THIENOPYRIMIDINONE DERIVATIVES AS mGluR1 ANTAGONISTS
    5.
    发明申请
    THIENOPYRIMIDINONE DERIVATIVES AS mGluR1 ANTAGONISTS 有权
    三硝基嘧啶衍生物作为mGluR1拮抗剂

    公开(公告)号:US20140228565A1

    公开(公告)日:2014-08-14

    申请号:US14038324

    申请日:2013-09-26

    CPC classification number: C07D495/04 A61K31/519

    Abstract: Disclosed are thienopyrimidinone derivatives as antagonists that act on metabotropic glutamate receptor subtype 1. The thienopyrimidinone derivatives show pharmacological activity against metabotropic glutamate receptor-related diseases, including pain, such as neuropathic pain and migraine, psychiatric diseases, such as anxiety disorder and schizophrenia, urinary incontinence, and neurodegenerative diseases, such as Parkinson's disease and Alzheimer's disease. Also disclosed are methods for preparing the thienopyrimidinone derivatives, and pharmaceutical compositions containing the thienopyrimidinone derivatives as active ingredients.

    Abstract translation: 公开了作为代谢型谷氨酸受体亚型1的拮抗剂的噻吩并嘧啶酮衍生物。噻吩并嘧啶酮衍生物显示针对代谢型谷氨酸受体相关疾病的药理学活性,包括疼痛,如神经性疼痛和偏头痛,精神疾病如焦虑障碍和精神分裂症,尿 失禁和神经变性疾病,如帕金森病和阿尔茨海默病。 还公开了制备噻吩并嘧啶酮衍生物的方法和含有噻吩并嘧啶酮衍生物作为活性成分的药物组合物。

    CARBAZOLE DERIVATIVES ACTING ON 5-HT7 RECEPTOR
    8.
    发明申请
    CARBAZOLE DERIVATIVES ACTING ON 5-HT7 RECEPTOR 有权
    在5-HT7受体上起作用的卡博唑衍生物

    公开(公告)号:US20160244408A1

    公开(公告)日:2016-08-25

    申请号:US14629821

    申请日:2015-02-24

    CPC classification number: C07D209/86 C07D401/06 C07D403/06 C07D413/06

    Abstract: Disclosed are carbazole derivatives and pharmaceutically acceptable salts thereof that act on the 5-HT7 receptor. The carbazole derivatives and the pharmaceutically acceptable salts thereof have high binding affinities for the 5-HT7 serotonin receptor and antagonistic activities against the 5-HT7 serotonin receptor. Further disclosed are pharmaceutical compositions including the compounds as active ingredients. The pharmaceutical compositions are useful as therapeutic and prophylactic agents for central nervous system diseases where antagonistic activities against 5-HT7 are required, such as depression, migraine, anxiety, pain, inflammatory pain, neuropathic pain, body temperature dysregulation, circadian rhythm dysregulation, sleep disturbance, and smooth muscle-related diseases.

    Abstract translation: 公开了作用于5-HT 7受体的咔唑衍生物及其药学上可接受的盐。 咔唑衍生物及其药学上可接受的盐对5-HT7血清素受体具有高结合亲和力,对5-HT7血清素受体具有拮抗活性。 进一步公开了包含作为活性成分的化合物的药物组合物。 药物组合物可用作中枢神经系统疾病的治疗和预防剂,其中需要针对5-HT7的拮抗活性,例如抑郁症,偏头痛,焦虑症,疼痛,炎性疼痛,神经性疼痛,体温调节异常,昼夜节律紊乱,睡眠 干扰和平滑肌相关疾病。

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