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1. 发明申请

WO2013162714A1 HIGHLY PURE PYRROLOQUINOLINYL-PYRROLE-2,5-DIONE AND PYRROLOQUINOLINYL-PYRROLIDINE-2,5-DIONE AND METHODS OF PREPARING SAME 审中-公开
标题翻译：高纯度吡咯烷醇溶液 - 吡咯烷-2,5-二酮和对羟基吡啶-2-基吡咯烷-2,5-二酮及其制备方法
公开(公告)号：WO2013162714A1
公开(公告)日：2013-10-31
申请号：PCT/US2013/029572
申请日：2013-03-07
申请人： ARQULE, INC.
发明人： OOYAMA, Jo , NAKAMURA, Yoshitaka
IPC分类号： A61K31/473 , A61P35/00
CPC分类号： C07D471/06
摘要： The present invention relates to highly-pure pyrroloquinolinyl-pyrrole-2,5-dione and pyrroloquinolinyl-pyrrolidine-2,5-dione, for example, 3-(5,6-dihydro-4H-pyrrolo[3,2,l-ij]quinolin-l- yl)-4-(lH-indol-3-yl)-lH-pyrrole-2,5-dione, 3-(5,6-dihydro-4H-pyrrolo[3,2,l-ij]quinolin-l-yl)-4-(lH- indol-3-yl)pyrrolidine-2,5-dione, and pharmaceutically acceptable salts, solvates, and diastereomers thereof. The present invention also relates to methods for preparing highly-pure pyrroloquinolinyl- pyrrole-2,5-dione and pyrroloquinolinyl-pyrrolidine-2,5-dione, for example, 3-(5,6-dihydro-4H- pyrrolo[3,2,l-ij]quinolin-l-yl)-4-(lH-indol-3-yl)-lH-pyrrole-2,5-dione, 3-(5,6-dihydro-4H- pyrrolo[3,2,l-ij]quinolin-l-yl)-4-(lH-indol-3-yl)pyrrolidine-2,5-dione, and pharmaceutically acceptable salts, solvates, and diastereomers thereof.
摘要翻译：本发明涉及高纯度的吡咯并喹啉基 - 吡咯-2,5-二酮和吡咯并喹啉基 - 吡咯烷-2,5-二酮，例如3-（5,6-二氢-4H-吡咯并[3,2,1- ij]喹啉-1-基）-4-（1H-吲哚-3-基）-1H-吡咯-2,5-二酮，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-2,5-二酮及其药学上可接受的盐，溶剂化物和非对映异构体。本发明还涉及制备高纯度的吡咯并喹啉基 - 吡咯-2,5-二酮和吡咯并喹啉基 - 吡咯烷-2,5-二酮的方法，例如3-（5,6-二氢-4H-吡咯并[ 1,2-ij]喹啉-1-基）-4-（1H-吲哚-3-基）-1H-吡咯-2,5-二酮，3-（5,6-二氢-4H-吡咯并[3,3- 1,2-ij]喹啉-1-基）-4-（1H-吲哚-3-基）吡咯烷-2,5-二酮及其药学上可接受的盐，溶剂化物和非对映异构体。

2. 发明申请

WO2013006761A2 PYRROLOQUINOLINYL-PYRROLIDINE-2,5-DIONE FORMULATIONS AND METHODS FOR PREPARING AND USING SAME 审中-公开
标题翻译：吡咯烷基吡啶-2,5-二酮配方及其制备和使用方法
公开(公告)号：WO2013006761A2
公开(公告)日：2013-01-10
申请号：PCT/US2012/045688
申请日：2012-07-06
申请人： ARQULE, INC. , YAMAKOSE, Hiroshi , KATO, Takafumi
发明人： YAMAKOSE, Hiroshi , KATO, Takafumi
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， 5-二酮化合物。

3. 发明申请

WO2012088491A3 PYRROLOQUINOLINYL-PYRROLIDINE-2,5-DIONE COMPOSITIONS AND METHODS FOR PREPARING AND USING SAME 审中-公开
标题翻译：吡咯烷基吲哚基吡咯烷-2,5-二酮组合物及其制备和使用方法
公开(公告)号：WO2012088491A3
公开(公告)日：2013-01-03
申请号：PCT/US2011067102
申请日：2011-12-23
申请人： ARQULE INC , ASHWELL MARK A , KIZER DARIN , MURAI TAKAHIRO , NAKAI DAISUKE , YASUKOCHI TAKANORI
发明人： ASHWELL MARK A , KIZER DARIN , MURAI TAKAHIRO , NAKAI DAISUKE , YASUKOCHI TAKANORI
IPC分类号： C07D471/06 , A61K31/407 , A61P35/00 , C07D403/14
CPC分类号： C07D403/14 , C07D471/06
摘要： The present invention relates to pyrroloquinolinyl-pyrrolidine-2,5-dione compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing pyrroloquinolinyl-pyrrolidine-2,5-dione 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：本发明涉及吡咯并喹啉基 - 吡咯烷-2,5-二酮化合物及其合成方法。本发明还涉及含有吡咯并喹啉基 - 吡咯烷-2,5-二酮化合物的药物组合物和通过将这些化合物或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。

4. 发明申请

WO2012177844A2 SUBSTITUTED IMIDAZOPYRIDINYL-AMINOPYRIDINE COMPOUNDS 审中-公开
标题翻译：取代的咪唑啉氨基亚氨基吡啶化合物
公开(公告)号：WO2012177844A2
公开(公告)日：2012-12-27
申请号：PCT/US2012/043501
申请日：2012-06-21
申请人： ARQULE, INC. , ASHWELL, Mark, A. , BRASSARD, Chris , FILIKOV, Anton , HILL, Jason , KOERNER, Steffi , LAPIERRE, Jean-Marc , LIU, Yanbin , NAMDEV, Nivedita , NICEWONGER, Robert , PALMA, Rocio , TANDON, Manish , VENSEL, David , MATSUDA, Akihisa , IIMURA, Shin , YOSHIDA, Kenichi , YAMAZAKI, Takanori , KITAMURA, Takahiro , ISOYAMA, Takeshi
发明人： ASHWELL, Mark, A. , BRASSARD, Chris , FILIKOV, Anton , HILL, Jason , KOERNER, Steffi , LAPIERRE, Jean-Marc , LIU, Yanbin , NAMDEV, Nivedita , NICEWONGER, Robert , PALMA, Rocio , TANDON, Manish , VENSEL, David , MATSUDA, Akihisa , IIMURA, Shin , YOSHIDA, Kenichi , YAMAZAKI, Takanori , KITAMURA, Takahiro , ISOYAMA, Takeshi
IPC分类号： C07D471/04 , C07D401/04 , C07D413/14 , A61K31/4745 , A61P35/00
CPC分类号： C07D471/04 , C07D451/02 , C07D491/08 , C07D498/08
摘要： The present invention relates to substituted imidazopyridinyl-aminopyridine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted imidazopyridinyl- aminopyridine 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 - 氨基吡啶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 - 氨基吡啶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。

5. 发明申请

WO2012088491A2 PYRROLOQUINOLINYL-PYRROLIDINE-2,5-DIONE COMPOSITIONS AND METHODS FOR PREPARING AND USING SAME 审中-公开
标题翻译：吡咯烷基吲哚基吡咯烷-2,5-二酮组合物及其制备和使用方法
公开(公告)号：WO2012088491A2
公开(公告)日：2012-06-28
申请号：PCT/US2011/067102
申请日：2011-12-23
申请人： ARQULE, INC. , ASHWELL, Mark, A. , KIZER, Darin , MURAI, Takahiro , NAKAI, Daisuke , YASUKOCHI, Takanori
发明人： ASHWELL, Mark, A. , KIZER, Darin , MURAI, Takahiro , NAKAI, Daisuke , YASUKOCHI, Takanori
IPC分类号： C07D471/06 , C07D403/14 , A61K31/407 , A61P35/00
CPC分类号： C07D403/14 , C07D471/06
摘要： The present invention relates to pyrroloquinolinyl-pyrrolidine-2,5-dione compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing pyrroloquinolinyl-pyrrolidine-2,5-dione 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：本发明涉及吡咯并喹啉基 - 吡咯烷-2,5-二酮化合物及其合成方法。本发明还涉及含有吡咯并喹啉基 - 吡咯烷-2,5-二酮化合物的药物组合物和通过将这些化合物或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。

6. 发明申请

WO2012061342A2 SUBSTITUTED BENZO-IMIDAZO-PYRIDO-DIAZEPINE COMPOUNDS 审中-公开
标题翻译：取代的苯并咪唑并吡啶 - 二氮杂化合物
公开(公告)号：WO2012061342A2
公开(公告)日：2012-05-10
申请号：PCT/US2011/058716
申请日：2011-11-01
申请人： ARQULE, INC. , ASHWELL, Mark, A. , EATHIRAJ, Sudharshan , FILIKOV, Anton , KOERNER, Steffi , LAPIERRE, Jean-Marc , LIU, Yanbin , PALMA, Rocio , VENSEL, David , IIMURA, Shin , SHIINA, Akiko , YOSHIDA, Kenichi , YAMAZAKI, Takanori , MATSUDA, Akihisa
发明人： ASHWELL, Mark, A. , EATHIRAJ, Sudharshan , FILIKOV, Anton , KOERNER, Steffi , LAPIERRE, Jean-Marc , LIU, Yanbin , PALMA, Rocio , VENSEL, David , IIMURA, Shin , SHIINA, Akiko , YOSHIDA, Kenichi , YAMAZAKI, Takanori , MATSUDA, Akihisa
IPC分类号： C07D471/14 , C07D487/14 , A61K31/5517 , A61K31/5513 , A61P35/00
CPC分类号： C07D471/14 , A61K31/551 , Y02A50/401 , Y02A50/409 , Y02A50/411
摘要： The present invention relates to substituted benzo-imidazo-pyrido-diazepine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted benzo-imidazo-pyrido-diazepine 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：本发明涉及取代的苯并咪唑并吡啶并二氮杂化合物和合成这些化合物的方法。本发明还涉及包含取代的苯并咪唑并吡啶并二氮杂化合物的药物组合物以及通过将这些化合物和药物组合物施用给有需要的受试者来治疗细胞增殖性病症如癌症的方法。

7. 发明申请

WO2012003421A9 COMBINATIONAL COMPOSITIONS AND METHODS FOR TREATMENT OF CANCER 审中-公开
标题翻译：联合组合物和治疗癌症的方法
公开(公告)号：WO2012003421A9
公开(公告)日：2012-04-12
申请号：PCT/US2011042744
申请日：2011-07-01
申请人： ARQULE INC , ABBADESSA GIOVANNI , FRANCE DENNIS S , CHEN CHANG-RUNG , CHAN THOMAS C K
发明人： ABBADESSA GIOVANNI , FRANCE DENNIS S , CHEN CHANG-RUNG , CHAN THOMAS C K
IPC分类号： A61K31/437 , A61K31/4375 , A61K31/47 , A61K31/70 , A61P35/00
CPC分类号： A61K31/437 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708

8. 发明申请

WO2011082267A3 SUBSTITUTED TRIAZOLO-PYRAZINE COMPOUNDS 审中-公开
公开(公告)号：WO2011082267A3
公开(公告)日：2011-11-24
申请号：PCT/US2010062429
申请日：2010-12-29
申请人： ARQULE INC , WESTLUND NEIL
发明人： WESTLUND NEIL
IPC分类号： C07D487/04 , A61K31/4985 , A61P35/00 , C07D401/04 , C07D401/12 , C07D403/12
CPC分类号： C07D487/04
摘要： The present invention relates to substituted triazolo-pyrazine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted triazolo-pyrazine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.

9. 发明申请

WO2011082270A2 SUBSTITUTED IMIDAZOPYRIDINYL-AMINOPYRIDINE COMPOUNDS 审中-公开
标题翻译：取代的咪唑啉氨基亚氨基吡啶化合物
公开(公告)号：WO2011082270A2
公开(公告)日：2011-07-07
申请号：PCT/US2010/062440
申请日：2010-12-29
申请人： ARQULE. INC. , ASHWELL, Mark, A. , BRASSARD, Chris , FILIKOV, Anton , HILL, Jason , KOERNER, Steffi , LAPIERRE, Jean-Marc , LIU, Yanbin , NAMDEV, Nivedita , NICEWONGER, Robert , PALMA, Rocio , TANDON, Manish , VENSEL, David , MATSUDA, Akihisa , IIMURA, Shin , YAMAMOTO, Yuko
发明人： ASHWELL, Mark, A. , BRASSARD, Chris , FILIKOV, Anton , HILL, Jason , KOERNER, Steffi , LAPIERRE, Jean-Marc , LIU, Yanbin , NAMDEV, Nivedita , NICEWONGER, Robert , PALMA, Rocio , TANDON, Manish , VENSEL, David , MATSUDA, Akihisa , IIMURA, Shin , YAMAMOTO, Yuko
CPC分类号： C07D471/04
摘要： The present invention relates to substituted imidazopyridinyl-aminopyridine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted imidazopyridinyl- aminopyridine 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 - 氨基吡啶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 - 氨基吡啶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。

10. 发明申请

WO2011079142A3 PURIFIED PYRROLOQUINOLINYL-PYRROLIDINE-2,5-DIONE COMPOSITIONS AND METHODS FOR PREPARING AND USING SAME 审中-公开
公开(公告)号：WO2011079142A3
公开(公告)日：2011-06-30
申请号：PCT/US2010/061625
申请日：2010-12-21
申请人： ARQULE, INC. , REED, David, P. , BARNES, Neil, R. , KANE, John, C. , LEE, Christopher, A. , CHEN, Jian-xie , REDMON, Martin, P.
发明人： REED, David, P. , BARNES, Neil, R. , KANE, John, C. , LEE, Christopher, A. , CHEN, Jian-xie , REDMON, Martin, P.
IPC分类号： A61K31/417 , A61P35/00
摘要： The present invention relates to a form 1 and form 2 polymorph of (-)-trans -3 -(5,6- dihydro-4 H -pyrrolo [3,2,1- ij ] quinolin-1-yl)-4-(1 H -indol-3-yl) pyrrolidine-2,5-dione. The present invention also relates to (-)-trans-3-(5,6-dihydro-4 H -pyrrolo [3,2,1- ij ] quinolin-1-yl)-4- (1 H -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-4 H -pyrrolo [3,2,1- ij ] quinolin-l-yl)-4-(lH-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-l-yl)-4-(l H -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-4 H -pyrrolo [3,2,1- ij ] quinolin-1-yl)-4-(1 H -indol-3-yl) pyrrolidine-2,5-dione.

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