公开(公告)号：US09388171B2

公开(公告)日：2016-07-12

申请号：US14011501

申请日：2013-08-27

Applicant: Array BioPharma Inc. ,  Genentech, Inc.

Inventor： Jim Blake ,  Huifen Chen ,  Mark Chicarelli ,  John Gaudino ,  Lewis Gazzard ,  Sam Kintz ,  Pete Mohr ,  Kirk Robarge ,  Jacob Schwarz ,  Aihe Zhou

IPC: C07D471/04 ,  C07D217/22 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  A61K31/4725 ,  A61K31/4375 ,  A61K31/472 ,  A61P35/00

CPC classification number: C07D405/14 ,  C07D217/22 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D471/04

Abstract: Compounds having the formula I wherein R2, X and Z as defined herein are inhibitors of ERK kinase. Also disclosed are compositions and methods for treating hyperproliferative disorders.

Abstract translation: 具有式I的化合物，其中本文定义的R2，X和Z是ERK激酶的抑制剂。 还公开了用于治疗过度增殖性疾病的组合物和方法。

公开(公告)号：US20130252934A1

公开(公告)日：2013-09-26

申请号：US13782513

申请日：2013-03-01

Applicant: ARRAY BIOPHARMA INC. ,  GENENTECH, INC.

Inventor： James F. Blake ,  Mark Joseph Chicarelli ,  Rustam Ferdinand Garrey ,  John Gaudino ,  Jonas Grina ,  David A. Moreno ,  Peter J. Mohr ,  Li Ren ,  Jacob Schwarz ,  Huifen Chen ,  Kirk Robarge ,  Aihe Zhou

IPC: A61K31/506 ,  C07D401/04 ,  A61K45/06 ,  C07D413/14 ,  C07D409/14 ,  C07D417/14 ,  C07D405/14 ,  C07D401/14

CPC classification number: C07D401/04 ,  A61K31/444 ,  A61K31/506 ,  A61K31/513 ,  A61K31/53 ,  A61K45/06 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07F9/65586

Abstract: Compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative, pain and inflammatory diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

Abstract translation: 提供式I化合物或其立体异构体，互变异构体，前药或其药学上可接受的盐，其可用于治疗过度增生，疼痛和炎性疾病。 公开了使用式I化合物或其立体异构体，互变异构体，前药或其药学上可接受的盐在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。

公开(公告)号：US20240309020A1

公开(公告)日：2024-09-19

申请号：US18644056

申请日：2024-04-23

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

Inventor： Xiaolun Wang ,  Aaron Craig Burns ,  James Gail Christensen ,  John Michael Ketcham ,  John David Lawson ,  Matthew Arnold Marx ,  Christopher Ronald Smith ,  Shelley Allen ,  James F. Blake ,  Mark Joseph Chicarelli ,  Joshua Ryan Dahlke ,  Donghua Dai ,  Jay Bradford Fell ,  John Peter Fischer ,  Macedonio J. Mejia ,  Brad Newhouse ,  Phong Nguyen ,  Jacob Matthew O'Leary ,  Spencer Pajk ,  Martha E. Rodriguez ,  Pavel Savechenkov ,  Tony P. Tang ,  Guy P.A. Vigers ,  Qian Zhao ,  Dean Russell Kahn ,  John Gaudino ,  Michael Christopher Hilton

IPC: C07D519/00

CPC classification number: C07D519/00

Abstract: The present invention relates to compounds that inhibit KRas G12D. In particular, the present invention relates to compounds that inhibit the activity of KRas G12D, pharmaceutical compositions comprising the compounds and methods of use therefor.

公开(公告)号：US11964989B2

公开(公告)日：2024-04-23

申请号：US17869575

申请日：2022-07-20

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

Inventor： Xiaolun Wang ,  Aaron Craig Burns ,  James Gail Christensen ,  John Michael Ketcham ,  John David Lawson ,  Matthew Arnold Marx ,  Christopher Ronald Smith ,  Shelley Allen ,  James F. Blake ,  Mark Joseph Chicarelli ,  Joshua Ryan Dahlke ,  Donghua Dai ,  Jay Bradford Fell ,  John Peter Fischer ,  Macedonio J. Mejia ,  Brad Newhouse ,  Phong Nguyen ,  Jacob Matthew O'Leary ,  Spencer Pajk ,  Martha E. Rodriguez ,  Pavel Savechenkov ,  Tony P. Tang ,  Guy P.A. Vigers ,  Qian Zhao ,  Dean Russell Kahn ,  John Gaudino ,  Michael Christopher Hilton

IPC: C07D519/00

CPC classification number: C07D519/00

Abstract: Compounds that inhibit KRas G12D. In particular, compounds that inhibit the activity of KRas G12D, pharmaceutical compositions comprising the compounds and methods of use therefor, and in particular, methods of treating cancer. The compounds have a general structure represented by Formula (I):




or a pharmaceutically acceptable salt thereof.

公开(公告)号：US11780835B2

公开(公告)日：2023-10-10

申请号：US17376571

申请日：2021-07-15

Applicant: Array BioPharma Inc.

Inventor： Ronald Jay Hinklin ,  Shelley Allen ,  Patrick Barbour ,  Adam Cook ,  Joshua Dahlke ,  John Gaudino ,  Ellen Laird ,  Oren T. McNulty ,  Qian Zhao

IPC: C07D471/04

CPC classification number: C07D471/04

Abstract: Provided herein are compounds of the Formula (I): and stereoisomers, tautomers and pharmaceutically acceptable salts thereof, wherein R1, R2, R9, X1 and G are as defined herein, which are inhibitors of one or more TAM kinases and/or c-Met kinase, and are useful in the treatment and prevention of diseases which can be treated with a TAM kinase inhibitor and/or a c-Met kinase inhibitor.

公开(公告)号：US11247990B1

公开(公告)日：2022-02-15

申请号：US16893784

申请日：2018-12-05

Applicant: ARRAY BIOPHARMA INC.

Inventor： Shelley Allen ,  Mark Laurence Boys ,  Adam Cook ,  John Gaudino ,  Ronald Jay Hinklin ,  Ellen Laird ,  Oren T. McNulty ,  Andrew T. Metcalf ,  Brad Newhouse ,  John E. Robinson

IPC: C07D471/04 ,  C07D519/00

Abstract: Provided herein are compounds of the Formula (I): and stereoisomers, tautomers and pharmaceutically acceptable salts thereof, wherein Ring A, X1, X2, X3, R1, R2 and R3 are as defined herein, which are inhibitors of one or more TAM kinases and are useful in the treatment and prevention of diseases which can be treated with a TAM kinase inhibitor.

公开(公告)号：US20200308170A1

公开(公告)日：2020-10-01

申请号：US16869079

申请日：2020-05-07

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

Inventor： Matthew Arnold Marx ,  Thomas P. Bobinski ,  Aaron Craig Burns ,  John Gaudino ,  Julia Haas ,  John Michael Ketcham ,  John David Lawson ,  Brad Newhouse ,  Spencer Pajk ,  Christopher Ronald Smith ,  Tony P. Tang

IPC: C07D471/04 ,  A61P35/00 ,  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：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：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：US20200079770A1

公开(公告)日：2020-03-12

申请号：US16555432

申请日：2019-08-29

Applicant: Array BioPharma Inc.

Inventor： Ronald Jay Hinklin ,  Shelley Allen ,  Patrick Barbour ,  Adam Cook ,  Joshua Dahlke ,  John Gaudino ,  Ellen Laird ,  Oren T. McNulty ,  Qian Zhao

IPC: C07D471/04

Abstract: Provided herein are compounds of the Formula I: and stereoisomers, tautomers and pharmaceutically acceptable salts thereof, wherein R1, R2, R9, X1 and G are as defined herein, which are inhibitors of one or more TAM kinases and/or c-Met kinase, and are useful in the treatment and prevention of diseases which can be treated with a TAM kinase inhibitor and/or a c-Met kinase inhibitor.