IPC分类号： A61K314427

    CPC分类号： C07D213/82 ,  C07D213/38 ,  C07D213/48 ,  C07D401/06 ,  C07F7/0814

    摘要： In accordance with the present invention, there is provided a class of pyridine compounds which are modulators of acetylcholine receptors. The compounds of the invention displace acetylcholine receptor ligands from their binding sites. Invention compounds may act as agonists, partial agonists, antagonists or allosteric modulators of acetylcholine receptors, and are useful for a variety of therapeutic applications, such as the treatment of Alzheimer's disease and other disorders involving memory loss and/or dementia (including AIDS dementia); disorders of attention and focus (such as attention deficit disorder); disorders of extrapyramidal motor function such as Parkinson's disease, Huntington's disease, Gilles de la Tourette syndrome and tardive dyskinesia; mood and emotional disorders such as depression, panic, anxiety and psychosis; substance abuse including withdrawal syndromes and substitution therapy; neuroendocrine disorders and dysregulation of food intake, including bulimia and anorexia; disorders of nociception and control of pain; autonomic disorders including dysfunction of gastrointestinal motility and function such as inflammatory bowel disease, irritable bowel syndrome, diarrhea, constipation, gastric acid secretion and ulcers; pheochromocytoma; cardiovascular dysfunction including hypertension and cardia arrhythmias, comedication in surgical procedures, and the like.

    摘要翻译： 根据本发明，提供了一类作为乙酰胆碱受体调节剂的吡啶化合物。 本发明的化合物从其结合位点取代乙酰胆碱受体配体。 本发明化合物可用作乙酰胆碱受体的激动剂，部分激动剂，拮抗剂或变构调节剂，并且可用于各种治疗应用，例如治疗阿尔茨海默氏病和涉及记忆丧失和/或痴呆的其它病症（包括AIDS痴呆） ; 注意力集中障碍（如注意力缺陷障碍）; 锥体外系运动功能紊乱，如帕金森病，亨廷顿疾病，吉列斯·杜列特综合征和迟发性运动障碍; 情绪和情绪障碍如抑郁，恐慌，焦虑和精神病; 药物滥用，包括戒断综合征和替代治疗; 神经内分泌障碍和食物摄入异常，包括贪食症和厌食症; 伤害感受障碍和疼痛控制; 自主神经障碍包括胃肠蠕动功能障碍和功能障碍，如炎性肠病，肠易激综合征，腹泻，便秘，胃酸分泌和溃疡; 嗜铬细胞瘤 心血管功能障碍，包括高血压和贲门节律不正，外科手术中的喜剧等。