公开(公告)号：WO2003077855A3

公开(公告)日：2003-09-25

申请号：PCT/US2003/007565

申请日：2003-03-13

Applicant: ARRAY BIOPHARMA, INC ,  WALLACE, Eli, M. ,  LYSSIKATOS, Joseph, P. ,  HURLEY, Brian, T. ,  MARLOW, Allison, L.

Inventor： WALLACE, Eli, M. ,  LYSSIKATOS, Joseph, P. ,  HURLEY, Brian, T. ,  MARLOW, Allison, L.

IPC: A61K31/5377

Abstract: Disclosed are compounds of the formula (I) and pharmaceutically acceptable salts and prodrugs thereof, wherein W, t, R 1 , R 2 , R 7 , R 9 , R 10 , R 11 and R 12 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed is a method of using such compounds in the treatment of hyperproliferative diseases in mammals, and pharmaceutical compositions containing such compounds.

公开(公告)号：WO2022208408A1

公开(公告)日：2022-10-06

申请号：PCT/IB2022/052982

申请日：2022-03-30

Applicant: ARRAY BIOPHARMA INC.

Inventor： BROWN, Katie Keaton ,  GOODWIN, Aaron Keith

IPC: A61P35/00 ,  C07D471/14 ,  A61K31/53

Abstract: This invention relates to a hemihydrate crystalline form of (S)-1'-(6-((2-amino-3-chloropyridin-4-yl)thio)-1,2,4-triazin-3-yl)-1,3-dihydrospiro[indene-2,4'-piperidin]-1-amine free base (Form 1). The invention also relates to pharmaceutical compositions comprising this crystalline form, and to methods of using the crystalline form and such compositions for the treatment of abnormal cell growth, such as cancer, in a mammal.

公开(公告)号：WO2020261156A1

公开(公告)日：2020-12-30

申请号：PCT/IB2020/055992

申请日：2020-06-24

Applicant: ARRAY BIOPHARMA INC.

Inventor： BARBOUR, Patrick Michael ,  BROWN, Katie Keaton ,  COOK, Adam Wade ,  HICKEN, Erik James ,  KAHN, Dean Russell ,  LAIRD, Ellen Ruth ,  METCALF, Andrew Terrance ,  MORENO, David Austin ,  NEWHOUSE, Bradley Jon ,  PAJK, Spencer Phillip ,  PRIGARO, Brett Joseph ,  REN, Li ,  TARLTON, Eugene

IPC: C07D239/90 ,  A61P35/00 ,  C07D239/91 ,  C07D401/12 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07C271/28 ,  A61K31/517

Abstract: Provided herein are compounds of the Formula I: and pharmaceutically acceptable salts, solvates and polymorphs thereof, wherein L, X 1 , R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are as defined herein, for the treatment of BRAF-associated diseases and disorders, including BRAF-associated tumors, including malignant and benign BRAF-associated tumors of the CNS and malignant extracranial BRAF-associated tumors.

公开(公告)号：WO2019217307A1

公开(公告)日：2019-11-14

申请号：PCT/US2019/030896

申请日：2019-05-06

Applicant: MIRATI THERAPEUTICS, INC. ,  ARRAY BIOPHARMA INC.

Inventor： MARX, Matthew, Arnold ,  LEE, Matthew, Randolph ,  BLAKE, James, F. ,  CHICARELLI, Mark, Joseph ,  FELL, Jay, Bradford ,  FISHER, John, P. ,  HINKEN, Erik, James ,  SAVENCHENKOV, Pavel ,  TANG, Tony ,  VIGERS, Guy, P.A. ,  ZECCA, Henry, J.

IPC: A61K31/538 ,  C07D265/36 ,  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.

公开(公告)号：WO2018136663A1

公开(公告)日：2018-07-26

申请号：PCT/US2018/014281

申请日：2018-01-18

Applicant: ARRAY BIOPHARMA, INC.

Inventor： ANDREWS, Steven W. ,  BLAKE, James F. ,  HAAS, Julia ,  JIANG, Yutong

IPC: C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  A61P35/00 ,  A61K31/506

Abstract: Provided herein are compounds of the Formula (I): and pharmaceutically acceptable salts or solvates thereof, where A, B, Y, X 1 , X 2 , X 3 , X 4 , R 1 , R 2 , n and m are as defined 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：WO2016077841A1

公开(公告)日：2016-05-19

申请号：PCT/US2015/060953

申请日：2015-11-16

Applicant: ARRAY BIOPHARMA, INC. ,  ARRIGO, Alisha B. ,  JUENGST, Derrick ,  SHAH, Khalid

Inventor： ARRIGO, Alisha B. ,  JUENGST, Derrick ,  SHAH, Khalid

IPC: C07D487/04 ,  A61K31/519 ,  A61P35/00

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.

Abstract translation: （S）-N-（5 - （（R）-2-（2,5-二氟苯基）吡咯烷-1-基） - 吡唑并[1,5-a]嘧啶-3-基） - 3-羟基吡咯烷-1-甲酰胺，含有所述结晶形式的药物组合物和所述结晶形式用于治疗疼痛，癌症，炎症，神经变性疾病或克氏锥虫感染的用途。 在一些实施方案中，新的结晶形式包含（S）-N-（5 - （（R）-2-（2,5-二氟苯基）吡咯烷-1-基） - 吡唑并[1,5-a ]嘧啶-3-基）-3-羟基吡咯烷-1-甲酰胺硫酸氢盐。 本发明进一步涉及制备新型结晶形式的方法。

公开(公告)号：WO2015103133A1

公开(公告)日：2015-07-09

申请号：PCT/US2014/072547

申请日：2014-12-29

Applicant: GENENTECH, INC. ,  ARRAY BIOPHARMA INC.

Inventor： BLAKE, James, F. ,  COOK, Adam ,  GUNAWARDANA, Indrani, W. ,  HUNT, Kevin, W. ,  LYON, Michael ,  METCALF, Andrew, T. ,  MOHR, Peter, J. ,  MORENO, David, A. ,  NEWHOUSE, Brad ,  REN, Li ,  TANG, Tony, P. ,  THOMAS, Allen, A. ,  SCHWARZ, Jacob ,  SCHMIDT, Jane ,  GAZZARD, Lewis ,  CHEN, Huifen

IPC: A61P35/00 ,  A61K31/506 ,  C07D401/14 ,  C07D405/14 ,  C07D403/04 ,  C07D403/14 ,  C07D417/14

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.

Abstract translation: 提供式I化合物或其立体异构体，互变异构体或其药学上可接受的盐，其可用于治疗过度增殖，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：WO2014134313A1

公开(公告)日：2014-09-04

申请号：PCT/US2014/019039

申请日：2014-02-27

Applicant: ARRAY BIOPHARMA INC.

Inventor： EARY, Todd C. ,  HACHE, Bruno P. ,  JUENGST, Derrick ,  SPENCER, Stacey Renee ,  STENGEL, Peter J. ,  WATSON, Daniel John

IPC: C07D403/12 ,  C07D231/56 ,  A61K31/416 ,  A61P29/00

CPC classification number: C07D403/12 ,  C07D231/56

Abstract: Provided herein are novel processes for preparing a compound of Formula (I) to the use of said compound as an intermediate in novel processes for the synthesis of indazole derivatives, and to indazole intermediates and derivatives prepared by the processes described herein.

Abstract translation: 本文提供了制备式（I）化合物以在合成吲唑衍生物的新方法中使用所述化合物作为中间体的新方法，以及通过本文所述的方法制备的吲唑中间体和衍生物。

公开(公告)号：WO2014078408A1

公开(公告)日：2014-05-22

申请号：PCT/US2013/069886

申请日：2013-11-13

Applicant: ARRAY BIOPHARMA INC. ,  ALLEN, Shelley ,  BRANDHUBER, Barbara J. ,  CONDROSKI, Kevin Ronald ,  HUANG, Lily ,  KERCHER, Timothy ,  WINSKI, Shannon L.

Inventor： ALLEN, Shelley ,  BRANDHUBER, Barbara J. ,  CONDROSKI, Kevin Ronald ,  HUANG, Lily ,  KERCHER, Timothy ,  WINSKI, Shannon L.

IPC: C07D231/56 ,  C07D471/04 ,  C07D487/04 ,  C07D491/048 ,  C07D495/04 ,  A61K31/4985 ,  A61K31/437 ,  A61K31/416 ,  A61P29/00 ,  A61P35/00 ,  A61P25/00 ,  A61P31/00

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.

Abstract translation: 其中环A，环C和X如本文所定义的式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是TrkA激酶的抑制剂，并且可用于治疗可以用 一种TrkA激酶抑制剂，如疼痛，癌症，炎症/炎性疾病，神经变性疾病，某些传染病，干燥综合征，子宫内膜异位症，糖尿病性周围神经病变，前列腺炎和骨盆疼痛综合征。

公开(公告)号：WO2014078322A1

公开(公告)日：2014-05-22

申请号：PCT/US2013/069728

申请日：2013-11-12

Applicant: ARRAY BIOPHARMA INC. ,  BRANDHUBER, Barbara, J. ,  JIANG, Yutong ,  KOLAKOWSKI, Gabrielle, R. ,  WINSKI, Shannon, L.

Inventor： BRANDHUBER, Barbara, J. ,  JIANG, Yutong ,  KOLAKOWSKI, Gabrielle, R. ,  WINSKI, Shannon, L.

IPC: C07D263/48 ,  C07D277/46 ,  C07D403/12

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

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, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis or pelvic pain syndrome.

Abstract translation: 式（I）化合物或其立体异构体，互变异构体或其药学上可接受的盐，溶剂合物或前药，其中环A，环C和X如本文所定义，是TrkA激酶的抑制剂，并且可用于治疗可以 用TrkA激酶抑制剂治疗，如疼痛，癌症，炎症，神经变性疾病，某些传染病，干燥综合征，子宫内膜异位症，糖尿病性周围神经病变，前列腺炎或盆腔疼痛综合征。