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31 条记录 (耗时 0.033 秒)

    4-aminoquinazoline derivatives and uses thereof
    21.
    发明授权
    4-aminoquinazoline derivatives and uses thereof 有权
    4-氨基喹唑啉衍生物及其用途

    公开(公告)号：US09034886B2

    公开(公告)日：2015-05-19

    申请号：US14124402

    申请日：2012-05-10

    申请人： Jianqi Li ,  Qingwei Zhang ,  Wangping Cai

    发明人： Jianqi Li ,  Qingwei Zhang ,  Wangping Cai

    IPC分类号： A01N43/54 ,  A61K31/517 ,  C07D401/00 ,  C07D239/94 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C07D409/12

    CPC分类号： C07D239/94 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C07D409/12

    摘要： The present invention provides a 4-aminoquinazoline derivative having the chemical structure of the following formula, and the use thereof. It is demonstrated by the pharmacological experiment that, the compound or a salt thereof according to the present invention not only has distinct inhibitory effect on histone deacetylases, but also has stronger differentiation induction and anti-proliferative activities for certain tumor cells. It can be used in the treatment of cancers and diseases related to cell differentiation and proliferation. Excellent efficacy is observed especially for leukemia and a solid tumor. As demonstrated by the animal test, the compound or a salt thereof according to the present invention is less toxic.

    摘要翻译： 本发明提供具有下式的化学结构的4-氨基喹唑啉衍生物及其用途。 通过药理实验证明，本发明的化合物或其盐不仅对组蛋白脱乙酰酶具有明显的抑制作用，而且对某些肿瘤细胞也具有更强的分化诱导和抗增殖活性。 它可用于治疗与细胞分化和增殖相关的癌症和疾病。 观察到特别是白血病和实体瘤的优异疗效。 如通过动物试验所证实的，根据本发明的化合物或其盐具有较小的毒性。

    BENZOTHIOPHENE ALKANOL PIPERAZINE DERIVATIVES AND THEIR USE AS ANTIDEPRESSANT
    29.
    发明申请
    BENZOTHIOPHENE ALKANOL PIPERAZINE DERIVATIVES AND THEIR USE AS ANTIDEPRESSANT 失效
    苯并噻唑烷醇衍生物及其用作抗生素

    公开(公告)号：US20110118263A1

    公开(公告)日：2011-05-19

    申请号：US13001998

    申请日：2009-06-30

    申请人： Jianqi Li ,  Kai Gao ,  Na Lv

    发明人： Jianqi Li ,  Kai Gao ,  Na Lv

    IPC分类号： A61K31/5377 ,  C07D409/06 ,  C07D409/14 ,  C07D413/14 ,  A61K31/497 ,  A61P25/24

    CPC分类号： C07D409/06 ,  C07D409/14

    摘要： The invention discloses benzothiophene alkanol piperazine derivatives and their use as antidepressants. The invention discloses the said benzothiophene alkanol piperazine derivative having triple inhibition effect on the reuptake of 5-HT, NA and DA. Compared with clinical used antidepressants so far having single target, e.g. desipramine and fluoxetine, and clinical used antidepressants so far having double targets, e.g venlafaxine and duloxetine, the said benzothiophene alkanol piperazine derivatives of the present invention may have a broader indication range and less toxic and side effects to nervous system. The benzothiophene alkanol piperazine derivatives are the compounds with the following formula or their pharmaceutically acceptable salts, wherein Ar1, R1-R4, X, Y, m and n have the same definition as defined in claim 1.

    摘要翻译： 本发明公开了苯并噻吩烷醇哌嗪衍生物及其作为抗抑郁药的用途。 本发明公开了对5-HT，NA和DA的再摄取具有三重抑制作用的所述苯并噻吩烷醇哌嗪衍生物。 与迄今为止具有单一目标的临床使用的抗抑郁药相比， 本发明的所述苯并噻吩烷醇哌嗪衍生物可能具有更广泛的适应范围和对神经系统的毒副作用较小的临床用途的抗抑郁药，目前为止具有双重目标，例如文拉法辛和度洛西汀。 苯并噻吩烷醇哌嗪衍生物是具有下式的化合物或其药学上可接受的盐，其中Ar1，R1-R4，X，Y，m和n具有与权利要求1中所定义的相同的定义。