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21. 发明授权

US09642847B2 Combinational compositions and methods for treatment of cancer 有权
公开(公告)号：US09642847B2
公开(公告)日：2017-05-09
申请号：US14807939
申请日：2015-07-24
申请人： ArQule, Inc. , Kyowa Hakko Kirin Co., Ltd.
发明人： Thomas C. K. Chan , Dennis S. France , Kenichi Ishii , Paolo Pucci
IPC分类号： A61K31/4745 , A61K31/517 , A61K45/06
CPC分类号： A61K31/4745 , A61K31/517 , A61K45/06 , A61K2300/00
摘要： The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or a pyrroloquinolinyl-pyrrolidine-2,5-dione compound in combination with a therapeutically effective amount of a second anti-proliferative agent.

22. 发明授权

US09447088B2 Compositions and methods for treatment of cancer 有权
标题翻译：用于治疗癌症的组合物和方法
公开(公告)号：US09447088B2
公开(公告)日：2016-09-20
申请号：US14215852
申请日：2014-03-17
申请人： ArQule, Inc.
发明人： Chiang J. Li , Mark A. Ashwell , Jason Hill , Magdi Moussa , Neru Munshi
IPC分类号： A61K31/4745 , C07D471/06 , C07D455/00 , C07D487/06 , C07F9/6558 , C07F9/6561 , A61K31/138 , A61K31/337 , A61K31/4535 , A61K31/513 , A61K31/5377 , A61K31/5517 , A61K31/664 , A61K31/675 , A61K31/704 , A61K31/7048 , A61K31/7068 , A61K38/08 , A61K38/12 , C07K2/00
CPC分类号： C07D471/06 , A61K31/138 , A61K31/337 , A61K31/4535 , A61K31/4745 , A61K31/513 , A61K31/5377 , A61K31/5517 , A61K31/664 , A61K31/675 , A61K31/683 , A61K31/704 , A61K31/7048 , A61K31/7068 , A61K38/08 , A61K38/12 , C07D455/00 , C07D487/06 , C07F9/65583 , C07F9/6561 , C07K2/00
摘要： The present invention relates to pyrroloquinolinyl-pyrrolidine-2,5-dione compounds in combination with chemotherapeutic agents. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or pyrroloquinolinyl-pyrrolidine-2,5-dione compound of the present invention and also administering a effective amount of a chemotherapeutic agent.
摘要翻译：本发明涉及吡咯并喹啉基 - 吡咯烷-2,5-二酮化合物与化学治疗剂的组合。本发明提供了治疗细胞增殖性疾病如癌症的方法，通过向有需要的受试者施用治疗有效量的吡咯并喹啉基 - 吡咯-2,5-二酮化合物或吡咯并喹啉基 - 吡咯烷-2,5-二酮，二酮化合物，并且还施用有效量的化学治疗剂。

23. 发明授权

US09180099B2 Pyrroloquinolinyl-pyrrolidine-2,5-dione formulations and methods for preparing and using same 有权
标题翻译：吡咯并喹啉基 - 吡咯烷-2,5-二酮制剂及其制备和使用方法
公开(公告)号：US09180099B2
公开(公告)日：2015-11-10
申请号：US13543007
申请日：2012-07-06
申请人： Hiroshi Yamakose , Takafumi Kato
发明人： Hiroshi Yamakose , Takafumi Kato
IPC分类号： A61K9/14 , A61K31/4745 , B29B9/12 , B32B5/16 , A61P35/00 , A61K9/20 , A61K31/4725
CPC分类号： A61K31/4745 , A61K9/2018 , A61K9/2054 , A61K9/2095 , A61K9/2866 , A61K31/4725 , Y10T428/2982
摘要： The present invention provides pyrroloquinolinyl-pyrrole-2,5-dione formulations and methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of the formulations containing pyrroloquinolinyl-pyrrole-2,5-dione compounds.
摘要翻译：本发明提供吡咯并喹啉基 - 吡咯-2,5-二酮制剂和治疗细胞增殖性疾病如癌症的方法，通过向有需要的受试者施用治疗有效量的含有吡咯并喹啉基 - 吡咯-2-酮的制剂， 5-二酮化合物。

24. 发明授权

US08871933B2 Purified pyrroloquinolinyl-pyrrolidine-2,5-dione compositions and methods for preparing and using same 有权
标题翻译：纯化的吡咯并喹啉基 - 吡咯烷-2,5-二酮组合物及其制备和使用方法
公开(公告)号：US08871933B2
公开(公告)日：2014-10-28
申请号：US14036672
申请日：2013-09-25
申请人： ArQule, Inc.
发明人： David P. Reed , Neil R. Barnes , John C. Kane , Christopher A. Lee , Jian-Xie Chen , Martin P. Redmon
IPC分类号： C07D471/06
CPC分类号： C07D471/04 , C07D471/06
摘要： The present invention relates to a form 1 and form 2 polymorph of (−)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione. The present invention also relates to (−)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione compounds having a chiral purity greater than 99%, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising these (−)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a composition comprising (−)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione having a chiral purity greater than 99% or a form 1 and form 2 polymorph of (−)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione.
摘要翻译：本发明涉及（ - ） - 反式-3-（5,6-二氢-4H-吡咯并[3,2,1-ij]喹啉-1-基）-4-（ -1H-吲哚-3-基）吡咯烷-2,5-二酮。本发明还涉及（ - ） - 反式-3-（5,6-二氢-4H-吡咯并[3,2,1-ij]喹啉-1-基）-4-（1H-吲哚-3-基）吡咯烷-2,5-二酮化合物及其制备方法。本发明还涉及包含这些（ - ） - 反式-3-（5,6-二氢-4H-吡咯并[3,2,1-ij]喹啉-1-基）-4-（1H-吲哚 -3-基）吡咯烷-2,5-二酮化合物。本发明提供了通过向有需要的受试者施用治疗有效量的包含（ - ） - 反式-3-（5,6-二氢-4H-吡喃并[ 吡咯并[3,2,1-ij]喹啉-1-基）-4-（1H-吲哚-3-基）吡咯烷-2,5-二酮，手性纯度大于99％，形式1和形式2 （ - ） - 反式-3-（5,6-二氢-4H-吡咯并[3,2,1-ij]喹啉-1-基）-4-（1H-吲哚-3-基）吡咯烷-2 ，5-二酮。

25. 发明授权

US08815854B2 Substituted imidazopyridinyl compounds 有权
标题翻译：取代的咪唑并吡啶基化合物
公开(公告)号：US08815854B2
公开(公告)日：2014-08-26
申请号：US13529493
申请日：2012-06-21
申请人： Mark A. Ashwell , Chris Brassard , Anton Filikov , Jason Hill , Steffi Koerner , Jean-Marc Lapierre , Yanbin Liu , Nivedita Namdev , Robert Nicewonger , Rocio Palma , Manish Tandon , David Vensel , Akihisa Matsuda , Shin Iimura , Yuko Yamamoto , Takeshi Isoyama
发明人： Mark A. Ashwell , Chris Brassard , Anton Filikov , Jason Hill , Steffi Koerner , Jean-Marc Lapierre , Yanbin Liu , Nivedita Namdev , Robert Nicewonger , Rocio Palma , Manish Tandon , David Vensel , Akihisa Matsuda , Shin Iimura , Yuko Yamamoto , Takeshi Isoyama
IPC分类号： A61K31/5377 , C07D413/14 , A61K31/437 , C07D471/04 , A61K31/506 , A61K31/497
CPC分类号： A61K31/437 , A61K31/497 , A61K31/506 , A61K31/5377 , C07D471/04
摘要： The present invention relates to substituted imidazopyridinyl compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted imidazopyridinyl compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
摘要翻译：本发明涉及取代的咪唑并吡啶基化合物和合成这些化合物的方法。本发明还涉及含有取代的咪唑并吡啶基化合物的药物组合物和通过将这些化合物和药物组合物施用于有需要的受试者来治疗细胞增殖性疾病如癌症的方法。

26. 发明授权

US08563567B2 Substituted heterocyclic compounds 有权
标题翻译：取代的杂环化合物
公开(公告)号：US08563567B2
公开(公告)日：2013-10-22
申请号：US12981095
申请日：2010-12-29
申请人： Syed M. Ali , Mark A. Ashwell , Yanbin Liu , Magdi Moussa , Jianqiang Wang , Hui Wu
发明人： Syed M. Ali , Mark A. Ashwell , Yanbin Liu , Magdi Moussa , Jianqiang Wang , Hui Wu
IPC分类号： A61K31/505 , A61K31/44 , C07D401/04 , C07D413/04 , C07D453/06
CPC分类号： C07D471/06
摘要： The present invention relates to substituted heterocyclic compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted heterocyclic compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
摘要翻译：本发明涉及取代的杂环化合物及其合成方法。本发明还涉及含有取代的杂环化合物的药物组合物和通过将这些化合物和药物组合物给予有需要的受试者来治疗细胞增殖性疾病如癌症的方法。

27. 发明授权

US08541407B2 Substituted benzo-pyrido-triazolo-diazepine compounds 有权
标题翻译：取代的苯并吡啶并三唑并二氮杂化合物
公开(公告)号：US08541407B2
公开(公告)日：2013-09-24
申请号：US13076695
申请日：2011-03-31
申请人： Syed M. Ali , Mark A. Ashwell , Eugene Kelleher , Steffi Koerner , Jean-Marc Lapierre , Jeffrey S. Link , Yanbin Liu , Magdi Moussa , Rocio Palma , Manish Tandon , David Vensel , Neil Westlund , Hui Wu , Rui-Yang Yang
发明人： Syed M. Ali , Mark A. Ashwell , Eugene Kelleher , Steffi Koerner , Jean-Marc Lapierre , Jeffrey S. Link , Yanbin Liu , Magdi Moussa , Rocio Palma , Manish Tandon , David Vensel , Neil Westlund , Hui Wu , Rui-Yang Yang
IPC分类号： C07D487/14
CPC分类号： C07D471/14 , C07D487/04
摘要： The present invention relates to substituted benzo-pyrido-triazolo-diazepine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted benzo-pyrido-triazolo-diazepine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof.
摘要翻译：本发明涉及取代的苯并吡啶并三唑并二氮杂化合物及其合成方法。本发明还涉及含有取代的苯并吡啶并三唑并二氮杂化合物的药物组合物和通过将这些化合物或药物组合物给予有需要的受试者来治疗细胞增殖性疾病如癌症的方法。

28. 发明授权

US08377927B2 Compositions and methods for treatment of cancer 有权
标题翻译：用于治疗癌症的组合物和方法
公开(公告)号：US08377927B2
公开(公告)日：2013-02-19
申请号：US12722394
申请日：2010-03-11
申请人： Chiang J. Li , Mark A. Ashwell , Jason Hill , Magdi M. Moussa , Neru Munshi
发明人： Chiang J. Li , Mark A. Ashwell , Jason Hill , Magdi M. Moussa , Neru Munshi
IPC分类号： A61P35/00 , A61K31/55 , C07D243/00
CPC分类号： C07D471/06 , A61K31/138 , A61K31/337 , A61K31/4535 , A61K31/4745 , A61K31/513 , A61K31/5377 , A61K31/5517 , A61K31/664 , A61K31/675 , A61K31/683 , A61K31/704 , A61K31/7048 , A61K31/7068 , A61K38/08 , A61K38/12 , C07D455/00 , C07D487/06 , C07F9/65583 , C07F9/6561 , C07K2/00
摘要： The present invention relates to pyrroloquinolinyl-pyrrole-2,5-dione compounds and pyrroloquinolinyl-pyrrolidine-2,5-dione compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising pyrroloquinolinyl-pyrrole-2,5-dione compounds and pyrroloquinolinyl-pyrrolidine-2,5-dione compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or pyrroloquinolinyl-pyrrolidine-2,5-dione compound of the present invention.
摘要翻译：本发明涉及吡咯并喹啉基 - 吡咯-2,5-二酮化合物和吡咯并喹啉基 - 吡咯烷-2,5-二酮化合物，以及这些化合物的制备方法。本发明还涉及包含吡咯并喹啉基 - 吡咯-2,5-二酮化合物和吡咯并喹啉基 - 吡咯烷-2,5-二酮化合物的药物组合物。本发明提供了治疗细胞增殖性疾病如癌症的方法，通过向有需要的受试者施用治疗有效量的吡咯并喹啉基 - 吡咯-2,5-二酮化合物或吡咯并喹啉基 - 吡咯烷-2,5-二酮，二酮化合物。

29. 发明授权

US08357694B2 Substituted 5,6-dihydro-6-phenylbenzo[F]isoquinolin-2-amine compounds 有权
标题翻译：取代的5,6-二氢-6-苯基苯并[F]异喹啉-2-胺化合物
公开(公告)号：US08357694B2
公开(公告)日：2013-01-22
申请号：US12649573
申请日：2009-12-30
申请人： Syed Ali , Mark Ashwell , Manish Tandon , Nivedita Namdev , Jean-Marc Lapierre , Neil Westlund , Rocio Palma , Rui-Yang Yang , Yanbin Liu , David Vensel , Sudharshan Eathiraj , Hui Wu , Eugene Kelleher
发明人： Syed Ali , Mark Ashwell , Manish Tandon , Nivedita Namdev , Jean-Marc Lapierre , Neil Westlund , Rocio Palma , Rui-Yang Yang , Yanbin Liu , David Vensel , Sudharshan Eathiraj , Hui Wu , Eugene Kelleher
IPC分类号： A01N43/54 , A61K31/505 , C07D239/00 , C07D239/70 , C07D487/00
CPC分类号： C07D239/70 , C07D221/10 , C07D401/12 , C07D403/12 , C07D409/12 , C07D471/10
摘要： The present invention relates to substituted 5,6-dihydro-6-phenylbenzo[f]isoquinolin-2-amine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted 5,6-dihydro-6-phenylbenzo[f]isoquinolin-2-amine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
摘要翻译：本发明涉及取代的5,6-二氢-6-苯基苯并[f]异喹啉-2-胺化合物及其合成方法。本发明还涉及含有取代的5,6-二氢-6-苯基苯并[f]异喹啉-2-胺化合物的药物组合物和通过将这些化合物和药物组合物给予受试者来治疗细胞增殖性疾病如癌症的方法需要。

30. 发明申请

US20120329793A1 Substituted Imidazopyridinyl Compounds 有权
标题翻译：取代的咪唑并吡啶基化合物
公开(公告)号：US20120329793A1
公开(公告)日：2012-12-27
申请号：US13529493
申请日：2012-06-21
申请人： Mark A. Ashwell , Chris Brassard , Anton Filikov , Jason Hill , Steffi Koerner , Jean-Marc Lapierre , Yanbin Liu , Nivedita Namdev , Robert Nicewonger , Rocio Palma , Manish Tandon , David Vensel , Akihisa Matsuda , Shin Iimura , Yuko Yamamoto , Takeshi Isoyama
发明人： Mark A. Ashwell , Chris Brassard , Anton Filikov , Jason Hill , Steffi Koerner , Jean-Marc Lapierre , Yanbin Liu , Nivedita Namdev , Robert Nicewonger , Rocio Palma , Manish Tandon , David Vensel , Akihisa Matsuda , Shin Iimura , Yuko Yamamoto , Takeshi Isoyama
IPC分类号： A61K31/5377 , A61P35/04 , A61K31/437 , C07D487/04 , A61K31/497 , A61K31/506
CPC分类号： A61K31/437 , A61K31/497 , A61K31/506 , A61K31/5377 , C07D471/04
摘要： The present invention relates to substituted imidazopyridinyl compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted imidazopyridinyl compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
摘要翻译：本发明涉及取代的咪唑并吡啶基化合物和合成这些化合物的方法。本发明还涉及含有取代的咪唑并吡啶基化合物的药物组合物和通过将这些化合物和药物组合物施用于有需要的受试者来治疗细胞增殖性疾病如癌症的方法。

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