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1. 发明申请

US20110301188A1 Synergistic Effects Between Sphingosine-1-Phosphate Receptor Antagonists and Antimicrotubule Agents 有权
标题翻译：鞘氨醇-1-磷酸受体拮抗剂与抗微管剂之间的协同作用
公开(公告)号：US20110301188A1
公开(公告)日：2011-12-08
申请号：US13124586
申请日：2009-10-16
申请人： Geetha Shankar , Frauke Bentzien , Peter Lamb , David Matthews
发明人： Geetha Shankar , Frauke Bentzien , Peter Lamb , David Matthews
IPC分类号： A61K31/475 , A61P35/00 , A61P35/02 , A61K31/4192
CPC分类号： A61K31/4196 , A61K31/16 , A61K31/337 , A61K31/34 , A61K31/4192 , A61K31/435 , A61K2300/00
摘要： This invention is based on the discovery that the administration of a sphingosine-1-phosphate receptor antagonist (S1P) and at least one chemotherapeutic agent selected from the the group of antimicrotubule agents provides an unexpectedly superior treatment for cancer. Antimicrobial agents such as the taxane compounds are known in the art, for example, paclitaxel (available as TAXOL® from Bristol-Myers Squibb, Princeton, N.J.), docetaxel (available as TAXOTERE® from Sanofi-aventis, Bridgewater, N.J.) and the like and other compounds that act as antimicrotubule agents, such as Vincristine (ONCOVIN®, VINCASAR PFS®, VCR), Vinblastin (VELBAN®, VELSAR®) and Vinorelbine, and similar compounds. The present invention also provides methods of modulating the growth of selected cell populations, such as cancer cells, by administering a therapeutically effective amount of at least one sphingosine-1-phosphate 1 (S1P1R) receptor antagonists, and at least one antimicrotubule agent.
摘要翻译：本发明基于以下发现：施用鞘氨醇-1-磷酸受体拮抗剂（S1P）和选自抗微管剂组的至少一种化学治疗剂提供了对于癌症的意想不到的优异治疗。抗菌剂如紫杉烷化合物是本领域已知的，例如紫杉醇（可从Bristol-Myers Squibb，Princeton，NJ获得），多西紫杉醇（可从Sanofi-aventis，Bridgewater，NJ获得）和类似物和其它作为抗微管剂的化合物，如长春新碱（ONCVIN®，VINCASARPFS®，VCR），长春花碱（VELBAN®，VELSAR）和长春瑞滨等）和类似化合物。本发明还提供了通过施用治疗有效量的至少一种鞘氨醇-1-磷酸1（S1P1R）受体拮抗剂和至少一种抗微管剂来调节所选细胞群体如癌细胞的生长的方法。

2. 发明授权

US08802692B2 Synergistic effects between sphingosine-1-phosphate receptor antagonists and antimicrotubule agents 有权
标题翻译：鞘氨醇-1-磷酸受体拮抗剂和抗微管剂之间的协同作用
公开(公告)号：US08802692B2
公开(公告)日：2014-08-12
申请号：US13124586
申请日：2009-10-16
申请人： Geetha Shankar , Frauke Bentzien , Peter Lamb , David Matthews
发明人： Geetha Shankar , Frauke Bentzien , Peter Lamb , David Matthews
IPC分类号： A61K31/44 , A01N43/36 , A61K31/40
CPC分类号： A61K31/4196 , A61K31/16 , A61K31/337 , A61K31/34 , A61K31/4192 , A61K31/435 , A61K2300/00
摘要： This invention is based on the discovery that the administration of a sphingosine-1-phosphate receptor antagonist (S1P) and at least one chemotherapeutic agent selected from the the group of antimicrotubule agents provides an unexpectedly superior treatment for cancer. Antimicrobial agents such as the taxane compounds are known in the art, for example, paclitaxel (available as TAXOL® from Bristol-Myers Squibb, Princeton, N.J.), docetaxel (available as TAXOTERE® from Sanofi-aventis, Bridgewater, N.J.) and the like and other compounds that act as antimicrotubule agents, such as Vincristine (ONCOVIN®, VINCASAR PFS®, VCR), Vinblastin (VELBAN®, VELSAR®) and Vinorelbine, and similar compounds. The present invention also provides methods of modulating the growth of selected cell populations, such as cancer cells, by administering a therapeutically effective amount of at least one sphingosine-1-phosphate 1 (S1P1R) receptor antagonists, and at least one antimicrotubule agent.
摘要翻译：本发明基于以下发现：施用鞘氨醇-1-磷酸受体拮抗剂（S1P）和选自抗微管剂组的至少一种化学治疗剂提供了对于癌症的意想不到的优异治疗。抗菌剂如紫杉烷化合物是本领域已知的，例如紫杉醇（可从Bristol-Myers Squibb，Princeton，NJ获得），多西紫杉醇（可从Sanofi-aventis，Bridgewater，NJ获得）和类似物和其它作为抗微管剂的化合物，如长春新碱（ONCVIN®，VINCASARPFS®，VCR），长春花碱（VELBAN®，VELSAR）和长春瑞滨等）和类似化合物。本发明还提供了通过施用治疗有效量的至少一种鞘氨醇-1-磷酸1（S1P1R）受体拮抗剂和至少一种抗微管剂来调节所选细胞群体如癌细胞的生长的方法。

3. 发明授权

US08513266B2 Methods of treating cancer using pyridopyrimidinone inhibitors of PI3K alpha 有权
标题翻译：使用PI3Kα的吡啶并嘧啶酮抑制剂治疗癌症的方法
公开(公告)号：US08513266B2
公开(公告)日：2013-08-20
申请号：US12595219
申请日：2008-04-09
申请人： Peter Lamb , David Matthews
发明人： Peter Lamb , David Matthews
IPC分类号： A61K31/519
CPC分类号： A61K31/4745 , A61K31/282 , A61K31/337 , A61K31/517 , A61K31/519 , A61K45/06 , A61K2300/00
摘要： The present invention provides methods of treating cancer by administering a compound of Formula I, optionally as a pharmaceutically acceptable salt, solvate and/or hydrate thereof, in combination with other cancer treatments.(Formula I)
摘要翻译：本发明提供了通过与其它癌症治疗组合施用式I化合物，任选地作为其药学上可接受的盐，溶剂合物和/或水合物来治疗癌症的方法。（式I）

4. 发明申请

US20100209420A1 METHODS OF TREATING CANCER USING PYRIDOPYRIMIDINONE INHIBITORS OF P13K ALPHA 有权
标题翻译：使用P13K ALPHA的吡嗪二酮抑制剂治疗癌症的方法
公开(公告)号：US20100209420A1
公开(公告)日：2010-08-19
申请号：US12595219
申请日：2008-04-09
申请人： Peter Lamb , David Matthews
发明人： Peter Lamb , David Matthews
IPC分类号： A61K39/395 , A61K31/519 , A61P35/04
CPC分类号： A61K31/4745 , A61K31/282 , A61K31/337 , A61K31/517 , A61K31/519 , A61K45/06 , A61K2300/00
摘要： The present invention provides methods of treating cancer by administering a compound of Formula I, optionally as a pharmaceutically acceptable salt, solvate and/or hydrate thereof, in combination with other cancer treatments.(Formula I)
摘要翻译：本发明提供了通过与其它癌症治疗组合施用式I化合物，任选地作为其药学上可接受的盐，溶剂合物和/或水合物来治疗癌症的方法。（式I）

5. 发明授权

US08481001B2 Combination therapies comprising quinoxaline inhibitors of P13K-alpha for use in the treatment of cancer 有权
标题翻译：组合疗法包括用于治疗癌症的P13K-α的喹喔啉抑制剂
公开(公告)号：US08481001B2
公开(公告)日：2013-07-09
申请号：US12595236
申请日：2008-04-08
申请人： Peter Lamb , David Matthews
发明人： Peter Lamb , David Matthews
IPC分类号： A61K31/5377 , A61K31/551 , A61K39/395
CPC分类号： A61K31/337 , A61K31/436 , A61K31/497 , A61K31/498 , A61K31/4985 , A61K31/517 , A61K31/555 , A61K45/06 , A61K2300/00
摘要： The present invention provides methods of treating cancer by administering a compound of Formula I, optionally as a pharmaceutically acceptable salt, solvate and/or hydrate thereof, in combination with other cancer treatments.
摘要翻译：本发明提供了通过与其它癌症治疗组合施用式I化合物，任选地作为其药学上可接受的盐，溶剂合物和/或水合物来治疗癌症的方法。

6. 发明申请

US20110123434A1 COMBINATION THERAPIES COMPRISING QUINOXALINE INHIBITORS OF P13K-ALPHA FOR USE IN THE TREATMENT OF CANCER 有权
标题翻译：包含用于治疗癌症的P13K-ALPHA的喹诺酮抑制剂的组合治疗
公开(公告)号：US20110123434A1
公开(公告)日：2011-05-26
申请号：US12595236
申请日：2008-04-08
申请人： Peter Lamb , David Matthews
发明人： Peter Lamb , David Matthews
IPC分类号： A61K51/00 , A61K31/635 , A61K31/498 , A61K31/4985 , A61K31/5377 , A61K31/551 , A61K39/395 , A61P35/00 , A61P35/02
CPC分类号： A61K31/337 , A61K31/436 , A61K31/497 , A61K31/498 , A61K31/4985 , A61K31/517 , A61K31/555 , A61K45/06 , A61K2300/00
摘要： The present invention provides methods of treating cancer by administering a compound of Formula I, optionally as a pharmaceutically acceptable salt, solvate and/or hydrate thereof, in combination with other cancer treatments.
摘要翻译：本发明提供了通过与其它癌症治疗组合施用式I化合物，任选地作为其药学上可接受的盐，溶剂合物和/或水合物来治疗癌症的方法。

7. 发明申请

US20080166359A1 Methods of using MEK inhibitors 有权
标题翻译：使用MEK抑制剂的方法
公开(公告)号：US20080166359A1
公开(公告)日：2008-07-10
申请号：US12002340
申请日：2007-12-14
申请人： Peter Lamb
发明人： Peter Lamb
IPC分类号： A61K39/395 , A61K31/397 , A61P35/00
CPC分类号： A61K31/397 , A61K31/4427 , A61K31/513
摘要： The present invention provides methods of treating cancer by administering a compound of Formula I, or a pharmaceutically acceptable salt or solvate thereof, in combination with other cancer treatments.
摘要翻译：本发明提供了通过与其它癌症治疗组合施用式I化合物或其药学上可接受的盐或溶剂合物来治疗癌症的方法。

8. 发明申请

US20120035212A1 (L)-Malate salt of N-(4-phenyl)-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide 有权
标题翻译：（L） - N-（4-苯基）-N' - （4-氟苯基）环丙烷-1,1-二甲酰胺的盐酸盐
公开(公告)号：US20120035212A1
公开(公告)日：2012-02-09
申请号：US13145054
申请日：2010-01-15
申请人： Adrian St. Clair Brown , Peter Lamb , William P. Gallagher
发明人： Adrian St. Clair Brown , Peter Lamb , William P. Gallagher
IPC分类号： A61K31/47 , A61P35/00 , C07D215/233
CPC分类号： C07D215/22 , C07D215/233
摘要： Disclosed are malate salts of N-(4-{[6,7-bis(methyloxy)-quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, including a (L)-malate salt, a (D)-malate salt, a (DL) malate salt, and mixtures thereof; and crystalline and amorphous forms of the malate salts. Also disclosed are pharmaceutical compositions comprising at least one malate salts of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl)-cyclopropane-1,1-dicarboxamide; and methods of treating cancer comprising administering at least one malate salt of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N′-(4-ffluorophenyl)cyclopropane-1,1-dicarboxamide.
摘要翻译：公开了N-（4 - {[6,7-双（甲氧基） - 喹啉-4-基]氧基}苯基）-N' - （4-氟苯基）环丙烷-1,1-二甲酰胺的苹果酸盐，包括（L） - 苹果酸盐，（D）苹果酸盐，（DL）苹果酸盐及其混合物; 和结晶和无定形形式的苹果酸盐。还公开了包含至少一种N-（4 - {[6,7-双（甲氧基）喹啉-4-基]氧基}苯基）-N' - （4-氟苯基） - 环丙烷-1 ，1-二甲酰胺; 和治疗癌症的方法包括给予N-（4 - {[6,7-双（甲氧基）喹啉-4-基]氧基}苯基）-N' - （4-氟苯基）环丙烷-1 ，1-二甲酰胺。

9. 发明授权

US07704995B2 Protein kinase modulators and methods of use 失效
标题翻译：蛋白激酶调节剂和使用方法
公开(公告)号：US07704995B2
公开(公告)日：2010-04-27
申请号：US10513081
申请日：2003-05-02
申请人： Chris A. Buhr , Tae-Gon Baik , Sunghoon Ma , Zerom Tesfai , Longcheng Wang , Erick Wang Co , Sergey Epshteyn , Abigail R Kennedy , Baili Chen , Larisa Dubenko , Neel Kumar Anand , Tsze H. Tsang , John M. Nuss , Csaba J Peto , Kenneth D. Rice , Mohamed Abdulkader Ibrahim , Kevin Luke Schnepp , Xian Shi , James William Leahy , Jeff Chen , Lisa Esther Dalrymple , Timothy Patrick Forsyth , Tai Phat Huynh , Grace Mann , Larry Wayne Mann , Craig Stacy Takeuchi , Peter Lamb , David J. Matthews , Nicole Miller
发明人： Chris A. Buhr , Tae-Gon Baik , Sunghoon Ma , Zerom Tesfai , Longcheng Wang , Erick Wang Co , Sergey Epshteyn , Abigail R Kennedy , Baili Chen , Larisa Dubenko , Neel Kumar Anand , Tsze H. Tsang , John M. Nuss , Csaba J Peto , Kenneth D. Rice , Mohamed Abdulkader Ibrahim , Kevin Luke Schnepp , Xian Shi , James William Leahy , Jeff Chen , Lisa Esther Dalrymple , Timothy Patrick Forsyth , Tai Phat Huynh , Grace Mann , Larry Wayne Mann , Craig Stacy Takeuchi , Peter Lamb , David J. Matthews , Nicole Miller
IPC分类号： C07D279/16 , C07D279/12 , C07D417/12 , C07D265/36 , C07D413/12 , C07D403/12 , C07D401/12 , C07D405/12 , C07D409/12 , C07D411/12 , C07D419/12 , C07D241/18 , C07D241/20 , A61K31/55 , A61K31/497 , A61K31/5355 , A61K31/541 , C07D305/12 , C07D307/79 , A61K31/44 , A61P35/00
CPC分类号： C07D241/26 , C07D401/04 , C07D401/10 , C07D401/12 , C07D403/04 , C07D403/10 , C07D403/14 , C07D405/04 , C07D405/12 , C07D413/04 , C07D413/12
摘要： This invention relates to compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion, and to pharmaceutical compositions containing such compounds. Even more specifically, the invention relates to compounds that inhibit, regulate and/or modulate kinases, particularly Checkpoint Kinases, even more particularly Checkpoint Kinase 1, or Chk1. Methods of therapeutically or prophylactically using the compounds and compositions to treat kinase-dependent diseases and conditions are also an aspect of the invention, and include methods of treating cancer, as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation, by administering effective amounts of such compounds.
摘要翻译：本发明涉及用于调节蛋白激酶酶活性以调节细胞活性如增殖，分化，程序性细胞死亡，迁移和化学侵蚀的化合物，以及含有这些化合物的药物组合物。更具体地，本发明涉及抑制，调节和/或调节激酶，特别是检查点激酶，甚至更特别是检查点激酶1或Chk1的化合物。治疗或预防性地使用化合物和组合物治疗激酶依赖性疾病和病症的方法也是本发明的一个方面，并且包括通过以下方法治疗癌症以及与不期望的血管生成和/或细胞增殖相关的其它疾病状态，施用有效量的这些化合物。

10. 发明申请

US20120302545A1 Method of Using PI3K and MEK Modulators 有权
标题翻译：使用PI3K和MEK调制器的方法
公开(公告)号：US20120302545A1
公开(公告)日：2012-11-29
申请号：US13568649
申请日：2012-08-07
申请人： Dana T. Aftab , A. Douglas Laird , Peter Lamb , Jean-Francois A. Martini
发明人： Dana T. Aftab , A. Douglas Laird , Peter Lamb , Jean-Francois A. Martini
IPC分类号： A61K31/498 , A61P35/02 , A61K31/5377 , A61P35/00 , A61K31/4985 , A61K31/551
CPC分类号： C07D487/04 , A61K31/498 , A61K31/519 , A61K45/06 , C07D241/44 , C07D295/135 , C07D401/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D409/12 , C07D417/12
摘要： The invention provides methods of treating cancer with a combination of compounds which inhibit kinases, more specifically MEK and PI3K.
摘要翻译：本发明提供了用抑制激酶，更具体地MEK和PI3K的化合物组合治疗癌症的方法。

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