公开(公告)号：US10441581B2

公开(公告)日：2019-10-15

申请号：US15860894

申请日：2018-01-03

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 ,  A61K31/4162 ,  A61K31/4545 ,  A61P1/00 ,  A61P35/00 ,  A61P35/02 ,  A61K31/444 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  A61P1/12

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：US10398683B2

公开(公告)日：2019-09-03

申请号：US15842715

申请日：2017-12-14

Applicant: Array BioPharma Inc.

Inventor： Christoph Max Krell ,  Marian Misun ,  Daniel Andreas Niederer ,  Werner Heinz Pachinger ,  Marie-Christine Wolf ,  Daniel Zimmermann ,  Weidong Liu ,  Peter J. Stengel ,  Paul Nichols

IPC: A61K31/4184 ,  A61K45/06 ,  A61K47/26 ,  A61K9/20 ,  C07D235/08 ,  C07D235/06 ,  A61K47/12 ,  A61K47/02 ,  C30B29/54 ,  C30B7/08 ,  A61K47/38 ,  A61K9/00

Abstract: The present invention relates to processes for preparing 6-(4-bromo-2-fluorophenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxyethyoxy)-amide, processes for preparing crystallized 6-(4-bromo-2-fluorophenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxyethyoxy)-amide, and intermediates useful therefore. Also provided herein are pharmaceutical compositions comprising this crystallized compound.

公开(公告)号：US10329288B2

公开(公告)日：2019-06-25

申请号：US14913635

申请日：2014-08-21

Applicant: Genentech, Inc. ,  Array BioPharma Inc.

Inventor： Chong Han ,  Keena Green ,  Francis Gosselin ,  Michelangelo Scalone ,  Paul J. Nichols ,  Weidong Liu ,  Keith L. Spencer ,  Zackary D. Crane ,  Peter J. Stengel ,  Sagar Shakya

IPC: C07D471/04

Abstract: The invention provides processes of preparation thereof useful in the preparation of compounds that can be used as CHK1 inhibitors.

公开(公告)号：US10285993B2

公开(公告)日：2019-05-14

申请号：US15706062

申请日：2017-09-15

Applicant: Array BioPharma, Inc.

Inventor： Alisha B. Arrigo ,  Derrick Juengst ,  Khalid Shah

IPC: A61K31/519 ,  C07D487/04 ,  C12Q1/48

Abstract: A novel crystalline form of (S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide, pharmaceutical compositions containing said crystalline form and the use of said crystalline form in the treatment of pain, cancer, inflammation, neurodegenerative disease or Trypanosoma cruzi infection are disclosed. In some embodiments, the novel crystalline form comprises a stable polymorph of (S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate. The present invention is further directed to a process for the preparation of the novel crystalline form.

公开(公告)号：US10258622B2

公开(公告)日：2019-04-16

申请号：US15452239

申请日：2017-03-07

Applicant: Array BioPharma, Inc.

Inventor： Daya Verma ,  Yogita Krishnamachari ,  Xiaohong Shen ,  Hanchen Lee ,  Ping Li ,  Rajinder Singh ,  LayChoo Tan

IPC: A61K31/506 ,  A61K9/20 ,  A61K9/28 ,  A61K9/48 ,  A61K9/00

Abstract: This invention relates to solid oral pharmaceutical formulations of (S)-methyl (1-((4-(3-(5-chloro-2-fluoro-3-(methyl-sulfonamido)phenyl)-1-isopropyl-1H-pyrazol-4-yl)pyrimidin-2-yl)amino)propan-2-yl)carbamate (COMPOUND A) and the use of these formulations for treating proliferative diseases, such as solid tumor diseases.

公开(公告)号：US10221194B2

公开(公告)日：2019-03-05

申请号：US15606928

申请日：2017-05-26

Applicant: ARRAY BIOPHARMA INC.

Inventor： Eli Wallace ,  Joseph Lyssikatos ,  George Topalov ,  Alexandre Buckmelter ,  Qian Zhao

IPC: C07D239/94 ,  C07D498/10 ,  C04B35/632 ,  C07D401/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D498/04 ,  A61K31/517 ,  A61P35/04

Abstract: The invention relates to compounds of Formula 11, and to pharmaceutically acceptable acid addition salts thereof, wherein R1—R3, R6, and X have any of the values defined in the specification. The compounds are suitable as synthetic intermediates for preparing imaging tools.

公开(公告)号：US20190062330A1

公开(公告)日：2019-02-28

申请号：US16173726

申请日：2018-10-29

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

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：US10172861B2

公开(公告)日：2019-01-08

申请号：US15872769

申请日：2018-01-16

Applicant: Array BioPharma, Inc.

Inventor： Alisha B. Arrigo ,  Derrick Juengst ,  Khalid Shah

IPC: A61K31/519 ,  C07D487/04 ,  C12Q1/48

Abstract: A novel crystalline form of (S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide, pharmaceutical compositions containing said crystalline form and the use of said crystalline form in the treatment of pain, cancer, inflammation, neurodegenerative disease or Trypanosoma cruzi infection are disclosed. In some embodiments, the novel crystalline form comprises a stable polymorph of (S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate. The present invention is further directed to a process for the preparation of the novel crystalline form.

公开(公告)号：US10143692B2

公开(公告)日：2018-12-04

申请号：US15861444

申请日：2018-01-03

Applicant: Array BioPharma Inc.

Inventor： Donald T. Corson ,  Christopher M. Lindemann ,  Daniel J. Watson

IPC: C07D471/04 ,  A61K31/437 ,  A61K31/517 ,  A61P35/00 ,  A61K45/06

Abstract: Polymorphs 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 are provided herein. Processes for preparing the polymorphs and pharmaceutical composition comprising the polymorphs are also disclosed.

公开(公告)号：US20180338958A1

公开(公告)日：2018-11-29

申请号：US16000756

申请日：2018-06-05

Applicant: Array BioPharma Inc.

Inventor： Brian J. Tunquist ,  Duncan HL. Walker ,  Richard D. Woessner

IPC: A61K31/433 ,  A61K31/00

Abstract: Methods of treating diseases caused by cell division or that are treated by inhibiting mitosis by administering two doses of an inhibitor of mitosis between the biologically effective dose and the maximum tolerated dose in a dosing cycle that allows for the recovery or subsiding of side effects, wherein the second dose is administered 24 to 48 hours after the first dose.