Carbazole derivatives acting on 5-HT7 receptor

    公开(公告)号:US09663464B2

    公开(公告)日:2017-05-30

    申请号:US14629821

    申请日:2015-02-24

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

    Abstract: The present invention provides a carbazole derivative represented by Formula 1: wherein X is CH2 or C(O), Y is selected from NR1R2, piperidinyl groups in which two of the carbon atoms are substituted with R3 and R4, piperazinyl groups in which the nitrogen atom is substituted with R5, and morpholinyl groups, n is an integer from 2 to 5, R1 and R2, which may be identical or different, are each independently selected from C1-C6 alkyl, phenyl, and benzyl, with the proviso that R1 and R2 may be bonded together to form a ring, R3 and R4, which may be identical or different, are each independently selected from hydrogen, C1-C6 alkyl, phenyl, and benzyl, and R5 is selected from C1-C6 alkyl, C1-C4 alkylcarbonyl, phenyl substituted with C1-C4 alkyloxy, hydroxyphenyl, benzyl, and benzoisoxazol-3-yl; or a pharmaceutically acceptable salt thereof.

    Thienopyrimidinone derivatives as mGluR1 antagonists
    6.
    发明授权
    Thienopyrimidinone derivatives as mGluR1 antagonists 有权
    噻吩并嘧啶酮衍生物作为mGluR1拮抗剂

    公开(公告)号:US09260448B2

    公开(公告)日:2016-02-16

    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。

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