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：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：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：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：US09359340B2

公开(公告)日：2016-06-07

申请号：US14458062

申请日：2014-08-12

Applicant: Array BioPharma Inc. ,  Genentech, Inc.

Inventor： Ian S. Mitchell ,  James F. Blake ,  Rui Xu ,  Nicholas C. Kallan ,  Dengming Xiao ,  Keith Lee Spencer ,  Josef R. Bencsik ,  Eli M. Wallace ,  Stephen T. Schlachter ,  Anna L. Leivers ,  Jun Liang ,  Brian Safina ,  Birong Zhang ,  Christine Chabot ,  Steven Do

IPC: C07D239/70 ,  C07D403/04 ,  C07D413/12 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D407/12 ,  A61P29/00 ,  A61P35/00 ,  A61P9/00 ,  A61P25/28 ,  A61P15/00 ,  A61P17/00 ,  A61K31/517 ,  A61K31/496

CPC classification number: A61K31/517 ,  C07D239/70 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D407/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12

Abstract: The present invention provides compounds, including resolved enantiomers, resolved diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula I: Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.

Abstract translation: 本发明提供了包含分解的对映异构体，分解的非对映异构体，溶剂合物和其药学上可接受的盐的化合物，其包含式I：还提供了使用本发明化合物作为AKT蛋白激酶抑制剂和用于治疗过度增殖性疾病 癌症。

公开(公告)号：US20160152601A9

公开(公告)日：2016-06-02

申请号：US14086717

申请日：2013-11-21

Applicant: Array BioPharma Inc. ,  Genentech, Inc.

Inventor： Josef Bencsik ,  James F. Blake ,  James M. Graham ,  Martin F. Hentemann ,  Nicholas C. Kallan ,  Ian S. Mitchell ,  Stephen T. Schlachter ,  Keith L. Spencer ,  Dengming Xiao ,  Rui Xu ,  Mike Welch ,  Jun Liang ,  Brian S. Safina

IPC: C07D403/12 ,  C07D403/14 ,  C07D409/14 ,  C07D413/12 ,  C07D401/12 ,  C07D405/14

CPC classification number: C07D403/12 ,  C07D401/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/12

Abstract: The present invention provides compounds of Formula I, including tautomers, resolved enantiomers, diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.

公开(公告)号：US09227975B2

公开(公告)日：2016-01-05

申请号：US13614968

申请日：2012-09-13

Applicant: Steven W. Andrews ,  Julia Haas ,  Yutong Jiang ,  Gan Zhang

Inventor： Steven W. Andrews ,  Julia Haas ,  Yutong Jiang ,  Gan Zhang

IPC: A01N43/58 ,  A01N43/60 ,  A61K31/495 ,  C07D487/04 ,  C07D471/04

CPC classification number: C07D487/04 ,  A61K31/5025 ,  A61K31/5377 ,  A61K31/541 ,  C07C51/412 ,  C07C53/18 ,  C07D471/04 ,  C07D519/00

Abstract: Methods for treating a disease or disorder selected from pain, cancer, inflammation, neurodegenerative disease, Typanosoma cruzi infection and osteolytic disease in a mammal, which comprise administering to said mammal a therapeutically effective amount of a compound of Formula I in which R1, R2, R3, R4, X, Y and n have the meanings given in the specification.

Abstract translation: 治疗哺乳动物选自疼痛，癌症，炎症，神经变性疾病，克氏锥虫感染和溶骨性疾病的疾病或病症的方法，其包括向所述哺乳动物施用治疗有效量的式I化合物，其中R1，R2， R3，R4，X，Y和n具有说​​明书中给出的含义。

公开(公告)号：US20150087664A1

公开(公告)日：2015-03-26

申请号：US14237143

申请日：2012-08-03

Applicant: James F. Blake ,  Huifen Chen ,  Mark Joseph Chicarelli ,  Jason Demeese ,  Rustam Ferdinand Garrey ,  John Gaudino ,  Lewis Gazzard ,  Robert J. Kaus ,  Samuel Kintz ,  Peter J. Mohr ,  David A. Moreno ,  Jacob Schwartz ,  Christopher S. Siedem ,  Eli M. Wallace

Inventor： James F. Blake ,  Huifen Chen ,  Mark Joseph Chicarelli ,  Jason Demeese ,  Rustam Ferdinand Garrey ,  John Gaudino ,  Lewis Gazzard ,  Robert J. Kaus ,  Samuel Kintz ,  Peter J. Mohr ,  David A. Moreno ,  Jacob Schwartz ,  Christopher S. Siedem ,  Eli M. Wallace

IPC: C07D405/14 ,  C07D403/12

CPC classification number: C07D405/14 ,  C07D403/12

Abstract: Compounds having the formula (I) wherein R1, R2, R3 and Ar 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R1，R2，R3和Ar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：US08962596B2

公开(公告)日：2015-02-24

申请号：US13640099

申请日：2011-04-11

Applicant: Laurence E. Burgess ,  Mark Laurence Boys ,  Robert D. Groneberg ,  Darren M. Harvey ,  Timothy Kercher ,  Christopher F. Kraser ,  Ellen Laird ,  Eugene Tarlton ,  Qian Zhao ,  Lily Huang

Inventor： Laurence E. Burgess ,  Mark Laurence Boys ,  Robert D. Groneberg ,  Darren M. Harvey ,  Timothy Kercher ,  Christopher F. Kraser ,  Ellen Laird ,  Eugene Tarlton ,  Qian Zhao ,  Lily Huang

IPC: C07D487/04 ,  A61K31/519 ,  A61P29/00 ,  A61P35/00 ,  A61P37/06 ,  C07D498/04

CPC classification number: C07D487/04 ,  C07D498/04

Abstract: Compounds of Formula I: and stereoisomers and pharmaceutically acceptable salts and solvates thereof in which R1, R2, R3, R4, R5, R6, R7, X1 and X2 have the meanings given in the specification, are inhibitors of one or more JAK kinases and are useful in the treatment of autoimmune diseases, inflammatory diseases, rejection of transplanted organs, tissues and cells, as well as hematologic disorders and malignancies and their co-morbidities.

Abstract translation: 式I化合物及其其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，X 1和X 2具有本说明书中给出的含义的立体异构体及其药学上可接受的盐和溶剂化物是一种或多种JAK激酶的抑制剂， 可用于治疗自身免疫性疾病，炎性疾病，移植器官，组织和细胞排斥，以及血液系统疾病和恶性肿瘤及其并发症。