公开(公告)号：US20160297796A1

公开(公告)日：2016-10-13

申请号：US14442522

申请日：2013-11-13

Applicant: ARRAY BIOPHARMA INC.

Inventor： Shelley Allen ,  Steven Wade Andrews ,  James F. Blake ,  Barbara J. Brandhuber ,  Kevin Ronald Condroski ,  Julia Haas ,  Yutong Jiang ,  Timothy Kercher ,  Gabrielle R. Kolakowski ,  Shannon L. Winski

IPC: C07D401/12 ,  C07D417/14 ,  C07D417/12 ,  C07D413/12 ,  C07D401/14 ,  C07D403/12

CPC classification number: C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14

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, Ring B, and Ring C are as defined herein, and wherein Ring 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/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis and pelvic pain syndrome.

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：US09365568B2

公开(公告)日：2016-06-14

申请号：US14591691

申请日：2015-01-07

Applicant: Array BioPharma Inc.

Inventor： Yvan Le Huerou ,  James F. Blake ,  Indrani W. Gunawardana ,  Peter J. Mohr ,  Eli M. Wallace ,  Bin Wang ,  Mark Joseph Chicarelli ,  Michael Lyon

IPC: C07D495/14 ,  C07D471/04 ,  C07D401/06

CPC classification number: C07D471/04 ,  C07D401/06 ,  C07D519/00

Abstract: Compounds of Formula I are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula I and stereoisomers and pharmaceutically acceptable salts 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：US08758830B2

公开(公告)日：2014-06-24

申请号：US13974895

申请日：2013-08-23

Applicant: Array BioPharma Inc.

Inventor： Yvan Le Huerou ,  James F. Blake ,  Indrani W. Gunawardana ,  Peter J. Mohr ,  Eli M. Wallace ,  Bin Wang ,  Mark Joseph Chicarelli ,  Michael Lyon

IPC: A61K31/4545 ,  A61K31/437 ,  A61K31/497 ,  A61K31/506 ,  A61K31/513 ,  A61K31/444 ,  A61K31/501 ,  A61K35/00 ,  A61K33/24

CPC classification number: C07D471/04 ,  C07D401/06 ,  C07D519/00

Abstract: Compounds of Formula I are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula I and stereoisomers and pharmaceutically acceptable salts 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: 式I的化合物可用于抑制CHK1和/或CHK2。 公开了使用式I化合物及其立体异构体及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：US20140100369A1

公开(公告)日：2014-04-10

申请号：US13974895

申请日：2013-08-23

Applicant: Array BioPharma Inc.

Inventor： Yvan Le Huerou ,  James F. Blake ,  Indrani W. Gunawardana ,  Peter J. Mohr ,  Eli M. Wallace ,  Bin Wang ,  Mark Joseph Chicarelli ,  Michael Lyon

IPC: C07D471/04

CPC classification number: C07D471/04 ,  C07D401/06 ,  C07D519/00

Abstract: Compounds of Formula I are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula I and stereoisomers and pharmaceutically acceptable salts 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：US11964988B2

公开(公告)日：2024-04-23

申请号：US17274990

申请日：2019-09-06

Applicant: ARRAY BIOPHARMA INC.

Inventor： James F. Blake ,  Donghua Dai ,  Julia Haas ,  Yutong Jiang ,  Dean Kahn ,  Gabrielle R. Kolakowski ,  Elizabeth A. McFaddin ,  Megan L McKenney ,  Andrew T. Metcalf ,  David A. Moreno ,  Brett Prigaro ,  Ginelle A. Ramann ,  Li Ren ,  Shane M. Walls ,  Hailong Zhang

IPC: C07D498/22 ,  A61K31/519 ,  A61K31/55 ,  A61K31/554 ,  A61K45/06 ,  A61P35/00 ,  C07D487/14 ,  C07D498/14 ,  C07D513/22

CPC classification number: C07D498/22 ,  A61K31/519 ,  A61K31/55 ,  A61K31/554 ,  A61K45/06 ,  A61P35/00 ,  C07D487/14 ,  C07D498/14 ,  C07D513/22

Abstract: Provided herein are compounds of the Formula (I): (I) and tautomers, stereoisomers and pharmaceutically acceptable salts and solvates thereof, wherein Rx, Ry, W, X, Y, Z, Ring A and (AA) 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：US11648243B2

公开(公告)日：2023-05-16

申请号：US17108528

申请日：2020-12-01

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: A61K31/4545 ,  A61K31/4162 ,  C07D471/04 ,  A61P1/00 ,  A61P35/00 ,  A61P35/02 ,  A61K31/444 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  A61P1/12

CPC classification number: A61K31/4545 ,  A61K31/4162 ,  A61K31/444 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  A61P1/00 ,  A61P1/12 ,  A61P35/00 ,  A61P35/02 ,  C07D471/04

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：US11603374B2

公开(公告)日：2023-03-14

申请号：US16962345

申请日：2019-01-18

Applicant: Array BioPharma Inc.

Inventor： James F. Blake ,  Donghua Dai ,  Julia Haas ,  Yutong Jiang ,  Gabrielle R. Kolakowski ,  Elizabeth A. McFaddin ,  Megan L. McKenney ,  Andrew T. Metcalf ,  David A. Moreno ,  Brett Prigaro ,  Ginelle A. Ramann ,  Li Ren

IPC: C07D487/04

Abstract: Provided herein are compounds of the Formula I: [INSERT FORMULA I] and tautomers, stereoisomers and pharmaceutically acceptable salts and solvates thereof, wherein R1, R2 and Ry 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：US11524963B2

公开(公告)日：2022-12-13

申请号：US16961973

申请日：2019-01-18

Applicant: Array Biopharma Inc.

Inventor： James F. Blake ,  Donghua Dai ,  Julia Haas ,  Yutong Jiang ,  Gabrielle R. Kolakowski ,  Andrew T. Metcalf ,  David A. Moreno ,  Brett Prigaro ,  Li Ren

IPC: A61K31/519 ,  C07D487/04

Abstract: Provided herein are compounds of the Formula I: and tautomers and pharmaceutically acceptable salts and solvates thereof, wherein R1 and R2 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：US11453683B1

公开(公告)日：2022-09-27

申请号：US17005004

申请日：2020-08-27

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: 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.