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23 条记录 (耗时 0.037 秒)

    Di-aryl substituted triazole modulators of metabotropic glutamate receptor-5
    11.
    发明授权
    Di-aryl substituted triazole modulators of metabotropic glutamate receptor-5 失效
    代谢型谷氨酸受体-5的二芳基取代三唑调节剂

    公开(公告)号：US07268151B2

    公开(公告)日：2007-09-11

    申请号：US10552362

    申请日：2004-03-31

    申请人： Nicholas D. P. Cosford ,  Jeffrey R. Roppe ,  Lida R. Tehrani ,  Bowei Wang

    发明人： Nicholas D. P. Cosford ,  Jeffrey R. Roppe ,  Lida R. Tehrani ,  Bowei Wang

    IPC分类号： A61K31/4439 ,  C07D401/14

    CPC分类号： A61K31/41 ,  A61K31/4192 ,  C07D401/10 ,  C07D401/14

    摘要： Novel triazole compounds represented by Formula (1): (where A, A1, A2, A3, A4, A5, B, R11, W, X, Y and Z are as defined herein) in which the triazole is substituted directly, or by a bridge, with i) a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl and ii) another heteroaryl or aryl ring, with at least one of the rings being further substituted with another ring, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, panic, and bipolar disorder, as well as in the treatment of pain, Parkinson's disease, cognitive dysfunction, epilepsy, circadian rhythm disorders, drug addiction, drug abuse, drug withdrawal, obesity and other diseases

    摘要翻译： 由式（1）表示的新型三唑化合物：其中A，A 1，A 2，A 3，A 4， A，B，R 11，W，X，Y和Z如本文所定义），其中三唑直接被取代，或通过桥 ，其中i）包含与杂芳基的连接点相邻的N的杂芳基部分和ii）另外的杂芳基或芳基环，其中至少一个环进一步被另一个环取代，是用于治疗精神病学的mGluR5调节剂 以及情绪障碍，例如精神分裂症，焦虑症，抑郁症，恐慌症和双相性精神障碍，以及治疗疼痛，帕金森病，认知功能障碍，癫痫，昼夜节律紊乱，药物成瘾，药物滥用，药物戒断 ，肥胖等疾病

    Substituted pyridine compounds useful as modulators of acetylcholine receptors
    12.
    发明授权
    Substituted pyridine compounds useful as modulators of acetylcholine receptors 失效
    可用作乙酰胆碱受体调节剂的取代吡啶化合物

    公开(公告)号：US06632823B1

    公开(公告)日：2003-10-14

    申请号：US08996308

    申请日：1997-12-22

    申请人： Jean-Michel Vernier ,  Nicholas D. P. Cosford ,  Ian A. McDonald

    发明人： Jean-Michel Vernier ,  Nicholas D. P. Cosford ,  Ian A. McDonald

    IPC分类号： C07D21300

    CPC分类号： C07D213/70 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/46 ,  C07D213/32 ,  C07D213/52 ,  C07D401/12 ,  C07D451/02 ,  C07D451/04 ,  C07D471/08

    摘要： In accordance with the present invention, a novel class of substituted pyridine compounds (optionally containing ether, ester, amide, ketone or thioether substitutions) that promote the release of ligands involved in neurotransmission have been discovered. In a particular aspect compounds of the present invention are capable of modulating acetylcholine receptors. The compounds of the present invention are capable of modulating acetylcholine receptors. Invention compounds may act as agonists, partial agonists, antagonists or allosteric modulators of acetylcholine receptors. Therapeutic indications for compounds with activity at acetylcholine receptors include diseases of the central nervous system such as Alzheimer's disease and other diseases involving memory loss and/or dementia (including AIDS dementia); cognitive dysfunction (including disorders of attention, focus and concentration), disorders of extrapyramidal motor function such as Parkinson's disease, progressive supramuscular palsy, Huntington's disease, Gilles de la Tourette syndrome and tardive dyskinesia; mood and emotional disorders such as depression, anxiety and psychosis; substance abuse including withdrawal symptoms and substitution therapy; neurocrine disorders and dysregulation of food intake, including bulimia and anorexia; disorders or 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 cardiac arrhythmias, as well as co-medication uses in surgical applications.

    摘要翻译： 已经发现，根据本发明，已经发现了促进参与神经传递的配体释放的新一类取代的吡啶化合物（任选地含有醚，酯，酰胺，酮或硫醚取代）。 在具体方面，本发明的化合物能够调节乙酰胆碱受体。 本发明的化合物能够调节乙酰胆碱受体。 本发明化合物可以充当乙酰胆碱受体的激动剂，部分激动剂，拮抗剂或变构调节剂。 具有乙酰胆碱受体活性的化合物的治疗适应症包括中枢神经系统的疾病如阿尔茨海默氏病和涉及记忆丧失和/或痴呆（包括AIDS痴呆）的其它疾病; 认知功能障碍（包括注意力集中和集中注意力障碍），帕特森氏病，锥体运动功能障碍，进行性肌肉麻痹，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，焦虑和精神病; 药物滥用，包括戒断症状和替代治疗; 神经分泌障碍和食物摄入异常，包括贪食症和厌食症; 疾病或疼痛的伤害和控制; 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，包括高血压和心律失常，以及在外科应用中的共同用药用途。

    BENZOISOTHIAZOLONES AS INHIBITORS OF PHOSPHOMANNOSE ISOMERASE
    18.
    发明申请
    BENZOISOTHIAZOLONES AS INHIBITORS OF PHOSPHOMANNOSE ISOMERASE 审中-公开
    苯并噻唑酮作为磷酸异辛酯的抑制剂

    公开(公告)号：US20110257233A1

    公开(公告)日：2011-10-20

    申请号：US13051910

    申请日：2011-03-18

    申请人： Nicholas D. P. Cosford ,  Hudson H. Freeze ,  Russell Dahl ,  Yalda Bravo ,  Vandana Sharma ,  Mie Ichikawa

    发明人： Nicholas D. P. Cosford ,  Hudson H. Freeze ,  Russell Dahl ,  Yalda Bravo ,  Vandana Sharma ,  Mie Ichikawa

    IPC分类号： A61K31/428 ,  A61P31/04 ,  A61P31/00 ,  A61P3/10 ,  A61P25/00 ,  A61P1/16 ,  A61P13/12 ,  C07D275/04 ,  A61P27/10

    CPC分类号： C07D275/04

    摘要： The disclosure provides new compounds and compositions thereof, and methods for treating or ameliorating a disorder relating to CDG-Ia. In particular, the disclosure provides benzoisothiazolone inhibitors of PMI, which have been synthesized and their ability to drive glycosylation has been demonstrated. The disclosure provides two synthetic routes for these compounds, including a new copper-catalyzed N-arylation reaction amenable to parallel derivitization. The disclosed compounds represent potent inhibitors of PMI, and their dose-dependent efficacy in cell-based models of glycosylation have been demonstrated. In addition, the disclosed compounds are selective over PMM and therefore, are useful in treating or ameliorating a disorder relating to CDG-Ia.

    摘要翻译： 本公开提供了新的化合物及其组合物，以及用于治疗或改善与CDG-1a有关的病症的方法。 特别地，本发明提供了已经合成的PMI的苯并异噻唑酮抑制剂及其驱动糖基化的能力。 本公开为这些化合物提供了两条合成途径，包括适于平行衍生的新的铜催化的N-芳基化反应。 所公开的化合物代表有效的PMI抑制剂，并且已经证明了它们在基于细胞的糖基化模型中的剂量依赖性功效。 此外，所公开的化合物对PMM是选择性的，因此可用于治疗或改善与CDG-1a相关的病症。