公开(公告)号：US20200345735A1

公开(公告)日：2020-11-05

申请号：US16736078

申请日：2020-01-07

Applicant: Array BioPharma Inc. ,  Genentech, Inc.

Inventor： Ian S. Mitchell ,  James F. Blake ,  Rui Xu ,  Nicholas C. Kallan ,  Dengming Xiao ,  Keith Lee Spencer ,  Josef R. Bencsik ,  Eli M. Wallace ,  Stephen T. Schlachter ,  Anna L. Leivers ,  Jun Liang ,  Brian Safina ,  Birong Zhang ,  Christine Chabot ,  Steven Do

IPC: A61K31/517 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D239/70 ,  C07D413/12 ,  C07D407/12

Abstract: The present invention provides compounds, including resolved enantiomers, resolved diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula I: Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.

公开(公告)号：US10780073B2

公开(公告)日：2020-09-22

申请号：US15975323

申请日：2018-05-09

Applicant: ARRAY BIOPHARMA, INC.

Inventor： Joseph P. Lyssikatos ,  Julie Marie Hicks ,  Fredrik P. Marmsater ,  Qian Zhao

IPC: A61K31/337 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D495/04 ,  C07D519/00 ,  C07D471/04 ,  A61K31/513 ,  A61K31/517 ,  A61K39/395

Abstract: This invention provides compounds of Formula I wherein B, G, A, E, R1, R2, R3, m and n are as defined herein, which are useful as type I receptor tyrosine kinase inhibitors, and methods of use thereof in the treatment of hyperproliferative disorders in mammals.

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：US10689377B2

公开(公告)日：2020-06-23

申请号：US16191190

申请日：2018-11-14

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

Inventor： James F. Blake ,  Laurence E. Burgess ,  Mark Joseph Chicarelli ,  James Gail Christensen ,  Adam Cook ,  Jay Bradford Fell ,  John P. Fischer ,  Matthew Arnold Marx ,  Macedonio J. Mejia ,  Pavel Savechenkov ,  Guy P. A. Vigers ,  Christopher Ronald Smith ,  Martha E. Rodriguez

IPC: C07D471/04 ,  A61P35/00 ,  C07D491/08

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：US10669269B2

公开(公告)日：2020-06-02

申请号：US15717700

申请日：2017-09-27

Applicant: ARRAY BIOPHARMA INC.

Inventor： Mark Laurence Boys ,  Robert Kirk DeLisle ,  Erik James Hicken ,  April L. Kennedy ,  David A. Mareska ,  Fredrik P. Marmsäter ,  Mark C. Munson ,  Brad Newhouse ,  Bryson Rast ,  James P. Rizzi ,  Martha E. Rodriguez ,  George T. Topalov ,  Qian Zhao

IPC: A61K31/496 ,  A61K45/06 ,  C07D471/04

Abstract: Compounds of Formula I: and pharmaceutically acceptable salts thereof in which R1, R2, R3, R4, R5 and R6 have the meanings given in the specification, are inhibitors of cFMS and are 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：US10568884B2

公开(公告)日：2020-02-25

申请号：US15818264

申请日：2017-11-20

Applicant: Array BioPharma, Inc.

Inventor： Shenlin Huang ,  Xianming Jin ,  Zuosheng Liu ,  Daniel Poon ,  John Tellew ,  Yongqin Wan ,  Xing Wang ,  Yongping Xie

IPC: A61K31/506 ,  A61K31/4184 ,  A61K9/00 ,  C07D405/14 ,  A61K45/06 ,  C07D403/04 ,  C07D401/14

Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of B-Raf.

公开(公告)号：US10434094B2

公开(公告)日：2019-10-08

申请号：US15169149

申请日：2016-05-31

Applicant: Array BioPharma Inc.

Inventor： Kurtis D. Davies ,  Stefan Gross

IPC: A61K31/4545 ,  A61K31/4745 ,  A61K31/519 ,  A61K31/7068 ,  A61K31/437 ,  A61K31/495 ,  A61K31/551 ,  A61K45/06

Abstract: A combination of a CHK1 inhibitor and a WEE1 inhibitor are provided.

公开(公告)号：US20190275043A1

公开(公告)日：2019-09-12

申请号：US16353951

申请日：2019-03-14

Applicant: Array BioPharma Inc.

Inventor： David Shank Fry ,  Christopher M. Lindemann ,  Michael Preigh ,  Corey Jay Bloom ,  Christopher Donovan Craig ,  Devon Brevard Dubose ,  Jeff Gautschi ,  Dan Smithey

IPC: A61K31/517 ,  A61K47/32 ,  A61K9/10 ,  A61K9/20 ,  A61K9/16 ,  A61K47/38 ,  A61K9/00

Abstract: A solid dispersion of N4-(4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)-3-methylphenyl)-N6-(4,4-dimethyl-4,5-dihydrooxazol-2-yl)quinazoline-4,6-diamine and processes for preparing the solid dispersion are provided herein. Also, a pharmaceutical composition comprising a solid dispersion of N4-(4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)-3-methylphenyl)-N6-(4,4-dimethyl-4,5-dihydrooxazol-2-yl)quinazoline-4,6-diamine and uses thereof are provided herein.