Diazabenzo[de] anthracen-3-one compounds and methods for inhibiting PARP
    4.
    发明授权
    Diazabenzo[de] anthracen-3-one compounds and methods for inhibiting PARP 失效
    二氮杂苯并[de]蒽-3-酮化合物和抑制PARP的方法

    公开(公告)号:US08470825B2

    公开(公告)日:2013-06-25

    申请号:US13246169

    申请日:2011-09-27

    IPC分类号: A61K31/5025

    摘要: The present invention relates to diazabenzo[de]anthracen-3-one compounds which inhibit poly(ADP-ribose) polymerase (“PARP”), compositions containing these compounds and methods for using these PARP inhibitors to treat, prevent and/or ameliorate the effects of the conditions described herein.

    摘要翻译: 本发明涉及抑制聚(ADP-核糖)聚合酶(“PARP”)的二氮杂苯并[de]蒽-3-酮化合物,含有这些化合物的组合物和使用这些PARP抑制剂治疗,预防和/或改善 本文所述条件的效果。

    PARP INHIBITOR COMPOUNDS, COMPOSITIONS AND METHODS OF USE
    5.
    发明申请
    PARP INHIBITOR COMPOUNDS, COMPOSITIONS AND METHODS OF USE 有权
    PARP抑制剂化合物,组合物和使用方法

    公开(公告)号:US20130011365A1

    公开(公告)日:2013-01-10

    申请号:US13527158

    申请日:2012-06-19

    摘要: 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 radio sensitize 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.

    摘要翻译: 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的敏感性的应用。 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。

    Process for preparing water-soluble phosphonooxymethyl derivatives of alcohol and phenol
    6.
    发明授权
    Process for preparing water-soluble phosphonooxymethyl derivatives of alcohol and phenol 失效
    制备醇和苯酚的水溶性膦酰氧甲基衍生物的方法

    公开(公告)号:US07534776B2

    公开(公告)日:2009-05-19

    申请号:US11586576

    申请日:2006-10-26

    IPC分类号: A61K31/66

    摘要: A process for making water-soluble phosphonooxymethyl ethers of hindered alcohol and phenol containing pharmaceuticals, such as camptothecin, propofol, etoposide, Vitamin E and Cyclosporin A. In particular, the process for preparing water-soluble phosphonooxymethyl derivatives comprises the steps of: R—OH represents an alcohol- or phenol-containing drug, n represents an integer of 1 or 2, R1 is hydrogen, an alkali metal ion, or a pharmaceutically acceptable cation, and R2 is hydrogen, an alkali metal ion, or a pharmaceutically acceptable cation.

    摘要翻译: 一种制备受阻醇和含苯酚的药物,如喜树碱,异丙酚,依托泊苷,维生素E和环孢菌素A的水溶性膦酰氧甲基醚的方法。特别地,制备水溶性膦酰氧甲基衍生物的方法包括以下步骤:R- OH表示含醇或苯酚的药物,n表示1或2的整数,R1表示氢,碱金属离子或药学上可接受的阳离子,R2表示氢,碱金属离子或药学上可接受的阳离子 。

    Process for preparing water soluble phosphonooxymethyl derivatives of alcohol and phenol
    8.
    发明授权
    Process for preparing water soluble phosphonooxymethyl derivatives of alcohol and phenol 有权
    制备醇和苯酚的水溶性膦酰氧甲基衍生物的方法

    公开(公告)号:US07229978B2

    公开(公告)日:2007-06-12

    申请号:US10498013

    申请日:2002-12-20

    IPC分类号: A61K31/66

    摘要: A process for making water-soluble phosphonooxymethyl ethers of hindered alcohol and phenol containing pharmaceuticals, such as camptothecin, propofol, etoposide, Vitamin E and Cyclosporin A. In particular, the process for preparing water-soluble phosphonooxymethyl derivatives comprises the steps of Formula (i) and Formula (ii); R—OH represents an alcohol- or phenol-containing drug, n represents an integer of 1 or 2, R1 is hydrogen, an alkali metal ion, or a pharmaceutically acceptable cation, and R2 is hydrogen, an alkali metal ion, or a pharmaceutically acceptable cation

    摘要翻译: 一种制备受阻醇和含苯酚的药物,如喜树碱,异丙酚,依托泊苷,维生素E和环孢菌素A的水溶性膦酰氧基甲基醚的方法。特别地,制备水溶性膦酰氧基甲基衍生物的方法包括以下步骤:式 )和式(ii); R-OH表示含醇或苯酚的药物,n表示1或2的整数,R 1是氢,碱金属离子或药学上可接受的阳离子, 2是氢,碱金属离子或药学上可接受的阳离子

    PARP inhibitor compounds, compositions and methods of use
    9.
    发明授权
    PARP inhibitor compounds, compositions and methods of use 有权
    PARP抑制剂化合物,组合物和使用方法

    公开(公告)号:US08894989B2

    公开(公告)日:2014-11-25

    申请号:US13527158

    申请日:2012-06-19

    摘要: 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.

    摘要翻译: 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。

    PARP INHIBITOR COMPOUNDS, COMPOSITIONS AND METHODS OF USE
    10.
    发明申请
    PARP INHIBITOR COMPOUNDS, COMPOSITIONS AND METHODS OF USE 有权
    PARP抑制剂化合物,组合物和使用方法

    公开(公告)号:US20090098084A1

    公开(公告)日:2009-04-16

    申请号:US12244399

    申请日:2008-10-02

    摘要: 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.

    摘要翻译: 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。