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公开(公告)号：US20160304519A1
公开(公告)日：2016-10-20
申请号：US15197445
申请日：2016-06-29
发明人： James F. Blake , Adam Cook , John Gaudino , Indrani W. Gunawardana , Erik James Hicken , Kevin W. Hunt , Michael Lyon , Andrew T. Metcalf , Peter J. Mohr , David A. Moreno , Brad Newhouse , Li Ren , Jacob Schwarz , Huifen Chen , Lewis Gazzard , Jane Schmidt , Steve Do
IPC分类号： C07D471/04 , A61K31/5377 , A61K31/55 , A61K31/444 , C07D487/04 , C07D519/00 , A61K45/06 , A61K31/506
CPC分类号： C07D471/04 , A61K31/444 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D487/04 , C07D519/00
摘要： Compounds of Formula I or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such diseases, or associated pathological conditions are disclosed.
摘要翻译： 提供式I化合物或其立体异构体，互变异构体或其药学上可接受的盐，其可用于治疗疾病。 公开了使用式I化合物或其立体异构体，互变异构体或其药学上可接受的盐在体外，原位和体内诊断，预防或治疗这些疾病或相关病理状况的方法。
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公开(公告)号：US09670208B2
公开(公告)日：2017-06-06
申请号：US15197445
申请日：2016-06-29
发明人： James F. Blake , Adam Cook , John Gaudino , Indrani W. Gunawardana , Erik James Hicken , Kevin W. Hunt , Michael Lyon , Andrew T. Metcalf , Peter J. Mohr , David A. Moreno , Brad Newhouse , Li Ren , Jacob Schwarz , Huifen Chen , Lewis Gazzard , Jane Schmidt , Steve Do
IPC分类号： C07D471/04 , A61K45/06 , A61K31/5377 , A61K31/506 , A61K31/444 , C07D487/04 , C07D519/00 , A61K31/55
CPC分类号： C07D471/04 , A61K31/444 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D487/04 , C07D519/00
摘要： Compounds of Formula I or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such diseases, or associated pathological conditions are disclosed.
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![Substituted N-(1H-indazol-4-yl)imidazo[1,2-a]pyridine-3-carboxamide compounds as type III receptor tyrosine kinase inhibitors](/abs-image/US/2017/11/07/US09809590B2/abs.jpg.150x150.jpg)
公开(公告)号：US09809590B2
公开(公告)日：2017-11-07
申请号：US14858029
申请日：2015-09-18
申请人： Array BioPharma Inc.
发明人： Mark Laurence Boys , Robert Kirk DeLisle , Erik James Hicken , April L. Kennedy , David A. Mareska , Fredrik P. Marmsater , Mark C. Munson , Brad Newhouse , Bryson Rast , James P. Rizzi , Martha E. Rodriguez , George T. Topalov , Qian Zhao
IPC分类号： C07D471/04 , A61K45/06 , A61K31/496
CPC分类号： C07D471/04 , A61K31/496 , A61K45/06
摘要： Compounds useful in the treatment of fibrosis, bone-related diseases, cancer, autoimmune disorders, inflammatory diseases, cardiovascular diseases, pain and burns in a mammal.
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![4,6-substituted-pyrazolo[1,5-a]pyrazines as janus kinase inhibitors](/abs-image/US/2021/06/08/US11028093B2/abs.jpg.150x150.jpg)
公开(公告)号：US11028093B2
公开(公告)日：2021-06-08
申请号：US16890663
申请日：2020-06-02
发明人： Shelley Allen , Mark Laurence Boys , Mark J. Chicarelli , Jay Bradford Fell , John P. Fischer , John Gaudino , Erik James Hicken , Ronald Jay Hinklin , Christopher F. Kraser , Ellen Laird , John E. Robinson , Tony P. Tang , Laurence E. Burgess , Robert Andrew Rieger , Jed Pheneger , Yoshitaka Satoh , Katerina Leftheris , Raj K. Raheja , Brydon L. Bennett
IPC分类号： A61K45/06 , C07D487/04 , A61K31/4985 , A61K31/5377
摘要： Compounds of Formula I: and stereoisomers and pharmaceutically acceptable salts and solvates thereof in which R1, R2, R3 and R4 have the meanings given in the specification, are inhibitors of one or more JAK kinases and are useful in the treatment of JAK kinase-associated diseases and disorders, such as autoimmune diseases, inflammatory diseases, rejection of transplanted organs, tissues and cells, as well as hematologic disorders and malignancies and their co-morbidities.
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![4,6-SUBSTITUTED-PYRAZOLO[1,5-a]PYRAZINES AS JANUS KINASE INHIBITORS](/abs-image/US/2017/12/21/US20170362240A1/abs.jpg.150x150.jpg)
公开(公告)号：US20170362240A1
公开(公告)日：2017-12-21
申请号：US15532937
申请日：2015-12-04
发明人： Shelley Allen , Mark Laurence Boys , Mark J. Chicarelli , Jay Bradford Fell , John P. Fischer , John Gaudino , Erik James Hicken , Ronald Jay Hinklin , Christopher F. Kraser , Ellen Laird , John E. Robinson , Tony P. Tang , Laurence E. Burgess , Robert Andrew Rieger , Jed Pheneger , Yoshitaka Satoh , Katerina Leftheris , Raj K. Raheja , Brydon L. Bennett
IPC分类号： C07D487/04 , A61K31/4985 , A61K31/5377 , A61K45/06
CPC分类号： C07D487/04 , A61K31/4985 , A61K31/5377 , A61K45/06
摘要： Compounds of Formula I: and stereoisomers and pharmaceutically acceptable salts and solvates thereof in which R1, R2, R3 and R4 have the meanings given in the specification, are inhibitors of one or more JAK kinases and are useful in the treatment of JAK kinase-associated diseases and disorders, such as autoimmune diseases, inflammatory diseases, rejection of transplanted organs, tissues and cells, as well as hematologic disorders and malignancies and their co-morbidities.
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![5,7-SUBSTITUTED-IMIDAZO[1,2-C]PYRIMIDINES](/abs-image/US/2014/08/14/US20140228349A1/abs.jpg.150x150.jpg)
公开(公告)号：US20140228349A1
公开(公告)日：2014-08-14
申请号：US14351415
申请日：2012-10-09
申请人： Array BioPharma Inc.
发明人： Mark Laurence Boys , Laurence E. Burgess , C. Todd Eary , Robert Groneberg , Bruno P. Hache , Darren Harvey , Erik James Hicken , Christopher F. Kraser , Ellen Laird , David A. Moreno , Mark C. Munson , Li Ren , John E. Robinson , Stephen T. Schlachter
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： Compounds of Formula I: and stereoisomers and pharmaceutically acceptable salts and solvates thereof in which R1, R2, R3, R4, R5, R6, X1 and X2 have the meanings given in the specification, are inhibitors of one or more JAK kinases and are useful in the treatment of autoimmune diseases, inflammatory diseases, rejection of transplanted organs, tissues and cells, as well as hematologic disorders and malignancies and their co-morbidities.
摘要翻译： R 1，R 2，R 3，R 4，R 5，R 6，X 1和X 2具有本说明书中给出的含义的式I化合物及其立体异构体及其药学上可接受的盐和溶剂化物是一种或多种JAK激酶的抑制剂，并且是有用的 治疗自身免疫性疾病，炎症性疾病，移植器官，组织和细胞排斥，以及血液系统疾病和恶性肿瘤及其并发症。
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公开(公告)号：US11267812B2
公开(公告)日：2022-03-08
申请号：US16099398
申请日：2017-05-17
发明人： John P. Fischer , Jay Bradford Fell , James F. Blake , Ronald Jay Hinklin , Macedonio J. Mejia , Erik James Hicken , Mark Joseph Chicarelli , John J. Gaudino , Guy P. A. Vigers , Laurence E. Burgess , Matthew Arnold Marx , James Gail Christensen , Matthew Randolph Lee , Pavel Savechenkov , Henry J. Zecca , Tony P. Tang
IPC分类号： C07D471/04 , C07D519/00 , A61P35/00
摘要： The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.
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公开(公告)号：US20190062330A1
公开(公告)日：2019-02-28
申请号：US16173726
申请日：2018-10-29
发明人： James F. Blake , Laurence E. Burgess , Mark Joseph Chicarelli , James Gail Christensen , Jay Bradford Fell , John P. Fischer , John J. Gaudino , Erik James Hicken , Ronald Jay Hinklin , Matthew Randolf Lee , Matthew Arnold Marx , Macedonio J. Mejia , Martha E. Rodriguez , Pavel Savechenkov , Tony P. Tang , Guy P.A. Vigers , Henry J. Zecca
IPC分类号： C07D471/04 , C07D519/00
摘要： The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.
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公开(公告)号：US20140045817A1
公开(公告)日：2014-02-13
申请号：US14057882
申请日：2013-10-18
申请人： Array BioPharma Inc.
发明人： Shelley Allen , Laura L. Celeste , T. Gregg Davis , Robert Kirk DeLisle , Julie Marie Hicks , Stefan D. Gross , Erik James Hicken , Leila J. Jackson , Nicholas C. Kallan , Joseph P. Lyssikatos , Fredrik P. Marmsater , Mark C. Munson , Jed Pheneger , Bryson Rast , John E. Robinson , Stephen T. Schlachter , George T. Topalov , A. Dale Wright , Qian Zhao
IPC分类号： C07D471/04 , C07D451/06
CPC分类号： C07D471/04 , A61K31/437 , C07D451/06 , C07D519/00
摘要： Provided herein is a method of treating a PIM-1 and/or PIM-2 and/or PIM-3 kinase-mediated condition in a mammal, which comprises administering to said mammal a therapeutically effective amount of a compound of Formula I: in which A, B, R1, R1a, R2, R3, R4, R5, R6, and R7 have the meanings given in the specification.
摘要翻译： 本文提供了一种在哺乳动物中治疗PIM-1和/或PIM-3和/或PIM-3激酶介导的病症的方法，其包括向所述哺乳动物施用治疗有效量的式I化合物：其中 A，B，R1，R1a，R2，R3，R4，R5，R6和R7具有说明书中给出的含义。
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公开(公告)号：US11414404B2
公开(公告)日：2022-08-16
申请号：US16910688
申请日：2020-06-24
申请人： Array BioPharma Inc.
发明人： Patrick Michael Barbour , Katie Keaton Brown , Adam Wade Cook , Erik James Hicken , Dean Russell Kahn , Ellen Ruth Laird , Andrew Terrance Metcalf , David Austin Moreno , Bradley Jon Newhouse , Spencer Phillip Pajk , Brett Joseph Prigaro , Li Ren , Eugene Tarlton
IPC分类号： C07D403/12 , C07D239/90 , C07D239/91 , A61K31/4184 , A61K45/06
摘要： Provided herein are compounds of the Formula I: and pharmaceutically acceptable salts, solvates and polymorphs thereof, wherein L, X1, R1, R2, R3, R4, R5 and R6 are as defined herein, for the treatment of BRAF-associated diseases and disorders, including BRAF-associated tumors, including malignant and benign BRAF-associated tumors of the CNS and malignant extracranial BRAF-associated tumors.
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