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    New neurokinin antagonists for use as medicaments
    8.
    发明申请
    New neurokinin antagonists for use as medicaments 失效
    用作药物的新型神经激肽拮抗剂

    公开(公告)号：US20070021406A1

    公开(公告)日：2007-01-25

    申请号：US11042752

    申请日：2005-01-24

    申请人： Jeffrey Albert ,  Peter Bernstein ,  Cyrus Ohnmacht ,  Keith Russell ,  Ashokkumar Shenvi

    发明人： Jeffrey Albert ,  Peter Bernstein ,  Cyrus Ohnmacht ,  Keith Russell ,  Ashokkumar Shenvi

    IPC分类号： A61K31/454 ,  C07D417/14

    CPC分类号： C07D413/06 ,  C07D273/00 ,  C07D413/12 ,  C07D413/14

    摘要： The present application relates to internally cyclized naphthamide compounds of the formula Ia (wherein R1a, R1b, R1c, R2, R3, R4, R5, R6, R7, R8, X1, X2, Y, Z, and n are as defined herein), which are useful, for example, for antagonizing the pharmacological actions of the neurokinin 1 (NK1) receptor. In particular, these compounds are useful in the treatment of diseases in which Substance P is involved such as, for example, major depressive disorder, severe anxiety disorders, stress disorders, major depressive disorder with anxiety, eating disorders, bipolar disorder, substance use disorder, schizophrenic disorders, psychotic disorders, movement disorders, cognitive disorders, depression and/or anxiety, mania or hypomania, aggressive behaviour, obesity, rheumatoid arthritis, Alzheimer's disease, cancer, oedema, allergic rhinitis, inflammation, pain, gastrointestinal-hypermotility, Huntington's disease, chronic obstructive pulmonary disorder (COPD), hypertension, migraine, bladder hypermotility, and urticaria.

    摘要翻译： 本申请涉及式Ia的其中环化的萘甲酰胺化合物（其中R 1a，R 1b，R 1c，R i，R 2， R 3，R 4，R 4，R 5，R 6，R 7， R 8，X 1，X 1，X 2，Y，Z和n如本文所定义），它们是有用的 例如，用于拮抗神经激肽1（NK 1 H 2）受体的药理作用。 特别地，这些化合物可用于治疗涉及物质P的疾病，例如重度抑郁障碍，严重焦虑障碍，应激障碍，焦虑症重度抑郁障碍，进食障碍，双相情感障碍，物质使用障碍 精神分裂症，精神病，运动障碍，认知障碍，抑郁和/或焦虑，躁狂或轻躁狂，侵略行为，肥胖症，类风湿性关节炎，阿尔茨海默氏病，癌症，水肿，过敏性鼻炎，炎症，疼痛，胃肠超运动，亨廷顿氏症 疾病，慢性阻塞性肺疾病（COPD），高血压，偏头痛，膀胱过度运动和荨麻疹。