公开(公告)号：US20190106438A1

公开(公告)日：2019-04-11

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

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：US10251889B2

公开(公告)日：2019-04-09

申请号：US15724601

申请日：2017-10-04

Applicant: Array BioPharma, Inc.

Inventor： Shelley Allen ,  Steven W. Andrews ,  Kevin Ronald Condroski ,  Julia Haas ,  Lily Huang ,  Yutong Jiang ,  Timothy Kercher ,  Jeongbeob Seo

IPC: C07D487/04 ,  A61K31/519 ,  C07D519/00 ,  C07D453/02 ,  C07D471/22 ,  C07D498/22 ,  A61K31/5377

Abstract: Compounds of Formula I: and salts thereof in which R1, R2, R3, R4, X, Y and n have the meanings given in the specification, are inhibitors of Trk kinases and are useful in the treatment of diseases which can be treated with a Trk kinase inhibitor such as pain, cancer, inflammation, neurodegenerative diseases and certain infectious 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.

公开(公告)号：US20180334450A1

公开(公告)日：2018-11-22

申请号：US15839706

申请日：2017-12-12

Applicant: Array BioPharma Inc.

Inventor： Shelley Allen ,  Steven W. Andrews ,  James F. Blake ,  Kevin R. Condroski ,  Julia Haas ,  Lily Huang ,  Yutong Jiang ,  Timothy Kercher ,  Gabrielle R. Kolakowski ,  Jeongbeob Seo

IPC: C07D403/12 ,  C07D491/048 ,  C07D401/14 ,  A61K31/5377 ,  A61K31/506 ,  A61K31/497 ,  A61K31/496 ,  A61K31/454 ,  A61K31/4439 ,  A61K31/4375 ,  A61K31/427 ,  A61K31/4245 ,  A61K31/422 ,  A61K31/4196 ,  A61K31/4192 ,  A61K31/4178 ,  A61K31/4162 ,  A61K31/4155 ,  C07D495/04 ,  C07D491/04 ,  C07D487/04 ,  C07D471/04 ,  C07D417/14 ,  C07D413/14 ,  C07D409/14 ,  C07D405/14 ,  C07D403/14

CPC classification number: C07D403/12 ,  A61K31/4155 ,  A61K31/4162 ,  A61K31/4178 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/4375 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5377 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D491/048 ,  C07D495/04 ,  Y02A50/414

Abstract: Compounds of Formula I: or stereoisomers, tautomers, or pharmaceutically acceptable salts, or solvates or prodrugs thereof, where R1, R2, Ra, Rb, Rc, Rd, X, Y, B, and Ring C are as defined herein, and wherein the Y—B moiety and the NH—C(═X)—NH moiety are in the trans configuration, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.

公开(公告)号：US20180282324A1

公开(公告)日：2018-10-04

申请号：US15806650

申请日：2017-11-08

Applicant: Genentech, Inc. ,  Array Biopharma Inc.

Inventor： Jeffrey Stults ,  Christopher M. Lindemann ,  Keith L. Spencer ,  Weidong Liu ,  Joseph Lubach

IPC: C07D471/04 ,  A61K31/437 ,  A61K45/06

Abstract: Disclosed are crystalline forms of (R)—N-(4-(3-aminopiperidin-1-yl)-5-bromo-1H-pyrrolo[2,3-b]pyridin-3-yl)cyclopropanecarboxamide, and salts, solvates, and hydrates thereof, and pharmaceutical compositions, formulations and a process of manufacturing thereof.

公开(公告)号：US20180207162A1

公开(公告)日：2018-07-26

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 ,  C12Q1/48

CPC classification number: A61K31/519 ,  C07D487/04 ,  C12Q1/485 ,  C12Y207/10001 ,  G01N2333/91205 ,  G01N2800/52 ,  Y02A50/414

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.