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1. 发明申请

US20130303489A1 MULTIKINASE INHIBITORS FOR USE IN THE TREATMENT OF CANCER 有权
公开(公告)号：US20130303489A1
公开(公告)日：2013-11-14
申请号：US13794635
申请日：2013-03-11
申请人： Sergei Agoulnik , Bruce Decosta , Hong Du , Yimin Jiang , Xiang-Yi Li , Kenichi Nomoto , John (Yuan) Wang , Huiming Zhang
发明人： Sergei Agoulnik , Bruce Decosta , Hong Du , Yimin Jiang , Xiang-Yi Li , Kenichi Nomoto , John (Yuan) Wang , Huiming Zhang
IPC分类号： A61K31/365 , A61K45/06 , A61K31/4178 , A61K31/496 , A61K31/422 , A61K31/5377 , A61K31/4025 , A61K31/4523 , A61K31/665
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.

2. 发明申请

US20090291998A1 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：US20090291998A1
公开(公告)日：2009-11-26
申请号：US12396849
申请日：2009-03-03
申请人： Sergei Agoulnik , Kozo Akasaka , Francis Fang , Jean-Christophe Harmange , Lynn Hawkins , Yimin Jiang , Charles Johannes , Xiang-Yi Li , Pamela McGuinness , Erin A. Murphy , Shawn Schiller , Mary Vermeulen , Jiayi Wu
发明人： Sergei Agoulnik , Kozo Akasaka , Francis Fang , Jean-Christophe Harmange , Lynn Hawkins , Yimin Jiang , Charles Johannes , Xiang-Yi Li , Pamela McGuinness , Erin A. Murphy , Shawn Schiller , Mary Vermeulen , Jiayi Wu
IPC分类号： A61K31/4035 , C07D303/36 , C07D317/06 , C07D307/78 , C07D209/04 , C07D311/04 , A61K31/336 , A61K31/357 , A61K31/343 , A61K31/352 , A61P35/00
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 (1): wherein R1-R6, A, J, D, A, 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（1）的化合物：其中R 1 -R 6，A，J，D，A，G，Q，w，x，y和z如本文中所述的类别和亚类所述，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。

3. 发明申请

US20060154312A1 Tubulin isotype screening in cancer therapy using halichondrin B analogs 审中-公开
标题翻译：使用软骨素B类似物的癌症治疗中的微管蛋白同种型筛选
公开(公告)号：US20060154312A1
公开(公告)日：2006-07-13
申请号：US11299260
申请日：2005-12-07
申请人： Sergei Agoulnik , Galina Kuznetsov , Bruce Littlefield
发明人： Sergei Agoulnik , Galina Kuznetsov , Bruce Littlefield
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. 发明授权

US08609640B2 Multikinase inhibitors for use in the treatment of cancer 有权
公开(公告)号：US08609640B2
公开(公告)日：2013-12-17
申请号：US12180408
申请日：2008-07-25
申请人： Sergei Agoulnik , Bruce Decosta , Hong Du , Yimin Jiang , Xiang-Yi Li , Kenichi Nomoto , John (Yuan) Wang , Huiming Zhang , Jiayi Wu
发明人： Sergei Agoulnik , Bruce Decosta , Hong Du , Yimin Jiang , Xiang-Yi Li , Kenichi Nomoto , John (Yuan) Wang , Huiming Zhang , Jiayi Wu
IPC分类号： A01N57/00 , A61K31/665 , A01N43/02 , A61K31/335 , A01N43/76 , A61K31/42 , A61K31/415 , A61K31/497 , A61K31/535
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.

5. 发明授权

US07524883B2 Eponemycin and epoxomicin analogs and uses thereof 失效
标题翻译：环孢霉素和环氧素类似物及其用途
公开(公告)号：US07524883B2
公开(公告)日：2009-04-28
申请号：US10501120
申请日：2003-01-08
申请人： Sergei Agoulnik , Kozo Akasaka , Frank Fang , Jean-Christophe Harmange , Lynn Hawkins , Yimin Jiang , Charles Johannes , Xiang-Yi Li , Pamela McGuiness , Erin A. Murphy , Shawn Schiller , Mary Vermeulen , Jiayi Wu
发明人： Sergei Agoulnik , Kozo Akasaka , Frank Fang , Jean-Christophe Harmange , Lynn Hawkins , Yimin Jiang , Charles Johannes , Xiang-Yi Li , Pamela McGuiness , Erin A. Murphy , Shawn Schiller , Mary Vermeulen , Jiayi Wu
IPC分类号： C07D303/46 , A61K31/336
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 (1): wherein R1-R6, 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：本发明提供了具有式（1）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。

6. 发明申请

US20090082313A1 Multikinase Inhibitors for Use in the Treatment of Cancer 有权
标题翻译：用于治疗癌症的多核苷酸酶抑制剂
公开(公告)号：US20090082313A1
公开(公告)日：2009-03-26
申请号：US12180408
申请日：2008-07-25
申请人： Sergei Agoulnik , Bruce Decosta , Hong Du , Yimin Jiang , Xiang-Yi Li , Kenichi Nomoto , John (Yuan) Wang , Huiming Zhang
发明人： Sergei Agoulnik , Bruce Decosta , Hong Du , Yimin Jiang , Xiang-Yi Li , Kenichi Nomoto , John (Yuan) Wang , Huiming Zhang
IPC分类号： A61K31/665 , A61K31/335 , A61K31/422 , A61K31/4178 , A61P35/00 , A61P35/02 , A61P35/04 , A61K31/496 , A61K31/5377
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。

7. 发明申请

US20050101781A1 Eponemycin and epoxomicin analogs and uses thereof 失效
标题翻译：环孢霉素和环氧素类似物及其用途
公开(公告)号：US20050101781A1
公开(公告)日：2005-05-12
申请号：US10501120
申请日：2003-01-08
申请人： Sergei Agoulnik , Kozo Akasaka , Francis Fang , Jean-Christophe Harmange , Lynn Hawkins , Yimin Jiang , Charles Johannes , Xiang-Yi Li , Pamela McGuinness , Erin Murphy , Shawn Schiller , Mary Vermeulen , Jiayi Wu
发明人： Sergei Agoulnik , Kozo Akasaka , Francis Fang , Jean-Christophe Harmange , Lynn Hawkins , Yimin Jiang , Charles Johannes , Xiang-Yi Li , Pamela McGuinness , Erin Murphy , Shawn Schiller , Mary Vermeulen , Jiayi Wu
IPC分类号： C07D303/14 , A61K31/165 , A61K31/166 , A61K31/167 , A61K31/336 , A61K31/343 , A61K31/353 , A61K31/36 , A61K31/40 , A61K31/4025 , A61K31/4035 , A61K31/4045 , A61K31/4427 , A61K31/4709 , A61K31/4725 , A61K31/497 , A61K31/498 , A61K31/662 , A61K31/69 , A61K38/00 , A61P29/00 , A61P31/18 , A61P35/00 , A61P35/02 , A61P37/00 , A61P43/00 , C07C233/76 , C07C235/82 , C07C237/06 , C07C237/08 , C07C271/22 , C07D209/48 , C07D303/36 , C07D405/12 , C07D407/12 , C07F5/02 , C07F9/655 , C07K5/078 , A61K31/382 , C07D43/02 , C07D49/02
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 haviang formula (1): wherein R1-R6, 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：本发明提供了式（1）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，并且另外提供其药物组合物，以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

US20100190843A1 Tubulin Isotype Screening in Cancer Therapy Using Halichondrin B Analogs 审中-公开
标题翻译：使用Halichondrin B类似物的癌症治疗中的微管蛋白同种型筛选
公开(公告)号：US20100190843A1
公开(公告)日：2010-07-29
申请号：US12534277
申请日：2009-08-03
申请人： Sergei Agoulnik , Galina Kuznetsov , Bruce A. Littlefield
发明人： Sergei Agoulnik , Galina Kuznetsov , Bruce A. Littlefield
IPC分类号： A61K31/335 , C07H21/04 , G01N33/68 , C12Q1/02 , G01N33/48 , C12Q1/68 , C40B30/04 , G01N33/53 , A61P35/00
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。

9. 发明申请

US20060148014A1 Tubulin isotype screening in cancer therapy using hemiasterlin analogs 审中-公开
标题翻译：使用半球蛋白类似物的癌症治疗中的微管蛋白同种型筛选
公开(公告)号：US20060148014A1
公开(公告)日：2006-07-06
申请号：US11296920
申请日：2005-12-07
申请人： Sergei Agoulnik , Galina Kuznetsov , Bruce Littlefield
发明人： Sergei Agoulnik , Galina Kuznetsov , Bruce Littlefield
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。

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