公开(公告)号：US20200291039A1

公开(公告)日：2020-09-17

申请号：US16890663

申请日：2020-06-02

Applicant: Array BioPharma Inc. ,  Celgene Corporation

Inventor： 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: C07D487/04 ,  A61K31/4985 ,  A61K31/5377 ,  A61K45/06

Abstract: 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：US10745419B2

公开(公告)日：2020-08-18

申请号：US16156955

申请日：2018-10-10

Applicant: Loxo Oncology, Inc. ,  Array BioPharma Inc.

Inventor： Charles Todd Eary ,  Stacey Spencer ,  Zack Crane ,  Katelyn Chando ,  Sylvie Asselin ,  Weidong Liu ,  Mike Welch ,  Adam Cook ,  Gabrielle R. Kolakowski ,  Andrew T. Metcalf ,  David A. Moreno ,  Tony P. Tang

IPC: C07D519/00 ,  C07D471/04

Abstract: In some embodiments, provided herein is a process for preparing a compound of Formula I or a pharmaceutically acceptable salt thereof, as disclosed herein.

公开(公告)号：US10730880B2

公开(公告)日：2020-08-04

申请号：US16212493

申请日：2018-12-06

Applicant: Array BioPharma Inc. ,  Celgene Corporation

Inventor： 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: A61K45/06 ,  C07D487/04 ,  A61K31/4985 ,  A61K31/5377

Abstract: 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：US10555944B2

公开(公告)日：2020-02-11

申请号：US16173100

申请日：2018-10-29

Applicant: Array BioPharma, Inc.

Inventor： Steven W. Andrews ,  Sean Aronow ,  James F. Blake ,  Barbara J. Brandhuber ,  Adam Cook ,  Julia Haas ,  Yutong Jiang ,  Gabrielle R. Kolakowski ,  Elizabeth A. McFaddin ,  Megan L. McKenney ,  Oren T. McNulty ,  Andrew T. Metcalf ,  David A. Moreno ,  Tony P. Tang ,  Li Ren

IPC: C07D401/02 ,  C07D401/10 ,  A61K31/437 ,  A61K31/4353 ,  A61K31/496 ,  C07D471/04 ,  A61P1/12 ,  A61P35/04 ,  C07D519/00 ,  A61P35/02 ,  A61P35/00 ,  A61K31/444 ,  A61K31/4985 ,  A61K31/4995 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  A61K31/551

Abstract: Provided herein are compounds of the Formula I: and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which A, B, X1, X2, X3, X4, Ring D, and E have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders.

公开(公告)号：US20190263811A1

公开(公告)日：2019-08-29

申请号：US16156880

申请日：2018-10-10

Applicant: Array BioPharma Inc.

Inventor： Andrew T. Metcalf ,  David Fry ,  Elizabeth A. McFaddin ,  Gabrielle R. Kolakowski ,  Julia Haas ,  Tony P. Tang ,  Yutong Jiang

IPC: C07D471/08 ,  A61K9/00 ,  A61P35/00

Abstract: Provided herein are compound of Formula I-IV and pharmaceutically acceptable salts thereof which exhibit rearranged during transfection (RET) kinase inhibition. In particular, provided herein are novel crystalline forms of 4-(6-(4-((6-methoxypyridin-3-yl)methyl)piperazin-1-yl)pyridin-3-yl)-6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile (Formula I), 6-(2-hydroxy-2-methylpropoxy)-4-(6-(6-((6-methoxypyridin-3-yl)methyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile (Formula II), 6-(2-hydroxy-2-methylpropoxy)-4-(6-(6-(6-methoxynicotinoyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile (Formula III), 6-(2-hydroxy-2-methylpropoxy)-4-(6-(4-hydroxy-4-(pyridin-2-ylmethyl)piperidin-1-yl)pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile (Formula IV), and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the compounds, processes for making the compounds, and the use of the compounds in therapy. More particularly, the application relates to novel crystalline forms of Formula I-IV and pharmaceutically acceptable salts thereof useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders.

公开(公告)号：US20190183886A1

公开(公告)日：2019-06-20

申请号：US16173100

申请日：2018-10-29

Applicant: Array BioPharma, Inc.

Inventor： Steven W. Andrews ,  Sean Aronow ,  James F. Blake ,  Barbara J. Brandhuber ,  Adam Cook ,  Julia Haas ,  Yutong Jiang ,  Gabrielle R. Kolakowski ,  Elizabeth A. McFaddin ,  Megan L. McKenney ,  Oren T. McNulty ,  Andrew T. Metcalf ,  David A. Moreno ,  Tony P. Tang ,  Li Ren

IPC: A61K31/496 ,  C07D471/04 ,  A61K31/551 ,  A61K31/4985 ,  A61P35/00 ,  A61K31/444 ,  A61K45/06 ,  A61P1/12 ,  A61K31/506 ,  A61K31/5377 ,  A61P35/02 ,  C07D519/00 ,  A61P35/04 ,  A61K31/4995

Abstract: Provided herein are compounds of the Formula I: and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which A, B, X1, X2, X3, X4, Ring D, and E have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders.

公开(公告)号：US10125134B2

公开(公告)日：2018-11-13

申请号：US15814279

申请日：2017-11-15

Applicant: Mirati Therapeutics, Inc. ,  Array BioPharma Inc.

Inventor： 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: C07D471/04 ,  C07D519/00 ,  A61K31/519

Abstract: 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.

公开(公告)号：US20180148445A1

公开(公告)日：2018-05-31

申请号：US15858929

申请日：2017-12-29

Applicant: Array BioPharma, Inc.

Inventor： Steven W. Andrews ,  Sean Aronow ,  James F. Blake ,  Barbara J. Brandhuber ,  James Collier ,  Adam Cook ,  Julia Haas ,  Yutong Jiang ,  Gabrielle R. Kolakowski ,  Elizabeth A. McFaddin ,  Megan L. McKenney ,  Oren T. McNulty ,  Andrew T. Metcalf ,  David A. Moreno ,  Ginelle A. Ramann ,  Tony P. Tang ,  Li Ren ,  Shane M. Walls

IPC: C07D471/04 ,  A61P35/00 ,  A61P1/00

CPC classification number: A61K31/4545 ,  A61K31/4162 ,  A61K31/444 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  A61P1/00 ,  A61P1/12 ,  A61P35/00 ,  A61P35/02 ,  C07D471/04

Abstract: Provided herein are compounds of the Formula I: or pharmaceutically acceptable salt or solvate thereof, wherein A, B, X1, X2, X3, X4, Ring D, E, Ra, Rb, n and m have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders.

公开(公告)号：US20180134702A1

公开(公告)日：2018-05-17

申请号：US15858240

申请日：2017-12-29

Applicant: Array BioPharma, Inc.

Inventor： Steven W. Andrews ,  Sean Aronow ,  James F. Blake ,  Barbara J. Brandhuber ,  Adam Cook ,  Julia Haas ,  Yutong Jiang ,  Gabrielle R. Kolakowski ,  Elizabeth A. McFaddin ,  Megan L. McKenney ,  Oren T. McNulty ,  Andrew T. Metcalf ,  David A. Moreno ,  Tony P. Tang ,  Li Ren

IPC: C07D471/04 ,  C07D519/00 ,  A61P35/04 ,  A61P1/12

CPC classification number: A61K31/496 ,  A61K31/444 ,  A61K31/4985 ,  A61K31/4995 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/551 ,  A61K45/06 ,  A61P1/12 ,  A61P35/00 ,  A61P35/02 ,  A61P35/04 ,  C07D471/04 ,  C07D519/00

Abstract: Provided herein are compounds of the Formula I: and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which A, B, X1, X2, X3, X4, Ring D, and E have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders.