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公开(公告)号：US08178570B2
公开(公告)日：2012-05-15
申请号：US10552424
申请日：2004-04-08
申请人： Jeff Chen , Lisa Esther Dalrymple , Sergey Epshteyn , Timothy Patrick Forsyth , Tai Phat Huynh , James William Leahy , Brian Hugh Ridgway , Grace Mann , Larry W. Mann , Craig Stacy Takeuchi , Joan C. Sangalang
发明人： Jeff Chen , Lisa Esther Dalrymple , Sergey Epshteyn , Timothy Patrick Forsyth , Tai Phat Huynh , James William Leahy , Brian Hugh Ridgway , Grace Mann , Larry W. Mann , Craig Stacy Takeuchi , Joan C. Sangalang
IPC分类号： A01N43/64 , A01N43/54 , A61K31/41 , C07D239/42 , C07D401/04 , C07D249/08
CPC分类号： C07D401/04 , A61K31/4439 , A61K31/506
摘要： The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinases, particularly Tie-2. Methods of using the compounds and pharmaceutical compositions thereof to treat kinase-dependent diseases and conditions are also an aspect of the invention.
摘要翻译： 本发明提供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。 本发明的化合物抑制，调节和/或调节激酶，特别是Tie-2。 使用化合物及其药物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。
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公开(公告)号：US20080249079A1
公开(公告)日：2008-10-09
申请号：US11722719
申请日：2005-12-28
申请人： Jeff Chen , Lisa Esther Dalrymple Meyr , Sergey Epshteyn , Timothy Patrick Forsyth , Tai Phat Huynh , Mohamed Abdulkader Ibrahim , James W. Leahy , Gary Lee Lewis , Grace Mann , Larry W. Mann , Robin Tammie Noguchi , Brian Hugh Ridgway , Joan Cruz Sangalang , Kevin Luke Schnepp , Xian Shi , Craig Stacy Takeuchi , Matthew Alan Williams , John Nuss , Atwood K. Cheung
发明人： Jeff Chen , Lisa Esther Dalrymple Meyr , Sergey Epshteyn , Timothy Patrick Forsyth , Tai Phat Huynh , Mohamed Abdulkader Ibrahim , James W. Leahy , Gary Lee Lewis , Grace Mann , Larry W. Mann , Robin Tammie Noguchi , Brian Hugh Ridgway , Joan Cruz Sangalang , Kevin Luke Schnepp , Xian Shi , Craig Stacy Takeuchi , Matthew Alan Williams , John Nuss , Atwood K. Cheung
IPC分类号： A61K31/506 , C07D413/14 , A61K31/5377 , A61K31/519 , A61P35/00 , C07D403/14 , C07D403/12
CPC分类号： C07D413/14 , C07D239/48 , C07D401/14 , C07D403/12 , C07D405/14 , C07D413/04 , C07D413/12 , C07D417/14 , C07D487/04
摘要： The invention provides compounds and methods for inhibition of kinases, more specifically IGF 1 R kinases. The invention also provides compounds and methods for inhibition of wildtype Abl. The invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinase receptor signal transduction pathways related to the changes in cellular activities as mentioned above, and the invention includes compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. A compound of formula (I), or a pharmaceutically acceptable salt, hydrate, or prodrug thereof, wherein, V is NR1R1a, or O—R1, wherein X is H, halo, C1-C6 alkyl, NO2, mono-, di-, or tri-halo substituted methyl, NR13R,14. C(O)O—C1-C6 alkyl, or N(R13)—C(O)—C1-C6 alkyl; Y is H, halo, OH, C1-C6 alkyl, C0-C6alkyl-NR,15R16, NR15R,6, C1-C6 alkoxy, —N(R13)—(CH2)n-NR15R16, —C(O)O—C1-C6 alkyl, —O—(CH2)n—NR15R16, —C(O)—C1-C6 alkyl, —C0-C6-alkyl-R21, —O—R21, —C(O)—R21, —O—(CH2)n—R21, —C(O)—NR13R14, —C(O)—N(R13)-aryl, —C(O)—N(R13)(CH2)n—NR15R16, —C(O)—N(R13)—(CH2)n-aryl —C(O)—N(R13)—(CH2)n-heterocyclyl; or X and Y together with the atoms to which they are attached form a 4-7 membered heterocyclyl or heteroaryl group containing one or two heteroatoms independently selected from O, N, and S. Z is H, NR2R3, —S—R2a, or —O—R2a
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公开(公告)号：US08211929B2
公开(公告)日：2012-07-03
申请号：US11722719
申请日：2005-12-28
申请人： Jeff Chen , Lisa Esther Dalrymple Meyr , Sergey Epshteyn , Timothy Patrick Forsyth , Tai Phat Huynh , Mohamed Abdulkader Ibrahim , James W. Leahy , Gary Lee Lewis , Grace Mann , Larry W. Mann , Robin Tammie Noguchi , Brian Hugh Ridgway , Joan Cruz Sangalang , Kevin Luke Schnepp , Xian Shi , Craig Stacy Takeuchi , Matthew Alan Williams , John Nuss , Atwood K. Cheung
发明人： Jeff Chen , Lisa Esther Dalrymple Meyr , Sergey Epshteyn , Timothy Patrick Forsyth , Tai Phat Huynh , Mohamed Abdulkader Ibrahim , James W. Leahy , Gary Lee Lewis , Grace Mann , Larry W. Mann , Robin Tammie Noguchi , Brian Hugh Ridgway , Joan Cruz Sangalang , Kevin Luke Schnepp , Xian Shi , Craig Stacy Takeuchi , Matthew Alan Williams , John Nuss , Atwood K. Cheung
IPC分类号： A01N43/56 , A61K31/415 , C07D239/02 , C07D231/00
CPC分类号： C07D413/14 , C07D239/48 , C07D401/14 , C07D403/12 , C07D405/14 , C07D413/04 , C07D413/12 , C07D417/14 , C07D487/04
摘要： The invention provides compounds and methods for inhibition of kinases, more specifically IGF 1 R kinases. The invention also provides compounds and methods for inhibition of wildtype Abl. The invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinase receptor signal transduction pathways related to the changes in cellular activities as mentioned above, and the invention includes compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. A compound of formula (I), or a pharmaceutically acceptable salt, hydrate, or prodrug thereof, wherein, V is NR1R1a, or O—R1, wherein X is H, halo, C1-C6 alkyl, NO2, mono-, di-, or tri-halo substituted methyl, NR13R,14. C(O)O—C1-C6 alkyl, or N(R13)—C(O)—C1-C6 alkyl; Y is H, halo, OH, C1-C6 alkyl, C0-C6alkyl-NR,15R16, NR15R,6, C1-C6 alkoxy, —N(R13)—(CH2)n-NR15R16, —C(O)O—C1-C6 alkyl, —O—(CH2)n—NR15R16, —C(O)—C1-C6 alkyl, —C0-C6-alkyl-R21, —O—R21, —C(O)—R21, —O—(CH2)n—R21, —C(O)—NR13R14, —C(O)—N(R13)-aryl, —C(O)—N(R13)(CH2)n—NR15R16, —C(O)—N(R13)—(CH2)n-aryl —C(O)—N(R13)—(CH2)n-heterocyclyl; or X and Y together with the atoms to which they are attached form a 4-7 membered heterocyclyl or heteroaryl group containing one or two heteroatoms independently selected from O, N, and S. Z is H, NR2R3, —S—R2a, or —O—R2a
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公开(公告)号：US08222263B2
公开(公告)日：2012-07-17
申请号：US12049225
申请日：2008-03-14
申请人： Suleyman Bahceci , William Bajjalieh , Jeff Chen , Sergey Epshteyn , Timothy Patrick Forsyth , Tai Phat Huynh , Byung Gyu Kim , James W. Leahy , Matthew Sangyup Lee , Gary L. Lewis , Morrison B. Mac , Grace Mann , Charles K. Marlowe , Brian Hugh Ridgway , Joan C. Sangalang , Xian Shi , Craig Stacy Takeuchi , Yong Wang
发明人： Suleyman Bahceci , William Bajjalieh , Jeff Chen , Sergey Epshteyn , Timothy Patrick Forsyth , Tai Phat Huynh , Byung Gyu Kim , James W. Leahy , Matthew Sangyup Lee , Gary L. Lewis , Morrison B. Mac , Grace Mann , Charles K. Marlowe , Brian Hugh Ridgway , Joan C. Sangalang , Xian Shi , Craig Stacy Takeuchi , Yong Wang
IPC分类号： A61K31/517 , A01N43/54
CPC分类号： C07D239/42 , C07D239/70 , C07D239/84 , C07D239/95 , C07D401/04 , C07D403/12
摘要： The present invention is directed to a compound of Formula I or a single isomer thereof; where the compound is optionally as a pharmaceutically acceptable salt, hydrate, solvate or combination thereof, in addition to methods of preparing a Compound of Formula I, and methods of using a Compound of Formula I to treat cancer.
摘要翻译： 本发明涉及式I化合物或其单一异构体; 其中除了制备式I化合物的方法之外，化合物任选为其药学上可接受的盐，水合物，溶剂合物或其组合，以及使用式I化合物治疗癌症的方法。
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公开(公告)号：US20120238570A1
公开(公告)日：2012-09-20
申请号：US13487559
申请日：2012-06-04
申请人： Suleyman Bahceci , William Bajjalieh , Jeff Chen , Sergey Epshteyn , Timothy Patrick Forsyth , Tai Phat Huynh , Byung Gyu Kim , James W. Leahy , Matthew Sangyup Lee , Gary L. Lewis , Morrison B. Mac , Grace Mann , Charles K. Marlowe , Brian Hugh Ridgway , Joan C. Sangalang , Xian Shi , Craig Stacy Takeuchi , Yong Wang
发明人： Suleyman Bahceci , William Bajjalieh , Jeff Chen , Sergey Epshteyn , Timothy Patrick Forsyth , Tai Phat Huynh , Byung Gyu Kim , James W. Leahy , Matthew Sangyup Lee , Gary L. Lewis , Morrison B. Mac , Grace Mann , Charles K. Marlowe , Brian Hugh Ridgway , Joan C. Sangalang , Xian Shi , Craig Stacy Takeuchi , Yong Wang
IPC分类号： A61K31/517 , A61K31/519 , C07D413/04 , A61P35/00 , C07D239/84 , C07D471/04 , C07D403/12 , A61K31/5377 , C07D239/70
CPC分类号： C07D239/42 , C07D239/70 , C07D239/84 , C07D239/95 , C07D401/04 , C07D403/12
摘要： The present invention is directed to a compound of Formula I or a single isomer thereof; where the compound is optionally as a pharmaceutically acceptable salt, hydrate, solvate or combination thereof, in addition to methods of preparing a Compound of Formula I, and methods of using a Compound of Formula I to treat cancer.
摘要翻译： 本发明涉及式I化合物或其单一异构体; 其中除了制备式I化合物的方法之外，化合物任选为其药学上可接受的盐，水合物，溶剂合物或其组合，以及使用式I化合物治疗癌症的方法。
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公开(公告)号：US08754092B2
公开(公告)日：2014-06-17
申请号：US13487594
申请日：2012-06-04
申请人： Suleyman Bahceci , William Bajjalieh , Jeff Chen , Sergey Epshteyn , Timothy Patrick Forsyth , Tai Phat Huynh , Byung Gyu Kim , James W. Leahy , Matthew Sangyup Lee , Gary L. Lewis , Morrison B. Mac , Grace Mann , Charles K. Marlowe , Brian Hugh Ridgway , Joan C. Sangalang , Xian Shi , Craig Stacy Takeuchi , Yong Wang
发明人： Suleyman Bahceci , William Bajjalieh , Jeff Chen , Sergey Epshteyn , Timothy Patrick Forsyth , Tai Phat Huynh , Byung Gyu Kim , James W. Leahy , Matthew Sangyup Lee , Gary L. Lewis , Morrison B. Mac , Grace Mann , Charles K. Marlowe , Brian Hugh Ridgway , Joan C. Sangalang , Xian Shi , Craig Stacy Takeuchi , Yong Wang
IPC分类号： A01N43/54 , A61K31/517 , C07D239/72 , C07D401/00
CPC分类号： C07D239/42 , C07D239/70 , C07D239/84 , C07D239/95 , C07D401/04 , C07D403/12
摘要： The present invention is directed to a compound of Formula I or a single isomer thereof; where the compound is optionally as a pharmaceutically acceptable salt, hydrate, solvate or combination thereof, in addition to methods of preparing a Compound of Formula I, and methods of using a Compound of Formula I to treat cancer.
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公开(公告)号：US20090105211A1
公开(公告)日：2009-04-23
申请号：US12049225
申请日：2008-03-14
申请人： Suleyman Bahceci , William Bajjalieh , Jeff Chen , Sergey Epshteyn , Timothy Patrick Forsyth , Tai Phat Huynh , Byung Gyu Kim , James W. Leahy , Matthew Sangyup Lee , Gary L. Lewis , Morrison B. Mac , Grace Mann , Charles K. Marlowe , Brian Hugh Ridgway , Joan C. Sangalang , Xian Shi , Craig Stacy Takeuchi , Yong Wang
发明人： Suleyman Bahceci , William Bajjalieh , Jeff Chen , Sergey Epshteyn , Timothy Patrick Forsyth , Tai Phat Huynh , Byung Gyu Kim , James W. Leahy , Matthew Sangyup Lee , Gary L. Lewis , Morrison B. Mac , Grace Mann , Charles K. Marlowe , Brian Hugh Ridgway , Joan C. Sangalang , Xian Shi , Craig Stacy Takeuchi , Yong Wang
IPC分类号： C07D239/84 , C07D413/12 , A61K31/517 , A61K31/5377 , A61K31/496 , A61K31/553 , A61K31/55 , C07D401/12 , C07D403/12 , A61P35/00 , C07D401/14
CPC分类号： C07D239/42 , C07D239/70 , C07D239/84 , C07D239/95 , C07D401/04 , C07D403/12
摘要： The present invention is directed to a compound of Formula I or a single isomer thereof; where the compound is optionally as a pharmaceutically acceptable salt, hydrate, solvate or combination thereof, in addition to methods of preparing a Compound of Formula I, and methods of using a Compound of Formula I to treat cancer.
摘要翻译： 本发明涉及式I化合物或其单一异构体; 其中除了制备式I化合物的方法之外，化合物任选为其药学上可接受的盐，水合物，溶剂合物或其组合，以及使用式I化合物治疗癌症的方法。
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公开(公告)号：US08796294B2
公开(公告)日：2014-08-05
申请号：US13487559
申请日：2012-06-04
申请人： Suleyman Bahceci , William Bajjalieh , Jeff Chen , Sergey Epshteyn , Timothy Patrick Forsyth , Tai Phat Huynh , Byung Gyu Kim , James W. Leahy , Matthew Sangyup Lee , Gary L. Lewis , Morrison B. Mac , Grace Mann , Charles K. Marlowe , Brian Hugh Ridgway , Joan C. Sangalang , Xian Shi , Craig Stacy Takeuchi , Yong Wang
发明人： Suleyman Bahceci , William Bajjalieh , Jeff Chen , Sergey Epshteyn , Timothy Patrick Forsyth , Tai Phat Huynh , Byung Gyu Kim , James W. Leahy , Matthew Sangyup Lee , Gary L. Lewis , Morrison B. Mac , Grace Mann , Charles K. Marlowe , Brian Hugh Ridgway , Joan C. Sangalang , Xian Shi , Craig Stacy Takeuchi , Yong Wang
IPC分类号： A01N43/54 , A61K31/517 , C07D239/72 , C07D401/00
CPC分类号： C07D239/42 , C07D239/70 , C07D239/84 , C07D239/95 , C07D401/04 , C07D403/12
摘要： The present invention is directed to a compound of Formula I or a single isomer thereof; where the compound is optionally as a pharmaceutically acceptable salt, hydrate, solvate or combination thereof, in addition to methods of preparing a Compound of Formula I, and methods of using a Compound of Formula I to treat cancer.
摘要翻译： 本发明涉及式I化合物或其单一异构体; 其中除了制备式I化合物的方法之外，化合物任选为其药学上可接受的盐，水合物，溶剂合物或其组合，以及使用式I化合物治疗癌症的方法。
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公开(公告)号：US20120245139A1
公开(公告)日：2012-09-27
申请号：US13487594
申请日：2012-06-04
申请人： Suleyman Bahceci , William Bajjalieh , Jeff Chen , Sergey Epshteyn , Timothy Patrick Forsyth , Tai Phat Huynh , Byung Gyu Kim , James W. Leahy , Matthew Sangyup Lee , Gary L. Lewis , Morrison B. Mac , Grace Mann , Charles K. Marlowe , Brian Hugh Ridgway , Joan C. Sangalang , Xian Shi , Craig Stacy Takeuchi , Yong Wang
发明人： Suleyman Bahceci , William Bajjalieh , Jeff Chen , Sergey Epshteyn , Timothy Patrick Forsyth , Tai Phat Huynh , Byung Gyu Kim , James W. Leahy , Matthew Sangyup Lee , Gary L. Lewis , Morrison B. Mac , Grace Mann , Charles K. Marlowe , Brian Hugh Ridgway , Joan C. Sangalang , Xian Shi , Craig Stacy Takeuchi , Yong Wang
IPC分类号： A61K31/517 , A61P35/00 , A61K31/55 , A61K31/519 , A61K31/5377 , A61K31/553
CPC分类号： C07D239/42 , C07D239/70 , C07D239/84 , C07D239/95 , C07D401/04 , C07D403/12
摘要： The present invention is directed to a compound of Formula I or a single isomer thereof; where the compound is optionally as a pharmaceutically acceptable salt, hydrate, solvate or combination thereof, in addition to methods of preparing a Compound of Formula I, and methods of using a Compound of Formula I to treat cancer.
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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。
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