NOVEL SUBSTITUTED-1, 1-DIOXO-BENZO[1,2,4]THIADIAZIN-3ONES, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME
    1.
    发明申请
    NOVEL SUBSTITUTED-1, 1-DIOXO-BENZO[1,2,4]THIADIAZIN-3ONES, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME 审中-公开
    新的取代的1,1-二氧代苯并[1,2,4]噻二嗪-3-酮,其制备方法和含有其的药物组合物

    公开(公告)号:US20100035866A1

    公开(公告)日:2010-02-11

    申请号:US12293965

    申请日:2006-03-28

    CPC分类号: C07D285/24

    摘要: The present invention relates to compounds of substituted-1,1-dioxo-benzo[1,2,4]thiadiazin-3-ones acting as a 5HT6 receptor antagonist, a preparation method thereof, and a pharmaceutical composition containing the same for treatment of the central nervous system disorders. The compounds of substituted-1,1-dioxo-benzo[1,2,4]thiadiazin-3-ones according to the present invention have excellent binding affinity for the 5HT6 receptor and excellent selectivity for the 5HT6 receptor over other receptors. Also, the compounds reverse a disruption of PPI by apomorphine and don't show rotatod deficit in mice. Therefore the compounds according to the present invention may be valuably used for treatment of a 5HT6 receptor relating disorders.

    摘要翻译: 本发明涉及作为5HT6受体拮抗剂的取代-1,1-二氧代 - 苯并[1,2,4]噻二嗪-3-酮的化合物,其制备方法和含有该化合物的药物组合物,其用于治疗 中枢神经系统疾病。 根据本发明的取代的-1,1-二氧代 - 苯并[1,2,4]噻二嗪-3-酮的化合物对5HT6受体具有优异的结合亲和力,对其它受体的5HT6受体的选择性优异。 此外,化合物反转了阿朴吗啡对PPI的破坏,并且在小鼠中不显示旋转异位缺陷。 因此,根据本发明的化合物可以有价值地用于治疗5HT6受体相关疾病。