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    • 7. 发明授权
    • PARP inhibitor compounds, compositions and methods of use
    • PARP抑制剂化合物,组合物和使用方法
    • US08236802B2
    • 2012-08-07
    • US12244399
    • 2008-10-02
    • Weizheng XuGreg DelahantyLing WeiJie Zhang
    • Weizheng XuGreg DelahantyLing WeiJie Zhang
    • A01N43/58A61K31/50C07D491/00
    • A61K31/519A61K31/53C07D487/06C07D519/00
    • The present invention relates to tetraaza phenalen-3-one compounds which inhibit poly (ADP-ribose) polymerase (PARP) and are useful in the chemosensitization of cancer therapeutics. The induction of peripheral neuropathy is a common side-effect of many of the conventional and newer chemotherapies. The present invention further provides means to reliably prevent or cure chemotherapy-induced neuropathy. The invention also relates to the use of the disclosed PARP inhibitor compounds in enhancing the efficacy of chemotherapeutic agents such as temozolomide. The invention also relates to the use of the disclosed PARP inhibitor compounds to radiosensitize tumor cells to ionizing radiation. The invention also relates to the use of the disclosed PARP inhibitor compounds for treatment of cancers with DNA repair defects.
    • 本发明涉及抑制聚(ADP-核糖)聚合酶(PARP)并可用于癌症治疗剂的化学敏化的四氮芥苯并三氮唑-3-酮化合物。 周围神经病变的诱导是许多常规和较新的化学疗法的常见副作用。 本发明还提供了可靠地预防或治愈化疗诱发的神经病变的方法。 本发明还涉及所公开的PARP抑制剂化合物在增强化疗剂如替莫唑胺的功效中的用途。 本发明还涉及所公开的PARP抑制剂化合物对肿瘤细胞对电离辐射进行放射增敏的用途。 本发明还涉及所公开的PARP抑制剂化合物用于治疗具有DNA修复缺陷的癌症的用途。