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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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公开(公告)号：US20070293507A1
公开(公告)日：2007-12-20
申请号：US11575411
申请日：2005-09-15
申请人： Tae-Gon Baik , Chris Buhr , Sunghoon Ma , John Nuss , Zerom Tesfai , Longcheng Wang , Bryan Yeung
发明人： Tae-Gon Baik , Chris Buhr , Sunghoon Ma , John Nuss , Zerom Tesfai , Longcheng Wang , Bryan Yeung
IPC分类号： A61K31/4184 , A61K31/415 , A61K31/4439 , A61K31/496 , C07D231/12 , C07D401/04 , C07D403/04 , C07D403/10 , C07D403/14
CPC分类号： C07D403/04 , C07D231/12 , C07D401/04 , C07D405/04 , C07D409/04
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. 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。 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：US20130165440A1
公开(公告)日：2013-06-27
申请号：US13821435
申请日：2011-09-13
IPC分类号： C07D237/34 , C07D403/10 , C07D409/10 , C07D215/44 , C07D409/04 , C07D403/12 , C07D413/12 , C07D417/10 , C07D471/04
CPC分类号： C07D409/04 , C07D217/22 , C07D237/34 , C07D403/10 , C07D405/04 , C07D417/10 , C07D471/04
摘要： JAK1 inhibitors of structural formula (I), wherein Ar1, Ar2, Q, W, X, Y, and Z are defined in the specification, pharmaceutically acceptable salts thereof, compositions thereof, and use of the compounds and compositions for treating diseases. The invention also comprises use of the compounds in and for the manufacture of medicaments, particularly for treating diseases.
摘要翻译： 其中Ar1，Ar2，Q，W，X，Y和Z的结构式（I）的JAK1抑制剂在本说明书中定义，其药学上可接受的盐，其组合物，以及用于治疗疾病的化合物和组合物的用途。 本发明还包括在化合物中和用于制备药物中的用途，特别是用于治疗疾病。
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公开(公告)号：US08710038B2
公开(公告)日：2014-04-29
申请号：US11575411
申请日：2005-09-15
申请人： Tae-Gon Baik , Chris A. Buhr , Sunghoon Ma , John M. Nuss , Zerom Tesfai , Longcheng Wang , Bryan K. S. Yeung
发明人： Tae-Gon Baik , Chris A. Buhr , Sunghoon Ma , John M. Nuss , Zerom Tesfai , Longcheng Wang , Bryan K. S. Yeung
IPC分类号： C07D403/00 , A01N43/00 , A61K31/33
CPC分类号： C07D403/04 , C07D231/12 , C07D401/04 , C07D405/04 , C07D409/04
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. 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。 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：US20110207712A1
公开(公告)日：2011-08-25
申请号：US13096942
申请日：2011-04-28
申请人： William Bajjalieh , Lynne Canne Bannen , S. David Brown , Patrick Kearney , Morrison Mac , Charles K. Marlowe , John M. Nuss , Zerom Tesfai , Yong Wang , Wei Xu
发明人： William Bajjalieh , Lynne Canne Bannen , S. David Brown , Patrick Kearney , Morrison Mac , Charles K. Marlowe , John M. Nuss , Zerom Tesfai , Yong Wang , Wei Xu
IPC分类号： C07D403/12 , A61K31/498 , C07D487/04 , C07D241/54 , A61K31/4985 , C07D413/12 , C07D401/12 , A61P35/00
CPC分类号： C07D401/12 , C07D241/44 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , Y02P20/55
摘要： The present invention comprises small molecule inhibitors of phosphatidylinositol 3-kinase (PI3K), which is associated with a number of malignancies such as ovarian cancer, cervical cancer, breast cancer, colon cancer, rectal cancer, and glioblastomas, among others. Accordingly, the compounds of the present invention are useful for treating, preventing, and/or inhibiting these diseases.
摘要翻译： 本发明包括与许多恶性肿瘤如卵巢癌，宫颈癌，乳腺癌，结肠癌，直肠癌和成胶质细胞瘤等相关的磷脂酰肌醇3-激酶（PI3K）的小分子抑制剂。 因此，本发明的化合物可用于治疗，预防和/或抑制这些疾病。
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公开(公告)号：US20060211709A1
公开(公告)日：2006-09-21
申请号：US10513081
申请日：2003-05-02
申请人： Chris Buhr , Tae-Gon Baik , Sunghoon Ma , Zerom Tesfai , Longcheng Wang , Erick Co , Sergey Epshteyn , Abigail Kennedy , Baili Chen , Larisa Dubenko , Neel Anand , Tsze Tsang , John Nuss , Csabaj Peto , Kenneth Rice , Mohamed Ibrahim , Xian Shi , James Leahy , Jeff Chen , Lisa Dalrymple , Timothy Forsyth , Tai Huynh , Grace Mann , Larry Mann , Craig Takeuchi
发明人： Chris Buhr , Tae-Gon Baik , Sunghoon Ma , Zerom Tesfai , Longcheng Wang , Erick Co , Sergey Epshteyn , Abigail Kennedy , Baili Chen , Larisa Dubenko , Neel Anand , Tsze Tsang , John Nuss , Csabaj Peto , Kenneth Rice , Mohamed Ibrahim , Xian Shi , James Leahy , Jeff Chen , Lisa Dalrymple , Timothy Forsyth , Tai Huynh , Grace Mann , Larry Mann , Craig Takeuchi
IPC分类号： A61K31/497 , C07D403/02
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： Substituted aryl 1,4-pyrazine derivatives and their use in treating anxiety disorders, depression and stress related disorders are disclosed.
摘要翻译： 公开了取代的芳基1,4-吡嗪衍生物及其在治疗焦虑症，抑郁症和应激相关疾病中的用途。
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公开(公告)号：US08889664B2
公开(公告)日：2014-11-18
申请号：US13096942
申请日：2011-04-28
申请人： William Bajjalieh , Lynne Canne Bannen , S. David Brown , Patrick Kearney , Morrison Mac , Charles K. Marlowe , John M. Nuss , Zerom Tesfai , Yong Wang , Wei Xu
发明人： William Bajjalieh , Lynne Canne Bannen , S. David Brown , Patrick Kearney , Morrison Mac , Charles K. Marlowe , John M. Nuss , Zerom Tesfai , Yong Wang , Wei Xu
IPC分类号： C07D403/12 , A61K31/498 , C07D487/04 , C07D241/54 , A61K31/4985 , C07D413/12 , C07D401/12 , A61P35/00 , C07D417/12 , C07D409/12 , C07D241/44
CPC分类号： C07D401/12 , C07D241/44 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , Y02P20/55
摘要： The present invention comprises small molecule inhibitors of phosphatidylinositol 3-kinase (PI3K), which is associated with a number of malignancies such as ovarian cancer, cervical cancer, breast cancer, colon cancer, rectal cancer, and glioblastomas, among others. Accordingly, the compounds of the present invention are useful for treating, preventing, and/or inhibiting these diseases.
摘要翻译： 本发明包括与许多恶性肿瘤如卵巢癌，宫颈癌，乳腺癌，结肠癌，直肠癌和成胶质细胞瘤等相关的磷脂酰肌醇3-激酶（PI3K）的小分子抑制剂。 因此，本发明的化合物可用于治疗，预防和/或抑制这些疾病。
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公开(公告)号：US07989622B2
公开(公告)日：2011-08-02
申请号：US11988862
申请日：2006-10-09
申请人： William Bajjalieh , Lynne Canne Bannen , S. David Brown , Patrick Kearney , Morrison B. Mac , Charles K. Marlowe , John M. Nuss , Zerom Tesfai , Yong Wang , Wei Xu
发明人： William Bajjalieh , Lynne Canne Bannen , S. David Brown , Patrick Kearney , Morrison B. Mac , Charles K. Marlowe , John M. Nuss , Zerom Tesfai , Yong Wang , Wei Xu
IPC分类号： A61K31/4985 , A61K31/498 , C07D241/36 , C07D403/14 , C07D471/04 , A61P35/02 , A61P35/00
CPC分类号： C07D401/12 , C07D241/44 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , Y02P20/55
摘要： The present invention comprises small molecule inhibitors of phosphatidylinositol 3-kinase (PI3K), which is associated with a number of malignancies such as ovarian cancer, cervical cancer, breast cancer, colon cancer, rectal cancer, and glioblastomas, among others. Accordingly, the compounds of the present invention are useful for treating, preventing, and/or inhibiting these diseases.
摘要翻译： 本发明包括与许多恶性肿瘤如卵巢癌，宫颈癌，乳腺癌，结肠癌，直肠癌和成胶质细胞瘤等相关的磷脂酰肌醇3-激酶（PI3K）的小分子抑制剂。 因此，本发明的化合物可用于治疗，预防和/或抑制这些疾病。
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公开(公告)号：US20100087440A1
公开(公告)日：2010-04-08
申请号：US11988862
申请日：2006-10-09
申请人： William Bajjalieh , Lynne Canne Bannen , S. David Brown , Patrick Kearney , Morrison B. Mac , Charles K. Marlowe , John M. Nuss , Zerom Tesfai , Yong Wang , Wei Xu
发明人： William Bajjalieh , Lynne Canne Bannen , S. David Brown , Patrick Kearney , Morrison B. Mac , Charles K. Marlowe , John M. Nuss , Zerom Tesfai , Yong Wang , Wei Xu
IPC分类号： A61K31/4985 , C07D241/36 , C07D403/14 , C07D471/04 , A61K31/498 , A61P35/02 , A61P35/00
CPC分类号： C07D401/12 , C07D241/44 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , Y02P20/55
摘要： The present invention comprises small molecule inhibitors of phosphatidylinositol 3-kinase (PI3K), which is associated with a number of malignancies such as ovarian cancer, cervical cancer, breast cancer, colon cancer, rectal cancer, and glioblastomas, among others. Accordingly, the compounds of the present invention are useful for treating, preventing, and/or inhibiting these diseases.
摘要翻译： 本发明包括与许多恶性肿瘤如卵巢癌，宫颈癌，乳腺癌，结肠癌，直肠癌和成胶质细胞瘤等相关的磷脂酰肌醇3-激酶（PI3K）的小分子抑制剂。 因此，本发明的化合物可用于治疗，预防和/或抑制这些疾病。
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