Harmine derivatives, intermediates used in their preparations, preparation processes and use therefo
    1.
    发明申请
    Harmine derivatives, intermediates used in their preparations, preparation processes and use therefo 有权
    哈曼衍生物,其制备中使用的中间体,制备过程和用途

    公开(公告)号:US20090227619A1

    公开(公告)日:2009-09-10

    申请号:US10559824

    申请日:2004-06-02

    CPC分类号: C07D471/04

    摘要: This invention relates to compounds of general formula (I), wherein R1, R2, R3, R4 and R5 are as defined in the specification; intermediates used in their preparation, preparation processes and use thereof. The present invention produces new harmine derivatives with enhanced antitumour activity and lower nervous system toxicity by structurally modification of the parent structure of β-carboline of harmines at position 1, 2, 3, 7 and 9. The compounds of the present invention can be prepared easily with high yield. They can be used in manufacture of a variety of antitumour medicines and medicines used in treatment of tumour diseases in combination of light or radiation therapy.

    摘要翻译: 本发明涉及通式(I)的化合物,其中R1,R2,R3,R4和R5如说明书中所定义; 用于其制备的中间体,制备方法及其用途。 本发明通过结构上改变位置1,2,3,7和9处的危害性的β-咔啉的母体结构,产生具有增强的抗肿瘤活性和降低神经系统毒性的新型有害化合物。本发明化合物可以制备 容易产量高。 它们可用于制造各种抗肿瘤药物和药物,用于治疗轻度或放射治疗的肿瘤疾病。

    Harmine derivatives, intermediates used in their preparations, preparation processes and use thereof
    2.
    发明授权
    Harmine derivatives, intermediates used in their preparations, preparation processes and use thereof 有权
    哈曼衍生物,其制备中使用的中间体,制备方法及其用途

    公开(公告)号:US08772311B2

    公开(公告)日:2014-07-08

    申请号:US10559824

    申请日:2004-06-02

    IPC分类号: A61K31/437 C07D487/04

    CPC分类号: C07D471/04

    摘要: This invention relates to compounds of general formula (I), wherein R1, R2, R3, R4 and R5 are as defined in the specification; intermediates used in their preparation, preparation processes and use thereof. The present invention produces new harmine derivatives with enhanced antitumor activity and lower nervous system toxicity by structurally modification of the parent structure of β-carboline of harmines at position 1, 2, 3, 7 and 9. The compounds of the present invention can be prepared easily with high yield. They can be used in manufacture of a variety of antitumor medicines and medicines used in treatment of tumor diseases in combination of light or radiation therapy.

    摘要翻译: 本发明涉及通式(I)的化合物,其中R1,R2,R3,R4和R5如说明书中所定义; 用于其制备的中间体,制备方法及其用途。 本发明通过结构上改变1,2,3,7和9位的胭脂红的母体结构,产生具有增强的抗肿瘤活性和降低神经系统毒性的新型有害化合物。本发明的化合物可以是 以高产量容易地制备。 它们可用于制造各种抗肿瘤药物和药物,用于治疗轻度或放射治疗的肿瘤疾病。