公开(公告)号：US10154995B2

公开(公告)日：2018-12-18

申请号：US15684733

申请日：2017-08-23

Applicant: Array BioPharma Inc. ,  Genentech, Inc.

Inventor： James F. Blake ,  Adam Cook ,  Indrani W. Gunawardana ,  Kevin W. Hunt ,  Michael Lyon ,  Andrew T. Metcalf ,  Peter J. Mohr ,  David A. Moreno ,  Brad Newhouse ,  Li Ren ,  Tony P. Tang ,  Allen A. Thomas ,  Jacob Schwarz ,  Jane Schmidt ,  Lewis Gazzard ,  Huifen Chen

IPC: A61K31/506 ,  C07D417/14 ,  C07D405/14 ,  C07D403/04 ,  C07D401/14 ,  C07D471/04 ,  C07D403/14 ,  A61K31/4439 ,  A61K31/444 ,  A61K45/06

Abstract: Compounds of Formula I or a stereoisomer, tautomer 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 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.

公开(公告)号：US20180086758A1

公开(公告)日：2018-03-29

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

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：US09763942B2

公开(公告)日：2017-09-19

申请号：US15197479

申请日：2016-06-29

Applicant: Array BioPharma Inc. ,  Genentech, Inc.

Inventor： James F. Blake ,  Adam Cook ,  Indrani W. Gunawardana ,  Kevin W. Hunt ,  Michael Lyon ,  Andrew T. Metcalf ,  Peter J. Mohr ,  David A. Moreno ,  Brad Newhouse ,  Li Ren ,  Tony P. Tang ,  Allen A. Thomas ,  Jacob Schwarz ,  Jane Schmidt ,  Lewis Gazzard ,  Huifen Chen

IPC: C07D403/14 ,  C07D471/04 ,  C07D417/14 ,  C07D403/04 ,  C07D401/14 ,  A61K31/506 ,  A61K31/4439 ,  A61K31/444 ,  A61K45/06 ,  C07D405/14

CPC classification number: A61K31/506 ,  A61K31/4439 ,  A61K31/444 ,  A61K45/06 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D417/14 ,  C07D471/04

Abstract: Compounds of Formula I or a stereoisomer, tautomer 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 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.

公开(公告)号：US20230077225A1

公开(公告)日：2023-03-09

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

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：US10647715B2

公开(公告)日：2020-05-12

申请号：US16412091

申请日：2019-05-14

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：US20160303126A1

公开(公告)日：2016-10-20

申请号：US15197479

申请日：2016-06-29

Applicant: Array BioPharma Inc. ,  Genentech, Inc.

Inventor： James F. Blake ,  Adam Cook ,  Indrani W. Gunawardana ,  Kevin W. Hunt ,  Michael Lyon ,  Andrew T. Metcalf ,  Peter J. Mohr ,  David A. Moreno ,  Brad Newhouse ,  Li Ren ,  Tony P. Tang ,  Allen A. Thomas ,  Jacob Schwarz ,  Jane Schmidt ,  Lewis Gazzard ,  Huifen Chen

IPC: A61K31/506 ,  C07D403/14 ,  C07D471/04 ,  A61K31/4439 ,  C07D417/14 ,  C07D403/04 ,  C07D401/14 ,  A61K31/444 ,  A61K45/06 ,  C07D405/14

CPC classification number: A61K31/506 ,  A61K31/4439 ,  A61K31/444 ,  A61K45/06 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D417/14 ,  C07D471/04

Abstract: Compounds of Formula I or a stereoisomer, tautomer 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 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.

公开(公告)号：US20160272592A1

公开(公告)日：2016-09-22

申请号：US14442576

申请日：2013-11-12

Applicant: ARRAY BIOPHARMA INC.

Inventor： James F. Blake ,  Barbara J. Brandhuber ,  Julia Haas ,  Brad Newhouse ,  Allen A. Thomas ,  Shannon L. Winski

IPC: C07D231/52 ,  C07D401/04 ,  C07D405/14 ,  C07D401/14 ,  C07D231/54 ,  C07D453/02 ,  C07D495/04 ,  C07D413/12 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D403/04 ,  C07D231/40

CPC classification number: C07D231/52 ,  C07D231/38 ,  C07D231/40 ,  C07D231/54 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C07D453/02 ,  C07D495/04

Abstract: Compounds of Formula I or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C, X, Ra, Rb, Rc, Rd and n are as defined herein, 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/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis or pelvic pain syndrome.

Abstract translation: 式I或其立体异构体，互变异构体或其药学上可接受的盐，溶剂合物或前药的化合物，其中环A，环C，X，R a，R b，R c，R d和n如本文所定义，是TrkA激酶的抑制剂，并且是有用的 治疗可用TrkA激酶抑制剂如疼痛，癌症，炎症/炎性疾病，神经变性疾病，某些感染性疾病，干燥综合征，子宫内膜异位症，糖尿病性周围神经病变，前列腺炎或骨盆疼痛综合征治疗的疾病。

公开(公告)号：US20160129010A1

公开(公告)日：2016-05-12

申请号：US14817291

申请日：2015-08-04

Applicant: VentiRx Pharmaceuticals, Inc. ,  Array BioPharma, Inc.

Inventor： James Jeffry Howbert ,  Gregory Dietsch ,  Robert Hershberg ,  Laurence E. Burgess ,  Joseph P. Lyssikatos ,  Brad Newhouse ,  Hong-Woon Yang

IPC: A61K31/55

CPC classification number: A61K31/55 ,  C07D223/14 ,  C07D223/16 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D405/04 ,  C07D405/10

Abstract: Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in treating or preventing disease, including cancer, autoimmune disease, infectious disease, inflammatory disorder, graft rejection, and graft-versus-host disease.

Abstract translation: 提供了可用于通过Toll样受体TLR7和/或TLR8调节信号传导的组合物和方法。 组合物和方法可用于治疗或预防疾病，包括癌症，自身免疫性疾病，感染性疾病，炎症性疾病，移植排斥反应和移植物抗宿主病。

公开(公告)号：US20140234376A1

公开(公告)日：2014-08-21

申请号：US14180939

申请日：2014-02-14

Applicant: Array BioPharma, Inc. ,  VentiRx Pharmaceuticals, Inc.

Inventor： James Jeffry Howbert ,  Gregory Dietsch ,  Robert Hershberg ,  Laurence E. Burgess ,  Joseph P. Lyssikatos ,  Brad Newhouse ,  Hong-Woon Yang

IPC: C07D223/16 ,  C07D405/04 ,  C07D401/04 ,  C07D405/10 ,  C07D401/12 ,  C07D403/10

CPC classification number: A61K31/55 ,  C07D223/14 ,  C07D223/16 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D405/04 ,  C07D405/10

Abstract: Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in treating or preventing disease, including cancer, autoimmune disease, infectious disease, inflammatory disorder, graft rejection, and graft-verses-host disease.

Abstract translation: 提供了可用于通过Toll样受体TLR7和/或TLR8调节信号传导的组合物和方法。 组合物和方法可用于治疗或预防疾病，包括癌症，自身免疫性疾病，感染性疾病，炎性疾病，移植物排斥反应和移植物宿主病。

公开(公告)号：US20200262837A1

公开(公告)日：2020-08-20

申请号：US16868258

申请日：2020-05-06

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 ,  C07D491/08 ,  A61P35/00

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.