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1. 发明申请

WO2012129100A1 METHODS AND COMPOSITIONS FOR PREDICTING RESPONSE TO ERIBULIN 审中-公开
标题翻译：用于预测对ERIBULIN的反应的方法和组合物
公开(公告)号：WO2012129100A1
公开(公告)日：2012-09-27
申请号：PCT/US2012/029479
申请日：2012-03-16
申请人： EISAI R&D MANAGEMENT CO., LTD. , AGOULNIK, Sergei, I. , BYRNE, Michael, Chapman , LITTLEFIELD, Bruce, A.
发明人： AGOULNIK, Sergei, I. , BYRNE, Michael, Chapman , LITTLEFIELD, Bruce, A.
IPC分类号： C12Q1/68
CPC分类号： C12Q1/6886 , A61K31/35 , C12Q2600/106 , G01N33/57415
摘要： The invention provides methods for predicting the efficacy of eribulin, an analog thereof, or a pharmaceutically acceptable salt thereof (e.g., eribulin mesylate), in the treatment of a subject suffering from breast cancer by determining the level of particular biomarkers in a sample derived from the subject.
摘要翻译：本发明提供了通过确定衍生自乳腺癌的样品中特定生物标志物的水平来预测患有乳腺癌患者的艾美林，其类似物或其药学上可接受的盐（例如，甲磺酸艾美林）的功效的方法，主题。

2. 发明申请

WO2009058908A3 METHODS FOR PROGNOSING THE ABILITY OF A ZEARALENONE ANALOG COMPOUND TO TREAT CANCER 审中-公开
标题翻译：用于预防ZEARALENONE类似物化合物治疗癌症的能力的方法
公开(公告)号：WO2009058908A3
公开(公告)日：2009-10-22
申请号：PCT/US2008081646
申请日：2008-10-29
申请人： EISAI R&D MAN CO LTD , WANG JOHN YUAN , AGOULNIK SERGEI , NOMOTO KENICHI
发明人： WANG JOHN YUAN , AGOULNIK SERGEI , NOMOTO KENICHI
IPC分类号： G01N33/50 , C12Q1/68
CPC分类号： G01N33/57488 , A61K31/365 , C12Q1/485 , C12Q1/6886 , C12Q2600/106 , G01N33/5011 , G01N2800/52
摘要： The instant invention provides methods of prognosing the ability of a zearalenone analog compound to treat a cancer in a subject, methods of prognosing the ability of a zearalenone analog compound to inhibit the growth of a cancer in a subject, and methods of prognosing the ability of a zearalenone analog compound to promote the activation of apoptosis of a cancer in a subject. Methods of treating a cancer in a subject are also provided. The invention also pertains to methods of determining whether a cancer in a subject is sensitive to treatment with a zearalenone analog compound.
摘要翻译：本发明提供了预测玉米赤霉烯酮类似物化合物治疗受试者癌症的能力的方法，预测玉米赤霉烯酮类似物化合物抑制受试者中癌症生长的能力的方法，以及预测受试者的能力的方法玉米赤霉烯酮类似物化合物以促进受试者中癌症的凋亡的激活。还提供了治疗受试者的癌症的方法。本发明还涉及确定受试者中的癌症是否对玉米赤霉烯酮类似物化合物的治疗敏感的方法。

3. 发明申请

WO2006063135A3 TUBULIN ISOTYPE SCRENNING IN CANCER THERAPY USING HEMIASTERLIN ANALOGS 审中-公开
标题翻译：使用红霉素类似物治疗癌症治疗中的TUBULIN同位异构体
公开(公告)号：WO2006063135A3
公开(公告)日：2009-04-09
申请号：PCT/US2005044426
申请日：2005-12-07
申请人： EISAI R&D MAN CO LTD , AGOULNIK SERGEI , KUZNETSOV GALINA , LITTLEFIELD BRUCE A
发明人： AGOULNIK SERGEI , KUZNETSOV GALINA , LITTLEFIELD BRUCE A
IPC分类号： C12Q1/00 , C12Q1/68 , G01N33/53 , G01N33/574
CPC分类号： G01N33/57415 , A61K9/06 , A61K31/18 , A61K31/44 , A61K38/04 , G01N33/574 , G01N33/57423 , G01N33/57449 , G01N2333/4703 , G01N2800/44
摘要： Chemotherapeutic agents that interfere with microtubule assembly or disassembly in the cell are potent inhibitors of cell replication. Examples of such agents include hemiasterlin analogs. It has been shown that the susceptibility of certain cancers to analogs of hemiasterlin correlates with the expression of particular tubulin isotypes or other microtubule-associated proteins such as MAP-4 and stathmin. Correlations such as these may be used in identifying patients suitable for treatment using a particular chemotherapeutic agent. Such a system avoids treating patients with cytotoxic compounds where there is a minimal or no effect on the cancer. The invention also provides a system of establishing these correlations for different compounds and cancer types. The system will be particularly useful in establishing correlations between anti-microtubule agents and cancers such as lung, breast, and ovarian cancer. Kits and reagents useful in practicing the invention are also provided.
摘要翻译：影响细胞中微管组装或分解的化学治疗剂是细胞复制的有效抑制剂。这些药剂的实例包括半球蛋白类似物。已经表明，某些癌症对半细胞因子类似物的易感性与特定的微管蛋白同种型或其它微管相关蛋白如MAP-4和stathmin的表达相关。诸如这些的相关性可以用于鉴定适合于使用特定化学治疗剂的治疗的患者。这样的系统避免了治疗患有细胞毒性化合物的患者，其中对癌症最小或没有影响。本发明还提供了一种为不同化合物和癌症类型建立这些相关性的系统。该系统将特别有用于建立抗微管剂和肺癌，乳腺癌和卵巢癌等癌症之间的相关性。还提供了可用于实践本发明的试剂盒和试剂。

4. 发明申请

WO2006076100A3 TUBULIN ISOTYPE SCREENING IN CANCER THERAPY USING HALICHONDRIN B ANALOGS 审中-公开
标题翻译：使用HALICHONDRIN B模拟物的癌症治疗中的TUBULIN同位素筛选
公开(公告)号：WO2006076100A3
公开(公告)日：2009-04-02
申请号：PCT/US2005044421
申请日：2005-12-07
申请人： EISAI CO LTD , AGOULNIK SERGEI , KUZNETSOV GALINA , LITTLEFIELD BRUCE A
发明人： AGOULNIK SERGEI , KUZNETSOV GALINA , LITTLEFIELD BRUCE A
IPC分类号： G01N33/574
CPC分类号： A61K31/353 , G01N33/5091 , G01N33/574 , G01N33/57407 , G01N33/57496 , G01N2500/00 , Y10T436/143333
摘要： Chemotherapeutic agents that interfere with microtubule assembly or disassembly in the cell are potent inhibitors of cell replication. Examples of such agents include halichondrin B analogs. It has been shown that the susceptibility of certain cancers to analogs of halichondrin B correlates with the expression of particular tubulin isotypes or other microtubule-associated proteins such as MAP-4 and stathmin. Correlations such as these may be used in identifying patients suitable for treatment using a particular chemotherapeutic agent. Such a system avoids treating patients with cytotoxic compounds where there is a minimal or no effect on the cancer. The invention also provides a system of establishing these correlations for different compounds and cancer types. The system will be particularly useful in establishing correlations between anti-microtubule agents and cancers such as lung, breast, and ovarian cancer. Kits and reagents useful in practicing the invention are also provided.
摘要翻译：影响细胞中微管组装或分解的化学治疗剂是细胞复制的有效抑制剂。这些试剂的实例包括软骨素B类似物。已经显示某些癌症对软骨素B类似物的敏感性与特定的微管蛋白同种型或其它微管相关蛋白如MAP-4和stathmin的表达相关。诸如这些的相关性可以用于鉴定适合于使用特定化学治疗剂的治疗的患者。这样的系统避免了治疗患有细胞毒性化合物的患者，其中对癌症最小或没有影响。本发明还提供了一种为不同化合物和癌症类型建立这些相关性的系统。该系统将特别有用于建立抗微管剂和肺癌，乳腺癌和卵巢癌等癌症之间的相关性。还提供了可用于实践本发明的试剂盒和试剂。

5. 发明申请

WO2009015368A3 MULTIKINASE INHIBITORS FOR USE IN THE TREATMENT OF CANCER 审中-公开
标题翻译：多杀菌素抑制剂用于治疗癌症
公开(公告)号：WO2009015368A3
公开(公告)日：2009-03-26
申请号：PCT/US2008071256
申请日：2008-07-25
申请人： EISAI R&D MAN CO LTD , AGOULNIK SERGEI , DECOSTA BRUCE , DU HONG , JIANG YIMIN , LI XIANG-YI , NOMOTO KENICHI , WANG JOHN YUAN , ZHANG HUIMING
发明人： AGOULNIK SERGEI , DECOSTA BRUCE , DU HONG , JIANG YIMIN , LI XIANG-YI , NOMOTO KENICHI , WANG JOHN YUAN , ZHANG HUIMING
IPC分类号： A61K31/365 , A61P35/00 , A61P35/02 , A61P35/04 , C07D313/00
CPC分类号： A61K31/365 , A61K31/4025 , A61K31/4178 , A61K31/422 , A61K31/4523 , A61K31/496 , A61K31/5377 , A61K31/665 , A61K45/06
摘要： The present invention provides compounds, pharmaceutical compositions and methods for the treatment of specific cancers. Such compositions may generally comprise a compound of formula (I): wherein R1-R3 are as defined herein, or pharmaceutically acceptable salts or esters thereof; and a pharmaceutically acceptable carrier.
摘要翻译：本发明提供了用于治疗特定癌症的化合物，药物组合物和方法。这样的组合物通常可以包含式（I）的化合物：其中R 1 -R 3如本文所定义，或其药学上可接受的盐或酯; 和药学上可接受的载体。

6. 发明申请

WO2006063135A2 TUBULIN ISOTYPE SCRENNING IN CANCER THERAPY USING HEMIASTERLIN ANALOGS 审中-公开
标题翻译：使用红霉素类似物治疗癌症治疗中的TUBULIN同位异构体
公开(公告)号：WO2006063135A2
公开(公告)日：2006-06-15
申请号：PCT/US2005/044426
申请日：2005-12-07
申请人： EISAI CO.LTD. , AGOULNIK, Sergei , KUZNETSOV, Galina , LITTLEFIELD, BRUCE, A.
发明人： AGOULNIK, Sergei , KUZNETSOV, Galina , LITTLEFIELD, BRUCE, A.
IPC分类号： G01N33/574 , A61K31/44 , A61K31/18 , A61K38/04
CPC分类号： G01N33/57415 , A61K9/06 , A61K31/18 , A61K31/44 , A61K38/04 , G01N33/574 , G01N33/57423 , G01N33/57449 , G01N2333/4703 , G01N2800/44
摘要： Chemotherapeutic agents that interfere with microtubule assembly or disassembly in the cell are potent inhibitors of cell replication. Examples of such agents include hemiasterlin analogs. It has been shown that the susceptibility of certain cancers to analogs of hemiasterlin correlates with the expression of particular tubulin isotypes or other microtubule-associated proteins such as MAP-4 and stathmin. Correlations such as these may be used in identifying patients suitable for treatment using a particular chemotherapeutic agent. Such a system avoids treating patients with cytotoxic compounds where there is a minimal or no effect on the cancer. The invention also provides a system of establishing these correlations for different compounds and cancer types. The system will be particularly useful in establishing correlations between anti-microtubule agents and cancers such as lung, breast, and ovarian cancer. Kits and reagents useful in practicing the invention are also provided.
摘要翻译：影响细胞中微管组装或分解的化学治疗剂是细胞复制的有效抑制剂。这些药剂的实例包括半球蛋白类似物。已经表明，某些癌症对半细胞因子类似物的易感性与特定的微管蛋白同种型或其它微管相关蛋白如MAP-4和stathmin的表达相关。诸如这些的相关性可以用于鉴定适合于使用特定化学治疗剂的治疗的患者。这样的系统避免了治疗患有细胞毒性化合物的患者，其中对癌症最小或没有影响。本发明还提供了一种为不同化合物和癌症类型建立这些相关性的系统。该系统将特别有用于建立抗微管剂和肺癌，乳腺癌和卵巢癌等癌症之间的相关性。还提供了可用于实践本发明的试剂盒和试剂。

7. 发明申请

WO2003059898A2 EPONEMYCIN AND EPOXOMICIN ANALOGS AND USES THEREOF 审中-公开
标题翻译： EPONEMYCIN和EPOXOMICIN类似物及其用途
公开(公告)号：WO2003059898A2
公开(公告)日：2003-07-24
申请号：PCT/US2003/000390
申请日：2003-01-08
申请人： EISAI CO. LTD. , AGOULNIK, Sergei , AKASAKA, Kozo , FANG, Frank , HARMANGE, Jean-Christophe , HAWKINS, Lynn , JIANG, Yimin , JOHANNES, Charles , LI, Xiang-Yi , MCGUINNESS, Pamela , MURPHY, Erin , SCHILLER, Shawn , VERMEULEN, Mary , WU, Jiayi
发明人： AGOULNIK, Sergei , AKASAKA, Kozo , FANG, Frank , HARMANGE, Jean-Christophe , HAWKINS, Lynn , JIANG, Yimin , JOHANNES, Charles , LI, Xiang-Yi , MCGUINNESS, Pamela , MURPHY, Erin , SCHILLER, Shawn , VERMEULEN, Mary , WU, Jiayi
IPC分类号： C07D303/36
CPC分类号： C07D209/48 , A61K38/00 , C07D303/36 , C07D405/12 , C07D407/12 , C07F5/025 , C07F9/65502 , C07K5/06139
摘要： The present invention provides compounds having formula (I) : wherein R 1 -R 6 , A, J, D, E, G, Q, w, x, y, and z are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof in the treatment of cancer and/or inflammatory disorders, and more generally as proteasome inhibitors.
摘要翻译：本发明提供具有式（I）的化合物：其中R 1 -R 6，A，J，D，E，G，Q，w，x，y和z如本文中所述的一般和类别和亚类所述，其药物组合物及其用于治疗癌症和/或炎症性疾病的方法，更一般地，作为蛋白酶体抑制剂。

8. 发明申请

WO2009058908A2 METHODS FOR PROGNOSING THE ABILITY OF A ZEARALENONE ANALOG COMPOUND TO TREAT CANCER 审中-公开
标题翻译：预测ZEARALENONE类似物复合物治疗癌症的能力的方法
公开(公告)号：WO2009058908A2
公开(公告)日：2009-05-07
申请号：PCT/US2008/081646
申请日：2008-10-29
申请人： EISAI R & D MANAGEMENT CO., LTD. , WANG, John, (yuan) , AGOULNIK, Sergei , NOMOTO, Kenichi
发明人： WANG, John, (yuan) , AGOULNIK, Sergei , NOMOTO, Kenichi
IPC分类号： G01N33/50 , C12Q1/68
CPC分类号： G01N33/57488 , A61K31/365 , C12Q1/485 , C12Q1/6886 , C12Q2600/106 , G01N33/5011 , G01N2800/52
摘要： The instant invention provides methods of prognosing the ability of a zearalenone analog compound to treat a cancer in a subject, methods of prognosing the ability of a zearalenone analog compound to inhibit the growth of a cancer in a subject, and methods of prognosing the ability of a zearalenone analog compound to promote the activation of apoptosis of a cancer in a subject. Methods of treating a cancer in a subject are also provided. The invention also pertains to methods of determining whether a cancer in a subject is sensitive to treatment with a zearalenone analog compound.
摘要翻译：本发明提供预测玉米赤霉烯酮类似物化合物治疗受试者中癌症的能力的方法，预测玉米赤霉烯酮类似物化合物抑制受试者中癌症生长的能力的方法以及预测玉米赤霉烯酮类似物化合物促进受试者中癌症凋亡活化的能力的方法。还提供了在受试者中治疗癌症的方法。本发明还涉及确定受试者中的癌症是否对用玉米赤霉烯酮类似物化合物治疗敏感的方法。

9. 发明申请

WO2009015368A2 MULTIKINASE INHIBITORS FOR USE IN THE TREATMENT OF CANCER 审中-公开
标题翻译：多杀菌素抑制剂用于治疗癌症
公开(公告)号：WO2009015368A2
公开(公告)日：2009-01-29
申请号：PCT/US2008/071256
申请日：2008-07-25
申请人： EISAI R & D MANAGEMENT CO., LTD. , AGOULNIK, Sergei , DECOSTA, Bruce , DU, Hong , JIANG, Yimin , LI, Xiang-Yi , NOMOTO, Kenichi , WANG, John (Yuan) , ZHANG, Huiming
发明人： AGOULNIK, Sergei , DECOSTA, Bruce , DU, Hong , JIANG, Yimin , LI, Xiang-Yi , NOMOTO, Kenichi , WANG, John (Yuan) , ZHANG, Huiming
IPC分类号： A61K31/365 , C07D313/00 , A61P35/00 , A61P35/02 , A61P35/04
CPC分类号： A61K31/365 , A61K31/4025 , A61K31/4178 , A61K31/422 , A61K31/4523 , A61K31/496 , A61K31/5377 , A61K31/665 , A61K45/06
摘要： The present invention provides compounds, pharmaceutical compositions and methods for the treatment of specific cancers. Such compositions may generally comprise a compound of formula (I):......................................................................................................................... wherein R1-R3 are as defined herein, or pharmaceutically acceptable salts or esters thereof; and a pharmaceutically acceptable carrier.
摘要翻译：本发明提供了用于治疗特定癌症的化合物，药物组合物和方法。这样的组合物通常可以包含式（I）的化合物：..................................... .................................................. 其中R1-R3如本文所定义，或其药学上可接受的盐或酯 ; 和药学上可接受的载体。

10. 发明申请

WO2006076100A2 TUBULIN ISOTYPE SCREENING IN CANCER THERAPY USING HALICHONDRIN B ANALOGS 审中-公开
标题翻译：使用HALICHONDRIN B模拟物的癌症治疗中的TUBULIN同位素筛选
公开(公告)号：WO2006076100A2
公开(公告)日：2006-07-20
申请号：PCT/US2005/044421
申请日：2005-12-07
申请人： EISAI CO. LTD. , AGOULNIK, Sergei , KUZNETSOV, Galina , LITTLEFIELD, Bruce, A.
发明人： AGOULNIK, Sergei , KUZNETSOV, Galina , LITTLEFIELD, Bruce, A.
IPC分类号： G01N33/574 , A61K31/353
CPC分类号： A61K31/353 , G01N33/5091 , G01N33/574 , G01N33/57407 , G01N33/57496 , G01N2500/00 , Y10T436/143333
摘要： Chemotherapeutic agents that interfere with microtubule assembly or disassembly in the cell are potent inhibitors of cell replication. Examples of such agents include halichondrin B analogs. It has been shown that the susceptibility of certain cancers to analogs of halichondrin B correlates with the expression of particular tubulin isotypes or other microtubule-associated proteins such as MAP-4 and stathmin. Correlations such as these may be used in identifying patients suitable for treatment using a particular chemotherapeutic agent. Such a system avoids treating patients with cytotoxic compounds where there is a minimal or no effect on the cancer. The invention also provides a system of establishing these correlations for different compounds and cancer types. The system will be particularly useful in establishing correlations between anti-microtubule agents and cancers such as lung, breast, and ovarian cancer. Kits and reagents useful in practicing the invention are also provided.
摘要翻译：影响细胞中微管组装或分解的化学治疗剂是细胞复制的有效抑制剂。这些试剂的实例包括软骨素B类似物。已经显示某些癌症对软骨素B类似物的敏感性与特定的微管蛋白同种型或其它微管相关蛋白如MAP-4和stathmin的表达相关。诸如这些的相关性可以用于鉴定适合于使用特定化学治疗剂的治疗的患者。这样的系统避免了治疗患有细胞毒性化合物的患者，其中对癌症最小或没有影响。本发明还提供了一种为不同化合物和癌症类型建立这些相关性的系统。该系统将特别有用于建立抗微管剂和肺癌，乳腺癌和卵巢癌等癌症之间的相关性。还提供了可用于实践本发明的试剂盒和试剂。

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