公开(公告)号：US20130345225A1

公开(公告)日：2013-12-26

申请号：US13914067

申请日：2013-06-10

申请人： Eisai Inc.

发明人： Weizheng XU ,  Greg Delahanty ,  jIE ZHANG

IPC分类号： C07D491/06 ,  A61K31/495 ,  A61K31/5025

CPC分类号： C07D491/06 ,  A61K31/495 ,  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。

公开(公告)号：US20150141429A1

公开(公告)日：2015-05-21

申请号：US14538447

申请日：2014-11-11

申请人： EISAI INC.

发明人： Weizheng XU ,  Greg Delahanty ,  Ling Wei ,  Jie Zhang

IPC分类号： A61K31/519 ,  A61K31/53

CPC分类号： A61K31/519 ,  A61K31/53 ,  C07D487/06 ,  C07D519/00

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.