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公开(公告)号：US08802864B2
公开(公告)日：2014-08-12
申请号：US13579040
申请日：2011-02-22
申请人： Nicholas D. Adams , Christopher Joseph Aquino , Amita M. Chaudhari , Jonathan M. Ghergurovich , Terence John Kiesow , Cynthia A. Parrish , Alexander Joseph Reif , Kenneth Wiggall
发明人： Nicholas D. Adams , Christopher Joseph Aquino , Amita M. Chaudhari , Jonathan M. Ghergurovich , Terence John Kiesow , Cynthia A. Parrish , Alexander Joseph Reif , Kenneth Wiggall
IPC分类号： C07D249/12 , A61K31/4196
CPC分类号： C07D403/14 , A61K31/397 , A61K31/4196 , C07D401/14 , C07D403/06 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要： This invention relates to the use of triazolone derivatives of Formula (I) for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of triazolones in the treatment of cancer.
摘要翻译： 本发明涉及式（I）的三唑酮衍生物用于调节，特别是抑制脂肪酸合酶（FAS）的活性或功能的用途。 合适地，本发明涉及三唑酮在治疗癌症中的用途。
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公开(公告)号：US20130172384A1
公开(公告)日：2013-07-04
申请号：US13824000
申请日：2011-09-15
申请人： Nicholas D. Adams , Christopher Joseph Aquino , Jonathan M. Ghergurovich , David Lee Musso , Cynthia A. Parrish
发明人： Nicholas D. Adams , Christopher Joseph Aquino , Jonathan M. Ghergurovich , David Lee Musso , Cynthia A. Parrish
IPC分类号： C07D471/04 , C07D413/14 , C07D405/14 , C07D401/14 , C07D403/06
CPC分类号： C07D471/04 , C07B2200/05 , C07D401/14 , C07D403/06 , C07D405/14 , C07D413/14
摘要： This invention relates to the use of triazolone and triazolethione derivatives for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of triazolones and triazolethiones in the treatment of cancer.
摘要翻译： 本发明涉及三唑酮和三唑硫酮衍生物用于调节，特别是抑制脂肪酸合酶（FAS）的活性或功能的用途。 合适地，本发明涉及三唑酮和三唑硫代乙酸在治疗癌症中的用途。
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公开(公告)号：US20100179143A1
公开(公告)日：2010-07-15
申请号：US12602333
申请日：2008-05-29
IPC分类号： A61K31/4375 , C07D471/04 , A61K31/496 , A61K31/5377 , A61P37/06 , A61P29/00 , A61P37/08 , A61P9/00 , A61P11/06 , A61P1/18 , A61P13/12 , A61P17/06 , A61P25/00 , A61P25/28 , A61P9/10 , A61P35/00
CPC分类号： C07D471/04
摘要： Invented is a method of inhibiting the activity/function of PI3 kinases using naphthyridine derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of naphthyridine derivatives.
摘要翻译： 本发明是使用萘啶衍生物抑制PI3激酶的活性/功能的方法。 还发明了一种治疗选自以下的一种或多种疾病状态的方法：自身免疫性疾病，炎性疾病，心血管疾病，神经变性疾病，变态反应，哮喘，胰腺炎，多器官功能衰竭，肾脏疾病，血小板聚集，癌症，精子活力，移植排斥反应， 通过施用萘啶衍生物的移植排斥和肺损伤。
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公开(公告)号：US20120165321A1
公开(公告)日：2012-06-28
申请号：US13411887
申请日：2012-03-05
申请人： Nicholas D. Adams , Joelle Lorraine Burgess , Michael Gerrard Darcy , Carla A. Donatelli , Steven David Knight , Kenneth Allen Newlander , Lance Ridgers , Martha A. Sarpong , Stanley J. Schmidt
发明人： Nicholas D. Adams , Joelle Lorraine Burgess , Michael Gerrard Darcy , Carla A. Donatelli , Steven David Knight , Kenneth Allen Newlander , Lance Ridgers , Martha A. Sarpong , Stanley J. Schmidt
IPC分类号： A61K31/4709 , C07D413/14 , A61K31/5377 , A61K31/496 , C07D471/04 , C07D498/04 , A61K31/5383 , C07D417/14 , A61K31/549 , A61P37/00 , A61P29/00 , A61P9/00 , A61P25/28 , A61P37/08 , A61P11/06 , A61P1/18 , A61P13/12 , A61P7/02 , A61P35/00 , A61P15/08 , A61P37/06 , A61P11/00 , A61P17/06 , A61P19/04 , A61P1/00 , A61P25/14 , A61P25/00 , A61P9/10 , A61P9/08 , A61P21/00 , A61P35/04 , A61P31/04 , A61P31/12 , A61P35/02 , C07D401/14
CPC分类号： C07D498/04 , A61K31/4709 , A61K31/496 , A61K31/5377 , A61K31/5383 , A61K31/549 , A61K45/06 , C07D285/24 , C07D401/04 , C07D401/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04
摘要： Invented is a method of inhibiting the activity/function of PI3 kinases using quinoline derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of quinoline derivatives.
摘要翻译： 本发明是使用喹啉衍生物抑制PI3激酶的活性/功能的方法。 还发明了一种治疗选自以下的一种或多种疾病状态的方法：自身免疫性疾病，炎性疾病，心血管疾病，神经变性疾病，变态反应，哮喘，胰腺炎，多器官功能衰竭，肾脏疾病，血小板聚集，癌症，精子活力，移植排斥反应， 通过给药喹啉衍生物的移植物排斥反应和肺损伤。
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公开(公告)号：US20100311736A1
公开(公告)日：2010-12-09
申请号：US12739176
申请日：2008-10-22
申请人： Nicholas D. Adams , Michael Gerard Darcy , Neil W. Johnson , Jiri Kasparec , Steven David Knight , Kenneth Allen Newlander , Xin Peng , Lance H. Ridgers
发明人： Nicholas D. Adams , Michael Gerard Darcy , Neil W. Johnson , Jiri Kasparec , Steven David Knight , Kenneth Allen Newlander , Xin Peng , Lance H. Ridgers
IPC分类号： A61K31/536 , A61K31/44 , C07D213/72 , A61K31/444 , C07D213/22 , A61K31/4439 , C07D401/02 , A61K31/5377 , C07D413/14 , A61K31/506 , C07D401/04 , A61K31/4709 , C07D413/02 , A61K31/498 , A61P35/00 , A61P37/06 , A61P29/00 , A61P9/00 , A61P25/00
CPC分类号： C07D213/76 , C07D401/04 , C07D401/14 , C07D405/04 , C07D409/04 , C07D413/04 , C07D413/14 , C07D417/04 , C07D471/04
摘要： Invented is a method of inhibiting the activity/function of PI3 kinases using pyridosulfonamide derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of pyridosulfonamide derivatives.
摘要翻译： 本发明是使用吡啶磺酰胺衍生物抑制PI3激酶的活性/功能的方法。 还发明了一种治疗选自以下的一种或多种疾病状态的方法：自身免疫性疾病，炎性疾病，心血管疾病，神经变性疾病，变态反应，哮喘，胰腺炎，多器官功能衰竭，肾脏疾病，血小板聚集，癌症，精子活力，移植排斥反应， 通过施用吡啶磺酰胺衍生物的移植排斥和肺损伤。
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公开(公告)号：US20100168100A1
公开(公告)日：2010-07-01
申请号：US12600752
申请日：2008-05-16
IPC分类号： A61K31/5377 , C07D215/12 , C07D471/04 , C07D401/14 , C07D413/14 , A61K31/4709 , A61K31/47 , A61K31/497 , A61P35/02 , A61P35/00
CPC分类号： A61K31/4709 , A61K31/496 , A61K31/5377 , A61K31/5383 , A61K31/549 , A61K45/06 , C07D285/24 , C07D401/04 , C07D401/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04 , C07D498/04
摘要： Invented is a method of inhibiting the activity/function of PI3 kinases using quinoline derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of quinoline derivatives.
摘要翻译： 本发明是使用喹啉衍生物抑制PI3激酶的活性/功能的方法。 还发明了一种治疗选自以下的一种或多种疾病状态的方法：自身免疫性疾病，炎性疾病，心血管疾病，神经变性疾病，变态反应，哮喘，胰腺炎，多器官功能衰竭，肾脏疾病，血小板聚集，癌症，精子活力，移植排斥反应， 通过给药喹啉衍生物的移植物排斥反应和肺损伤。
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公开(公告)号：US20080255115A1
公开(公告)日：2008-10-16
申请号：US11844404
申请日：2007-08-24
IPC分类号： C07D401/14 , A61K31/4709 , A61K31/497 , A61K31/501 , C07D413/14 , A61K31/5377 , A61P35/00
CPC分类号： C07D417/14
摘要： Invented is a method of inhibiting the activity/function of PI3 kinases using thiazolidinedione derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of thiazolidinedione derivatives.
摘要翻译： 本发明是使用噻唑烷二酮衍生物抑制PI3激酶的活性/功能的方法。 还发明了一种治疗选自以下的一种或多种疾病状态的方法：自身免疫性疾病，炎性疾病，心血管疾病，神经变性疾病，变态反应，哮喘，胰腺炎，多器官功能衰竭，肾脏疾病，血小板聚集，癌症，精子活力，移植排斥反应， 通过施用噻唑烷二酮衍生物的移植排斥和肺损伤。
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公开(公告)号：US08404837B2
公开(公告)日：2013-03-26
申请号：US12600745
申请日：2008-05-16
申请人： Nicholas D. Adams , Joelle Lorraine Burgess , Michael Gerard Darcy , Carla A. Donatelli , Steven David Knight , Kenneth Allen Newlander , Lance Ridgers , Martha A. Sarpong , Stanley J. Schmidt
发明人： Nicholas D. Adams , Joelle Lorraine Burgess , Michael Gerard Darcy , Carla A. Donatelli , Steven David Knight , Kenneth Allen Newlander , Lance Ridgers , Martha A. Sarpong , Stanley J. Schmidt
IPC分类号： C07D401/14 , C07D413/14 , C07D498/04
CPC分类号： C07D498/04 , A61K31/4709 , A61K31/496 , A61K31/5377 , A61K31/5383 , A61K31/549 , A61K45/06 , C07D285/24 , C07D401/04 , C07D401/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04
摘要： Invented is a method of inhibiting the activity/function of PI3 kinases using quinoline derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of quinoline derivatives.
摘要翻译： 本发明是使用喹啉衍生物抑制PI3激酶的活性/功能的方法。 还发明了一种治疗选自以下的一种或多种疾病状态的方法：自身免疫性疾病，炎性疾病，心血管疾病，神经变性疾病，变态反应，哮喘，胰腺炎，多器官功能衰竭，肾脏疾病，血小板聚集，癌症，精子活力，移植排斥反应， 通过给药喹啉衍生物的移植物排斥反应和肺损伤。
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公开(公告)号：US20100179144A1
公开(公告)日：2010-07-15
申请号：US12664496
申请日：2008-06-12
申请人： Nicholas D. Adams , Joelle Lorraine Burgess , Michael Gerard Darcy , Steven David Knight , Kenneth Allen Newlander , Lance H. Ridgers , Stanley J. Schmidt
发明人： Nicholas D. Adams , Joelle Lorraine Burgess , Michael Gerard Darcy , Steven David Knight , Kenneth Allen Newlander , Lance H. Ridgers , Stanley J. Schmidt
IPC分类号： A61K31/5377 , C07D401/14 , A61K31/517 , C07D413/14 , A61K31/496 , C07D403/14 , A61K31/501 , A61P35/00
CPC分类号： A61K31/5377 , A61K31/517 , C07D401/04 , C07D401/14 , C07D471/04
摘要： Invented is a method of inhibiting the activity/function of PI3 kinases using quinazoline derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of quinazoline derivatives.
摘要翻译： 发明是使用喹唑啉衍生物抑制PI3激酶的活性/功能的方法。 还发明了一种治疗选自以下的一种或多种疾病状态的方法：自身免疫性疾病，炎性疾病，心血管疾病，神经变性疾病，变态反应，哮喘，胰腺炎，多器官功能衰竭，肾脏疾病，血小板聚集，癌症，精子活力，移植排斥反应， 通过施用喹唑啉衍生物的移植物排斥和肺损伤。
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公开(公告)号：US20080300239A1
公开(公告)日：2008-12-04
申请号：US12121891
申请日：2008-05-16
申请人： Nicholas D. Adams , Joelle Lorraine Burgess , Michael Gerrard Darcy , Carla A. Donatelli , Steven David Knight , Kenneth Allen Newlander , Lance Ridgers , Martha A. Sarpong , Stanley J. Schmidt
发明人： Nicholas D. Adams , Joelle Lorraine Burgess , Michael Gerrard Darcy , Carla A. Donatelli , Steven David Knight , Kenneth Allen Newlander , Lance Ridgers , Martha A. Sarpong , Stanley J. Schmidt
IPC分类号： A61K31/4709 , C07D401/14 , C07D413/14 , A61K31/5383 , A61P35/00 , A61K31/549 , A61K31/5377 , C07D285/24
CPC分类号： C07D498/04 , A61K31/4709 , A61K31/496 , A61K31/5377 , A61K31/5383 , A61K31/549 , A61K45/06 , C07D285/24 , C07D401/04 , C07D401/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04
摘要： Invented is a method of inhibiting the activity/function of PI3 kinases using quinoline derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of quinoline derivatives.
摘要翻译： 本发明是使用喹啉衍生物抑制PI3激酶的活性/功能的方法。 还发明了一种治疗选自以下的一种或多种疾病状态的方法：自身免疫性疾病，炎性疾病，心血管疾病，神经变性疾病，变态反应，哮喘，胰腺炎，多器官功能衰竭，肾脏疾病，血小板聚集，癌症，精子活力，移植排斥反应， 通过给药喹啉衍生物的移植物排斥反应和肺损伤。
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