FUSED QUINAZOLINE DERIVATIVES AND USES THEREOF
    1.
    发明公开
    FUSED QUINAZOLINE DERIVATIVES AND USES THEREOF 审中-公开
    KENENSIERTE CHINAZOLINDERIVATE UND DEREN VERWENDUNGEN

    公开(公告)号:EP2592083A1

    公开(公告)日:2013-05-15

    申请号:EP11782976.2

    申请日:2011-05-20

    CPC分类号: C07D487/04

    摘要: Fused quinazoline derivatives and uses thereof as protein tyrosine kinase inhibitors and aurora kinase inhibitors are disclosed. Said protein tyrosine kinase inhibitors and aurora kinase inhibitors can be used in treating cancers, leukaemia and the diseases relevant to differentiation and proliferation. Said protein tyrosine kinase and aurora kinase dual inhibitors are the compounds represented by the following general formula or salts thereof.

    摘要翻译: 公开了熔融喹唑啉衍生物及其作为蛋白质酪氨酸激酶抑制剂和极光激酶抑制剂的用途。 所述蛋白酪氨酸激酶抑制剂和极光激酶抑制剂可用于治疗癌症,白血病和与分化和增殖相关的疾病。 所述蛋白酪氨酸激酶和极光激酶双重抑制剂是由以下通式表示的化合物或其盐。

    BENZOTHIOPHENE ALKANOL PIPERAZINE DERIVATIVES AND THEIR USE AS ANTIDEPRESSANT
    3.
    发明公开

    公开(公告)号:EP2311828A1

    公开(公告)日:2011-04-20

    申请号:EP09771968.6

    申请日:2009-06-30

    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 Ar 1 , R 1 -R 4 , 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。 本发明公开了所述苯并噻吩烷醇哌嗪衍生物对5-HT,NA和DA的再摄取具有三重抑制作用。 与迄今为止具有单一靶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Ar 1,R 1 -R 4,X,Y,m和n具有与权利要求1中所定义的相同的定义。

    4-AMINOQUINAZOLINE DERIVATIVES AND USES THEREOF
    5.
    发明公开
    4-AMINOQUINAZOLINE DERIVATIVES AND USES THEREOF 审中-公开
    4-AMINOCHINAZOLIN-DERIVATE UND VERWENDUNGEN DAVON

    公开(公告)号:EP2708532A1

    公开(公告)日:2014-03-19

    申请号:EP12786071.6

    申请日:2012-05-10

    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。 如通过动物实验证明的,根据本发明的化合物或其盐具有较小的毒性。