公开(公告)号：US11028093B2

公开(公告)日：2021-06-08

申请号：US16890663

申请日：2020-06-02

申请人： Array BioPharma Inc. ,  Celgene Corporation

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.

公开(公告)号：US20170362240A1

公开(公告)日：2017-12-21

申请号：US15532937

申请日：2015-12-04

申请人： ARRAY BIOPHARMA INC. ,  CELGENE CORPORATION

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.

公开(公告)号：US20200291039A1

公开(公告)日：2020-09-17

申请号：US16890663

申请日：2020-06-02

申请人： Array BioPharma Inc. ,  Celgene Corporation

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

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.

公开(公告)号：US10730880B2

公开(公告)日：2020-08-04

申请号：US16212493

申请日：2018-12-06

申请人： Array BioPharma Inc. ,  Celgene Corporation

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.

公开(公告)号：US20190177328A1

公开(公告)日：2019-06-13

申请号：US16212493

申请日：2018-12-06

申请人： Array BioPharma Inc. ,  Celgene Corporation

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 ,  A61K45/06 ,  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.

公开(公告)号：US10189845B2

公开(公告)日：2019-01-29

申请号：US15532937

申请日：2015-12-04

申请人： ARRAY BIOPHARMA INC. ,  CELGENE CORPORATION

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.

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.

公开(公告)号：US20160304519A1

公开(公告)日：2016-10-20

申请号：US15197445

申请日：2016-06-29

申请人： Array BioPharma Inc. ,  Genentech, Inc.

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。

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。

公开(公告)号：US11267812B2

公开(公告)日：2022-03-08

申请号：US16099398

申请日：2017-05-17

申请人： Mirati Therapeutics, Inc. ,  Array BioPharma Inc.

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.