公开(公告)号：US20180179182A1

公开(公告)日：2018-06-28

申请号：US15851418

申请日：2017-12-21

Applicant: Array BioPharma Inc.

Inventor： Shelley Allen ,  Barbara J. Brandhuber ,  Timothy Kercher ,  Gabrielle R. Kolakowski ,  Shannon L. Winski

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

CPC classification number: C07D401/14 ,  A61P29/00 ,  A61P35/00 ,  C07D403/12 ,  C07D403/14

Abstract: Compounds useful for the treatment of pain or cancer in a mammal.

公开(公告)号：US20180140603A1

公开(公告)日：2018-05-24

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: A61K31/517 ,  A61K45/06 ,  C07D471/04

CPC classification number: A61K31/517 ,  A61K31/437 ,  A61K45/06 ,  A61P35/00 ,  C07D471/04

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：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：US09850229B2

公开(公告)日：2017-12-26

申请号：US15179385

申请日：2016-06-10

Applicant: Array BioPharma, Inc.

Inventor： Shenlin Huang ,  Xianming Jin ,  Zuosheng Liu ,  Daniel Poon ,  John Tellew ,  Yongqin Wan ,  Xing Wang ,  Yongping Xie

IPC: C07D401/00 ,  C07D403/04 ,  C07D401/14 ,  A61K31/506 ,  A61K45/06 ,  C07D405/14 ,  A61K9/00 ,  A61K31/4184

CPC classification number: C07D403/04 ,  A61K9/0053 ,  A61K31/4184 ,  A61K31/506 ,  A61K45/06 ,  C07D401/14 ,  C07D405/14 ,  A61K2300/00

Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of B-Raf.

公开(公告)号：US09822118B2

公开(公告)日：2017-11-21

申请号：US14442503

申请日：2013-11-13

Applicant: Array BioPharma Inc.

Inventor： Shelley Allen ,  Barbara J. Brandhuber ,  Kevin Ronald Condroski ,  Lily Huang ,  Timothy Kercher ,  Shannon L. Winski

IPC: C07D487/04 ,  C07D231/56 ,  C07D471/04 ,  C07D491/048 ,  C07D495/04 ,  C07D403/12 ,  C07D519/00

CPC classification number: C07D487/04 ,  C07D231/56 ,  C07D403/12 ,  C07D471/04 ,  C07D491/048 ,  C07D495/04 ,  C07D519/00

Abstract: Compounds of Formula I or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C and X 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 and pelvic pain syndrome.

公开(公告)号：US09790210B2

公开(公告)日：2017-10-17

申请号：US14442604

申请日：2013-11-12

Applicant: Array BioPharma Inc.

Inventor： Steven Wade Andrews ,  James F. Blake ,  Barbara J. Brandhuber ,  Timothy Kercher ,  Shannon L. Winski

IPC: C07D231/00 ,  C07D403/00 ,  C07D401/00 ,  C07D211/72 ,  C07D413/00 ,  C07D405/12 ,  C07D403/12 ,  C07D401/14 ,  C07D231/40 ,  C07D231/44 ,  C07D401/04 ,  C07D413/12 ,  C07D231/52 ,  C07D401/12 ,  C07D405/04 ,  A61K31/4155

CPC classification number: C07D405/12 ,  A61K31/4155 ,  C07D231/40 ,  C07D231/44 ,  C07D231/52 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/04 ,  C07D413/12

Abstract: Compounds of Formula (I) or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C and X 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.

公开(公告)号：US09782414B2

公开(公告)日：2017-10-10

申请号：US15399207

申请日：2017-01-05

Applicant: Array BioPharma, Inc.

Inventor： Alisha B. Arrigo ,  Derrick Juengst ,  Khalid Shah

IPC: A01N43/90 ,  A61K31/519 ,  C07D487/00 ,  C12Q1/48

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

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：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：US09750744B2

公开(公告)日：2017-09-05

申请号：US15401952

申请日：2017-01-09

Applicant: Array BioPharma, Inc.

Inventor： Steven W. Andrews ,  Kevin Ronald Condroski ,  Julia Haas ,  Yutong Jiang ,  Gabrielle R. Kolakowski ,  Jeongbeob Seo ,  Hong-Woon Yang ,  Qian Zhao

IPC: A61K31/519

CPC classification number: C07D498/22 ,  A61K31/519 ,  C07D471/22 ,  C07D487/04 ,  C07D487/22 ,  C07D519/00

Abstract: Compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein ring A, ring B, W, m, D, R2, R2a, R3, R3a, and Z are as defined herein, are inhibitors of Trk kinases and are useful in the treatment of pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.

公开(公告)号：US20170217936A1

公开(公告)日：2017-08-03

申请号：US15382028

申请日：2016-12-16

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 ,  C07D405/14 ,  C07D403/14 ,  C07D409/14 ,  C07D495/04 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/048 ,  C07D401/14 ,  C07D417/14

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.