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1. 发明申请

US20120115873A1 DIAZABENZO[DE] ANTHRACEN-3-ONE COMPOUNDS AND METHODS FOR INHIBITING PARP 失效
标题翻译： DIAZABENZO [DE] ANTHRACEN-3-ONE化合物和抑制PARP的方法
公开(公告)号：US20120115873A1
公开(公告)日：2012-05-10
申请号：US13246169
申请日：2011-09-27
申请人： Weizheng XU , Greg Delahanty , Jie Zhang
发明人： Weizheng XU , Greg Delahanty , Jie Zhang
IPC分类号： A61K31/5025 , A61K35/02 , A61P35/00
CPC分类号： C07D491/06 , A61K31/495 , A61K31/5025
摘要： The present invention relates to diazabenzo[de]anthracen-3.-onei 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/或改善的方法本文所述条件的影响。

2. 发明申请

US20110092478A1 DIAZABENZO[DE] ANTHRACEN-3-ONE COMPOUNDS AND METHODS FOR INHIBITING PARP 有权
标题翻译： DIAZABENZO [DE] ANTHRACEN-3-ONE化合物和抑制PARP的方法
公开(公告)号：US20110092478A1
公开(公告)日：2011-04-21
申请号：US12910448
申请日：2010-10-22
申请人： Weizheng Xu , Greg Delahanty , Jie Zhang
发明人： Weizheng Xu , Greg Delahanty , Jie Zhang
IPC分类号： A61K31/5025 , A61K31/5377 , A61P29/00 , A61P9/00 , A61P25/28 , A61P17/00 , A61P31/18 , A61P27/02 , A61P25/00
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。

3. 发明授权

US07820668B2 Diazabenzo[de]anthracen-3-one compounds and methods for inhibiting PARP 有权
标题翻译：二氮杂苯并[de]蒽-3-酮化合物和抑制PARP的方法
公开(公告)号：US07820668B2
公开(公告)日：2010-10-26
申请号：US11814238
申请日：2006-01-19
申请人： Weizheng Xu , Greg Delahanty , Jie Zhang
发明人： Weizheng Xu , Greg Delahanty , Jie Zhang
IPC分类号： C07D487/06 , 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。

4. 发明授权

US08470825B2 Diazabenzo[de] anthracen-3-one compounds and methods for inhibiting PARP 失效
标题翻译：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
申请人： Weizheng Xu , Greg Delahanty , Jie Zhang
发明人： Weizheng Xu , Greg Delahanty , Jie Zhang
IPC分类号： 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。

5. 发明申请

US20130011365A1 PARP INHIBITOR COMPOUNDS, COMPOSITIONS AND METHODS OF USE 有权
标题翻译： 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
申请人： Weizheng XU , Greg Delahanty , Ling Wei , Jie Zhang
发明人： Weizheng XU , Greg Delahanty , Ling Wei , Jie Zhang
IPC分类号： A61K31/519 , A61K33/24 , A61K31/7008 , A61K38/21 , A61K31/7036 , A61K31/7048 , A61K31/664 , A61P35/00 , A61P35/02 , A61K38/14 , A61K31/704 , A61K38/20
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 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。

6. 发明授权

US07534776B2 Process for preparing water-soluble phosphonooxymethyl derivatives of alcohol and phenol 失效
标题翻译：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
申请人： George Bonneville , Greg Delahanty , Andrew J. Walz
发明人： George Bonneville , Greg Delahanty , Andrew J. Walz
IPC分类号： A61K31/66
CPC分类号： C07K7/645 , C07F9/091 , C07F9/65522 , C07F9/6561
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。

7. 发明授权

US07378441B2 Resistance-repellent retroviral protease inhibitors 失效
标题翻译：耐药性逆转录病毒蛋白酶抑制剂
公开(公告)号：US07378441B2
公开(公告)日：2008-05-27
申请号：US11124056
申请日：2005-05-09
申请人： Michael Eissenstat , Andrey Topin , Greg Delahanty , Gnana Ravi Rajendran
发明人： Michael Eissenstat , Andrey Topin , Greg Delahanty , Gnana Ravi Rajendran
IPC分类号： A01N43/08 , C07D493/00
CPC分类号： C07D493/04 , A61K31/343 , A61K31/353 , A61K31/416 , A61K31/665
摘要： Resistance-repellent and multidrug resistant retroviral protease inhibitors are provided. Pharmaceutical composition comprising such compounds, and methods of using such compounds to treat HIV infections in mammals, are also provided.
摘要翻译：提供抗驱虫和多药耐药的逆转录病毒蛋白酶抑制剂。还提供了包含这些化合物的药物组合物，以及使用这些化合物治疗哺乳动物HIV感染的方法。

8. 发明授权

US07229978B2 Process for preparing water soluble phosphonooxymethyl derivatives of alcohol and phenol 有权
标题翻译：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
申请人： George Bonneville , Greg Delahanty , Andrew J. Walz
发明人： George Bonneville , Greg Delahanty , Andrew J. Walz
IPC分类号： A61K31/66
CPC分类号： C07K7/645 , C07F9/091 , C07F9/65522 , C07F9/6561
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

9. 发明授权

US08894989B2 PARP inhibitor compounds, compositions and methods of use 有权
标题翻译： 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
申请人： Weizheng Xu , Greg Delahanty , Ling Wei , Jie Zhang
发明人： Weizheng Xu , Greg Delahanty , Ling Wei , Jie Zhang
IPC分类号： A61K45/00 , A01N43/58 , C07D491/00
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.
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。

10. 发明申请

US20090098084A1 PARP INHIBITOR COMPOUNDS, COMPOSITIONS AND METHODS OF USE 有权
标题翻译： 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
申请人： Weizheng Xu , Greg Delahanty , Ling Wei , Jie Zhang
发明人： Weizheng Xu , Greg Delahanty , Ling Wei , Jie Zhang
IPC分类号： A61K31/519 , C07D487/06 , A61P35/00 , A61K31/704 , A61K38/21 , A61K38/20 , A61K33/24 , A61K31/551
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.
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。

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