15-O-Desmethylmacbecin Derivatives and Their Use in the Treatment of Cancer or B-Cell Malignancies
    8.
    发明申请
    15-O-Desmethylmacbecin Derivatives and Their Use in the Treatment of Cancer or B-Cell Malignancies 审中-公开
    15-O-去甲基衍生物及其在治疗癌症或B细胞恶性肿瘤中的应用

    公开(公告)号:US20090209507A1

    公开(公告)日:2009-08-20

    申请号:US12294253

    申请日:2007-03-30

    CPC分类号: C07D225/06

    摘要: The present invention relates to 15-O-desmethylmacbecin analogues according to the formula (IA) or (IB) herein, or a pharmaceutically acceptable salt thereof: wherein: R1 and R2 either both represent H or together they represent a bond (i.e. C4 to C5 is a double bond); and R3 represents H or CONH2 that are useful, e.g. in the treatment of cancer, B-cell malignancies, malaria, fungal infection, diseases of the central nervous system and neurodegenerative diseases, diseases dependent on angiogenesis, autoimmune diseases and/or as a prophylactic pretreatment for cancer. The present invention also provides methods for the production of these compounds and their use in medicine, in particular in the treatment and/or prophylaxis of cancer or B-cell malignancies.

    摘要翻译: 本发明涉及根据本文的式(IA)或(IB)的15-O-去甲基蒿酸类似物或其药学上可接受的盐:其中:R 1和R 2都表示H或一起表示一个键(即C 4至 C5是双键); 并且R 3表示可用的H或CONH 2,例如。 在治疗癌症,B细胞恶性肿瘤,疟疾,真菌感染,中枢神经系统疾病和神经变性疾病,依赖于血管生成的疾病,自身免疫疾病和/或作为癌症的预防性预处理。 本发明还提供了这些化合物的制备方法及其在医药中的用途,特别是用于治疗和/或预防癌症或B细胞恶性肿瘤的方法。