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91. 发明申请

WO2010114894A1 SUBSTITUTED HETEROCYCLIC COMPOUNDS 审中-公开
标题翻译：取代的杂环化合物
公开(公告)号：WO2010114894A1
公开(公告)日：2010-10-07
申请号：PCT/US2010/029393
申请日：2010-03-31
申请人： ARQULE, INC. , NICEWONGER, Robert , DALTON, Audra , BRASSARD, Chris , ASHWELL, Mark, A. , PALMA, Rocio
发明人： NICEWONGER, Robert , DALTON, Audra , BRASSARD, Chris , ASHWELL, Mark, A. , PALMA, Rocio
IPC分类号： C07D473/26 , C07D487/04 , A61K31/52 , A61P35/00
CPC分类号： C07D473/26 , C07D487/04
摘要： The present invention relates to substituted heterocyclic compounds and substituted tetrahydroisoquinoline compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted benzodiazepine compounds and substituted tetrahydroisoquinoline 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：本发明涉及取代的杂环化合物和取代的四氢异喹啉化合物及其合成方法。本发明还涉及含有取代的苯并二氮杂化合物和取代的四氢异喹啉化合物的药物组合物以及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。

92. 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。

93. 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。

94. 发明申请

WO2006020719A3 AMINOACID CONJUGATES OF BETA - LAPACHONE FOR TUMOR TARGETING 审中-公开
标题翻译： BETA的氨基酸结合 - 用于肿瘤靶向的LAPACHONE
公开(公告)号：WO2006020719A3
公开(公告)日：2007-05-18
申请号：PCT/US2005028438
申请日：2005-08-11
申请人： ARQULE INC , ASHWELL MARK , TANDON MANISH , LAPIERRE JEAN-MARC , LIU YANBIN
发明人： ASHWELL MARK , TANDON MANISH , LAPIERRE JEAN-MARC , LIU YANBIN
IPC分类号： A61K47/48 , A61P35/00 , C07D311/92
CPC分类号： B82Y5/00 , A61K31/785 , A61K47/54 , A61K47/542 , A61K47/64 , A61K47/665
摘要： The present invention relates to quinone prodrug compositions and therapeutic methods using such prodrug compositions. Preferably, the quinone compounds of the invention are napthoquinone compounds such as ß-lapachone or ß-lapachone analogs. The quinone prodrug compositions of the invention exhibit improved solubility, stability, bioavailability, and pharmacokinetic properties, as well as improved plasma half-life in vivo.
摘要翻译：本发明涉及醌前药组合物和使用这种前药组合物的治疗方法。优选地，本发明的醌化合物是萘醌化合物，例如ß-lapachone或ß-lapachone类似物。本发明的醌前药组合物表现出改进的溶解度，稳定性，生物利用度和药代动力学性质，以及体内改善的血浆半衰期。

95. 发明申请

WO2006128120A3 NOVEL LAPACHONE COMPOUNDS AND METHODS OF USE THEREOF 审中-公开
标题翻译：新型LAPACHONE化合物及其使用方法
公开(公告)号：WO2006128120A3
公开(公告)日：2007-01-18
申请号：PCT/US2006020780
申请日：2006-05-26
申请人： ARQULE INC , ASHWELL MARK , TANDON MANISH , LAPIERRE JEAN-MARC , ALI SYED , LIU YANBIN , LI CHIANG J
发明人： ASHWELL MARK , TANDON MANISH , LAPIERRE JEAN-MARC , ALI SYED , LIU YANBIN , LI CHIANG J
IPC分类号： C07D327/08 , A61K31/39 , A61P35/00 , C07D401/12 , C07D419/06 , C07D471/06
CPC分类号： C07D491/10 , C07D327/02 , C07D327/06 , C07D411/06 , C07D411/12
摘要： The invention provides lapachone analogs and derivatives as well as methods of use thereof. These compounds can be used in pharmaceutical compositions for the treatment or prevention of cell proliferation disorders. These compounds can also be used in the treatment or prevention of cancer or precancerous conditions.
摘要翻译：本发明提供了拉帕酮类似物和衍生物及其使用方法。这些化合物可以用于治疗或预防细胞增殖障碍的药物组合物中。这些化合物也可用于治疗或预防癌症或癌前病症。

96. 发明申请

WO2006010082A1 1,4-DISUBSTITUTED NAPHTALENES AS INHIBITORS OF P38 MAP KINASE 审中-公开
标题翻译：作为P38 MAP激酶的抑制剂的1,4-取代的NAPHTALENENEN
公开(公告)号：WO2006010082A1
公开(公告)日：2006-01-26
申请号：PCT/US2005/024441
申请日：2005-07-08
申请人： ARQULE, INC. , ASHWELL, Mark Antony , LIU, Yanbin , ALI, Syed , HILL, Jason , WRONA, Woj
发明人： ASHWELL, Mark Antony , LIU, Yanbin , ALI, Syed , HILL, Jason , WRONA, Woj
IPC分类号： C07D213/81 , C07D401/04 , C07D491/20 , C07D295/14 , C07D231/12 , C07D217/26 , C07D213/82 , C07D239/42 , C07D239/48 , C07D209/42 , C07D285/14 , C07D321/10 , C07D241/08 , C07D307/54 , C07D209/48
CPC分类号： C07D295/185 , C07D207/27 , C07D207/327 , C07D207/404 , C07D209/12 , C07D209/42 , C07D209/44 , C07D209/48 , C07D211/22 , C07D211/46 , C07D211/58 , C07D211/60 , C07D213/30 , C07D213/56 , C07D213/61 , C07D213/81 , C07D213/82 , C07D215/38 , C07D217/04 , C07D217/26 , C07D231/12 , C07D231/14 , C07D239/38 , C07D239/42 , C07D239/47 , C07D239/48 , C07D239/56 , C07D241/08 , C07D249/12 , C07D257/04 , C07D261/08 , C07D263/14 , C07D277/24 , C07D285/14 , C07D295/088 , C07D295/155 , C07D307/42 , C07D317/60 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/04 , C07D491/10
摘要： In general, the present invention relates to compounds capable of inhibiting P38, methods for inhibiting P38 in vivo or in vitro, diagnostics for determining activity in the treatment of P38 and/or cytokine-associated conditions and methods for treating conditions associated with P38 activity or cytokine activity.
摘要翻译：通常，本发明涉及能够抑制P38的化合物，体内或体外抑制P38的方法，用于确定治疗P38和/或细胞因子相关病症的活性的诊断和用于治疗与P38活性有关的病症的方法或细胞因子活性。

97. 发明申请

WO2005082358A3 USE OF BETA-LAPACHONE AS A BROAD SPECTRUM ANTI-CANCER AGENT 审中-公开
标题翻译：使用BETA-LAPACHONE作为广谱抗癌剂
公开(公告)号：WO2005082358A3
公开(公告)日：2005-12-15
申请号：PCT/US2005005647
申请日：2005-02-18
申请人： ARQULE INC , LI CHIANG J , LI YOUZHI
发明人： LI CHIANG J , LI YOUZHI
IPC分类号： A61K31/352 , A61P35/00 , A61P35/02
CPC分类号： A61K31/352
摘要： The present invention provides for methods that utilize agents effective in the treatment of a wide range of cancerous and pre-cancerous conditions. Moreover, the present invention provides agents capable of acting as an inhibitor of cell proliferation in a broad range of cell types.
摘要翻译：本发明提供了利用有效治疗广泛的癌性和癌前病症的药剂的方法。此外，本发明提供能够在广泛范围的细胞类型中作为细胞增殖抑制剂的药剂。

98. 发明申请

WO2005082358A2 BETA-LAPACHONE IS A BROAD SPECTRUM ANTI-CANCER AGENT 审中-公开
标题翻译： BETA-LAPACHONE是广谱抗癌剂
公开(公告)号：WO2005082358A2
公开(公告)日：2005-09-09
申请号：PCT/US2005/005647
申请日：2005-02-18
申请人： ARQULE, INC. , LI, Chiang J. , LI, YouZhi
发明人： LI, Chiang J. , LI, YouZhi
IPC分类号： A61K31/352
CPC分类号： A61K31/352
摘要： The present invention provides for methods that utilize agents effective in the treatment of a wide range of cancerous and pre-cancerous conditions. Moreover, the present invention provides agents capable of acting as an inhibitor of cell proliferation in a broad range of cell types.
摘要翻译：本发明提供了利用有效治疗广泛癌性和癌前病症的药物的方法。此外，本发明提供能够在广泛范围的细胞类型中作为细胞增殖抑制剂的药剂。

99. 发明申请

WO2005082357A1 USE OF BETA-LAPACHONE FOR TREATING HEMATOLOGIC TUMORS 审中-公开
标题翻译：用于治疗血液肿瘤的BETA-LAPACHONE的用途
公开(公告)号：WO2005082357A1
公开(公告)日：2005-09-09
申请号：PCT/US2005/005646
申请日：2005-02-18
申请人： ArQULE, INC. , LI, Chiang J. , LI, YouZhi
发明人： LI, Chiang J. , LI, YouZhi
IPC分类号： A61K31/352
CPC分类号： A61K31/352
摘要： The present invention provides for methods that utilize agents effective in the treatment of hematologic cancers and pre-cancerous hematologic cancer conditions. Moreover, the present invention provides agents capable of acting as an inhibitor of cell proliferation in hematologic cells.
摘要翻译：本发明提供了利用有效治疗血液癌症和癌前血液癌症状况的药物的方法。此外，本发明提供能够作为血液细胞中细胞增殖抑制剂的药剂。

100. 发明申请

WO2005082354A1 BETA-LAPACHONE AND S-PHASE DRUG COMBINATIONS FOR CANCER TREATMENT 审中-公开
标题翻译：用于癌症治疗的BETA-LAPACHONE和S-Phase药物组合
公开(公告)号：WO2005082354A1
公开(公告)日：2005-09-09
申请号：PCT/US2005/005620
申请日：2005-02-23
申请人： ARQULE, INC. , LI, Chiang J.
发明人： LI, Chiang J.
IPC分类号： A61K31/352
CPC分类号： A61K31/352 , A61K31/7064 , A61K2300/00
摘要： Cancers and /or malignancies can be treated by administration of a G1/S phase drug, which is preferably β-lapachone, or a pharmaceutically acceptable salt, prodrug, metabolite, analog or derivative thereof, combined with an S phase drug, which is advantageously gemcitabine. This combination of a G1/S phase drug with an S phase drug results in an unexpectedly effective treatment of cancer. The invention includes methods of treating cancers by administering a combination of a G1/S phase drug and an S phase drug, pharmaceutical compositions comprising the combination of drugs used in these methods, as well as pharmaceutical kits.
摘要翻译：可以通过施用G1 / S期药物来治疗癌症和/或恶性肿瘤，所述G1 / S期药物优选是β-拉帕酮，或其药学上可接受的盐，前药，代谢物，类似物或衍生物，其与S期药物组合，其有利吉西他滨。 G1 / S期药物与S期药物的组合导致了意想不到的有效治疗癌症。本发明包括通过施用G1 / S期药物和S期药物的组合来治疗癌症的方法，包括在这些方法中使用的药物的组合的药物组合物以及药物试剂盒。

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