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1. 发明申请

WO2010078421A8 SUBSTITUTED 5,6-DIHYDRO-6-PHENYLBENZO[F] ISOQUINOLIN-2-AMINE COMPOUNDS 审中-公开
公开(公告)号：WO2010078421A8
公开(公告)日：2010-07-08
申请号：PCT/US2009/069813
申请日：2009-12-30
申请人： ARQULE, INC. , ALI, Syed, M. , ASHWELL, Mark , TANDON, Manish , YANG, Rui-yang , LIU, Yanbin , VENSEL, David , EATHIRAJ, Sudharshan , PALMA, Rocio , LAPIERRE, Jean-marc , WESTLUND, Neil , WU, Hui , NAMDEV, Nivedita , KELLEHER, Eugene
发明人： ALI, Syed, M. , ASHWELL, Mark , TANDON, Manish , YANG, Rui-yang , LIU, Yanbin , VENSEL, David , EATHIRAJ, Sudharshan , PALMA, Rocio , LAPIERRE, Jean-marc , WESTLUND, Neil , WU, Hui , NAMDEV, Nivedita , KELLEHER, Eugene
IPC分类号： C07D221/10 , C07D401/12 , C07D471/10 , A61K31/55 , A61P35/00
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.

2. 发明申请

WO2009002808A2 QUINAZOLINONE COMPOUNDS AND METHODS OF USE THEREOF 审中-公开
标题翻译：喹唑啉酮化合物及其使用方法
公开(公告)号：WO2009002808A2
公开(公告)日：2008-12-31
申请号：PCT/US2008/067571
申请日：2008-06-19
申请人： ARQULE, INC. , LIU, Jifeng , ALI, Syed, M. , ASHWELL, Mark, A. , YE, Ping , GUAN, Yousheng , NG, Shi-chung , PALMA, Rocio , YOHANNES, Dan
发明人： LIU, Jifeng , ALI, Syed, M. , ASHWELL, Mark, A. , YE, Ping , GUAN, Yousheng , NG, Shi-chung , PALMA, Rocio , YOHANNES, Dan
IPC分类号： C07D239/90 , A61K31/517 , A61P35/00
CPC分类号： C07D239/90
摘要： The present invention relates to quinazolinone compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising the quinazolinone 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 quinazolinone compound of the present invention
摘要翻译：本发明涉及喹唑啉酮化合物及其制备方法。本发明还涉及包含喹唑啉酮化合物的药物组合物。本发明提供了通过向有需要的受试者施用治疗有效量的本发明的喹唑啉酮化合物来治疗细胞增殖性疾病如癌症的方法

3. 发明申请

WO2011123678A3 SUBSTITUTED BENZO-PYRIDO-TRIAZOLO-DIAZEPINE COMPOUNDS 审中-公开
标题翻译：取代的苯并吡喃三唑并 - 二氮杂萘化合物
公开(公告)号：WO2011123678A3
公开(公告)日：2012-01-12
申请号：PCT/US2011030774
申请日：2011-03-31
申请人： ARQULE INC , ALI SYED M , ASHWELL MARK A , KELLEHER EUGENE , KOERNER STEFFI , LAPIERRE JEAN-MARC , LINK JEFFREY S , LIU YANBIN , MOUSSA MAGDI , PALMA ROCIO , TANDON MANISH , VENSEL DAVID , WESTLUND NEIL , WU HUI , YANG RUI-YANG
发明人： ALI SYED M , ASHWELL MARK A , KELLEHER EUGENE , KOERNER STEFFI , LAPIERRE JEAN-MARC , LINK JEFFREY S , LIU YANBIN , MOUSSA MAGDI , PALMA ROCIO , TANDON MANISH , VENSEL DAVID , WESTLUND NEIL , WU HUI , YANG RUI-YANG
IPC分类号： C07D471/14 , A61K31/5517 , A61P35/00 , C07D401/04 , C07D405/04 , C07D487/04
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。

4. 发明申请

WO2011082271A3 SUBSTITUTED TRIAZOLO-PYRIMIDINE COMPOUNDS 审中-公开
标题翻译：取代的三唑基 - 嘧啶化合物
公开(公告)号：WO2011082271A3
公开(公告)日：2011-11-17
申请号：PCT/US2010062442
申请日：2010-12-29
申请人： ARQULE INC , ALI SYED M
发明人： ALI SYED M
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00 , C07D401/10 , C07D401/14 , C07D403/04
CPC分类号： C07D487/04
摘要： The present invention relates to substituted triazolo-pyrimidine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted triazolo-pyrimidine 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：本发明涉及取代的三唑并嘧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三唑并嘧啶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于有需要的受试者来治疗细胞增殖性病症如癌症的方法。

5. 发明申请

WO2011123678A2 SUBSTITUTED BENZO-PYRIDO-TRIAZOLO-DIAZEPINE COMPOUNDS 审中-公开
标题翻译：取代的苯并吡喃三唑并 - 二氮杂萘化合物
公开(公告)号：WO2011123678A2
公开(公告)日：2011-10-06
申请号：PCT/US2011/030774
申请日：2011-03-31
申请人： ARQULE, INC. , ALI, Syed, M. , ASHWELL, Mark, A. , KELLEHER, Eugene , KOERNER, Steffi , LAPIERRE, Jean-Marc , LINK, Jeffrey, S. , LIU, Yanbin , MOUSSA, Magdi , PALMA, Rocio , TANDON, Manish , VENSEL, David , WESTLUND, Neil , WU, Hui , YANG, Rui-Yang
发明人： ALI, Syed, M. , ASHWELL, Mark, A. , KELLEHER, Eugene , KOERNER, Steffi , LAPIERRE, Jean-Marc , LINK, Jeffrey, S. , LIU, Yanbin , MOUSSA, Magdi , PALMA, Rocio , TANDON, Manish , VENSEL, David , WESTLUND, Neil , WU, Hui , YANG, Rui-Yang
IPC分类号： C07D471/14 , C07D405/04 , C07D401/04 , C07D487/04 , A61K31/5517 , A61P35/00
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。

6. 发明申请

WO2011082271A2 SUBSTITUTED TRIAZOLO-PYRIMIDINE COMPOUNDS 审中-公开
标题翻译：取代的三唑并吡啶化合物
公开(公告)号：WO2011082271A2
公开(公告)日：2011-07-07
申请号：PCT/US2010/062442
申请日：2010-12-29
申请人： ARQULE, INC. , ALI, Syed, M.
发明人： ALI, Syed, M.
CPC分类号： C07D487/04
摘要： The present invention relates to substituted triazolo-pyrimidine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted triazolo-pyrimidine 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：本发明涉及取代的三唑并嘧啶化合物及其合成方法。本发明还涉及含有取代的三唑并嘧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。

7. 发明申请

WO2009049305A3 5- (2-HYDROXYPHENYL) TETRAZOLES AS HSP90 INHIBITORS AGAINST CANCER 审中-公开
标题翻译： 5-（2-羟基苯基）四氢叶酸作为HSP90抗癌剂抑制剂
公开(公告)号：WO2009049305A3
公开(公告)日：2009-07-02
申请号：PCT/US2008079755
申请日：2008-10-14
申请人： ARQULE INC , YANG RUI-YANG , ALI SYED M , ASHWELL MARK A , KELLEHER EUGENE , PALMA ROCIO , WESTLUND NEIL
发明人： YANG RUI-YANG , ALI SYED M , ASHWELL MARK A , KELLEHER EUGENE , PALMA ROCIO , WESTLUND NEIL
IPC分类号： C07D257/04 , A61K31/41 , A61P35/00 , C07D401/10 , C07D403/04 , C07D403/10 , C07D403/12
CPC分类号： C07D257/04 , C07D401/10 , C07D403/04 , C07D403/10 , C07D403/12
摘要： The present invention provides tetrazole compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising the tetrazole 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 compound of the present invention, formula (I) wherein: R1 is selected from the group consisting of hydrogen, CH3, F, Cl, Br, and I; R2 is selected from the group consisting of hydrogen, OH, SH, CH3, -CONH2, NHR16, -CH2OH, - CH2SH, and -CH2NH2; R16 is hydrogen, CH3, or C2H3; R3 is selected from the group consisting of hydrogen, F, Cl, Br, I, NO2, CN, -(C1-C6) alkyl, -(C1 -C6) substituted alkyl, C2-C6 alkenyl, (C3-C9) cycloalkyl, (C3-C9) substituted cycloalkyl; -OR8, -NR9R10, -C(=O)-, WR11, -C(=O)-NR12R13, and formula (II); R4 is selected from the group consisting of hydrogen, (C1 -C6) alkyl, (C1-C6) substituted alkyl, (C3-C9) cycloalkyl, (C3-C9) substituted cycloalkyl; aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocyclyl, substituted heterocyciyl, -OR14, and formula (III). The present invention relates to tetrazole compounds and the use of as HSP90 inhibitors for cancer.
摘要翻译：本发明提供了四唑化合物，以及这些化合物的制备方法。本发明还涉及包含四唑化合物的药物组合物。本发明提供了通过向有需要的受试者施用治疗有效量的本发明化合物式（I）的式（I）化合物，其中：R1选自下组：治疗细胞增殖性疾病如癌症的方法，的氢，CH3，F，Cl，Br和I; R 2选自氢，OH，SH，CH 3，-CONH 2，NHR 16，-CH 2 OH，-CH 2 SH和-CH 2 NH 2; R 16是氢，CH 3或C 2 H 3; R3选自氢，F，Cl，Br，I，NO2，CN， - （C1-C6）烷基， - （C1-C6）取代的烷基，C2-C6烯基，（C3-C9），（C 3 -C 9）取代的环烷基; -OR8，-NR9R10，-C（= O） - ，WR11，-C（= O）-NR12R13和式（Ⅱ）; R4选自氢，（C1-C6）烷基，（C1-C6）取代的烷基，（C3-C9）环烷基，（C3-C9）取代的环烷基; 芳基，取代的芳基，杂芳基，取代的杂芳基，杂环基，取代的杂胞基，-OR14和式（III）。本发明涉及四唑化合物和作为HSP90抑制剂用于癌症的用途。

8. 发明申请

WO2009049305A2 SUBSTITUTED TETRAZOLE COMPOUNDS AND USES THEREOF 审中-公开
标题翻译：取代的四唑化合物及其用途
公开(公告)号：WO2009049305A2
公开(公告)日：2009-04-16
申请号：PCT/US2008/079755
申请日：2008-10-14
申请人： ARQULE, INC. , YANG, Rui-Yang , ALI, Syed, M. , ASHWELL, Mark, A. , KELLEHER, Eugene , PALMA, Rocio , WESTLUND, Neil
发明人： YANG, Rui-Yang , ALI, Syed, M. , ASHWELL, Mark, A. , KELLEHER, Eugene , PALMA, Rocio , WESTLUND, Neil
IPC分类号： C07D257/04 , C07D403/04 , C07D401/04 , C07D401/14 , C07D403/10 , C07D413/14 , C07D413/12
CPC分类号： C07D257/04 , C07D401/10 , C07D403/04 , C07D403/10 , C07D403/12
摘要： The present invention provides tetrazole compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising the tetrazole 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 compound of the present invention.
摘要翻译：本发明提供了四唑化合物及其制备方法。本发明还涉及包含四唑化合物的药物组合物。本发明提供了通过向有需要的受试者施用治疗有效量的本发明化合物来治疗细胞增殖性疾病如癌症的方法。

9. 发明申请

WO2006126991A1 METHOD AND APPARATUS FOR GENERATING COMPONENTS FOR PATTERN-BASED SYSTEM DESIGN ANALYSIS USING A CHARACTERISTICS MODEL 审中-公开
标题翻译：用于使用特征模型生成基于模式的系统设计分析的组件的方法和装置
公开(公告)号：WO2006126991A1
公开(公告)日：2006-11-30
申请号：PCT/US2005/018008
申请日：2005-05-23
申请人： SUN MICROSYSTEMS, INC. , ALI, Syed, M. , KAMEN, Yury , ALUR, Deepak , CRUPI, John, P. , MALKS, Daniel, B.
发明人： ALI, Syed, M. , KAMEN, Yury , ALUR, Deepak , CRUPI, John, P. , MALKS, Daniel, B.
IPC分类号： G06F9/44
CPC分类号： G06F8/75
摘要： A method for analyzing a target system (100) that includes obtaining a characteristics model (108), generating at least one selected from the group consisting of a schema, characteristics store API (104), and a characteristics extractor (102A, 102N), using the characteristics model (108), obtaining a plurality of characteristics from the target system (100) using characteristics extractor (102A, 102N), wherein each of the plurality of characteristics is associated with the characteristics model (108), storing each of the plurality of characteristics in the characteristics store (106) using the schema, and analyzing the target system (100) by issuing at least one query to the characteristics store (106) to obtain an analysis result.
摘要翻译：一种用于分析目标系统（100）的方法，包括获得特征模型（108），生成从由模式，特征存储API（104）和特征提取器（102A，102N）组成的组中选择的至少一个，使用特征模型（108），使用特征提取器（102A，102N）从目标系统（100）获得多个特征，其中多个特征中的每一个与特征模型（108）相关联，存储每个使用该模式的特征存储器（106）中的多个特征，以及通过向特征存储器（106）发出至少一个查询来分析目标系统（100）以获得分析结果。

10. 发明申请

WO2006126989A1 METHOD AND APPARATUS FOR PATTERN-BASED SYSTEM DESIGN ANALYSIS 审中-公开
标题翻译：用于基于模式的系统设计分析的方法和装置
公开(公告)号：WO2006126989A1
公开(公告)日：2006-11-30
申请号：PCT/US2005/018003
申请日：2005-05-23
申请人： SUN MICROSYSTEMS, INC., , ALI, Syed, M. , KAMEN, Yury , ALUR, Deepak , CRUPI, John, P. , MALKS, Daniel, B. , KRISHNAMURTHY, Rajmohan , GODFREY, Michael, W.
发明人： ALI, Syed, M. , KAMEN, Yury , ALUR, Deepak , CRUPI, John, P. , MALKS, Daniel, B. , KRISHNAMURTHY, Rajmohan , GODFREY, Michael, W.
IPC分类号： G06F9/44
CPC分类号： G06F8/75
摘要： A method for analyzing a target system, where the method includes obtaining a plurality of characteristics from the target system using a characteristics extractor wherein each of the plurality of characteristics is associated with a characteristics model, storing each of the plurality of characteristics obtained from the target system in a characteristics store, and analyzing the target system by issuing at least one query to the characteristics store to obtain an analysis result.
摘要翻译：一种用于分析目标系统的方法，其中所述方法包括使用特征提取器从所述目标系统获得多个特征，其中所述多个特征中的每一个与特征模型相关联，存储从所述目标系统获得的所述多个特征中的每一个系统，并通过向特征库发出至少一个查询来分析目标系统以获得分析结果。

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