公开(公告)号：US09457093B2

公开(公告)日：2016-10-04

申请号：US14351840

申请日：2012-10-12

Applicant: Array BioPharma Inc.

Inventor： David Shank Fry ,  Christopher M. Lindemann ,  Michael Preigh ,  Corey Jay Bloom ,  Christopher Donovan Craig ,  Devon Brevard Dubose ,  Jeff Gautschi ,  Dan Smithey

IPC: A61K47/38 ,  A61K31/517 ,  A61K47/32 ,  A61K9/10 ,  A61K9/20 ,  A61K9/16

CPC classification number: A61K31/517 ,  A61K9/0053 ,  A61K9/10 ,  A61K9/1635 ,  A61K9/1652 ,  A61K9/2009 ,  A61K9/2027 ,  A61K9/2054 ,  A61K9/2077 ,  A61K47/32 ,  A61K47/38

Abstract: A solid dispersion 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 and processes for preparing the solid dispersion are provided herein. Also, a pharmaceutical composition comprising a solid dispersion of N4-(4-([1,2,4]triazolo[1,5-α]pyridin-7-yloxy)-3-methylphenyl)-N6-(4,4-dimethyl-4,5-dihydrooxazol-2-yl)quinazoline-4,6-diamine and uses thereof are provided herein.

公开(公告)号：US20160280702A1

公开(公告)日：2016-09-29

申请号：US14442488

申请日：2013-11-12

Applicant: ARRAY BIOPHARMA INC.

Inventor： Barbara J. Brandhuber ,  Yutong Jiang ,  Gabrielle R. Kolakowski ,  Shannon L. Winski

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

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.

公开(公告)号：US20160280681A1

公开(公告)日：2016-09-29

申请号：US14442584

申请日：2013-11-12

Applicant: ARRAY BIOPHARMA INC.

Inventor： Shelley Allen ,  James F. Blake ,  Barbara J. Brandhuber ,  Yutong Jiang ,  Gabrielle R. Kolakowski ,  Rui Xu ,  Shannon L. Winski

IPC: C07D401/14 ,  C07D231/56 ,  C07D231/52 ,  C07D403/04 ,  C07D401/12 ,  C07D401/04 ,  C07D231/40

CPC classification number: C07D401/14 ,  C07D231/40 ,  C07D231/44 ,  C07D231/52 ,  C07D231/56 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04

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：US20160251357A1

公开(公告)日：2016-09-01

申请号：US14984353

申请日：2015-12-30

Applicant: Array BioPharma, Inc.

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

IPC: C07D487/04 ,  C07C53/18 ,  C07C51/41 ,  C07D519/00

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：US09416110B2

公开(公告)日：2016-08-16

申请号：US14401087

申请日：2013-05-17

Applicant: Array BioPharma Inc. ,  Genentech, Inc.

Inventor： David Askin ,  Chong Han ,  Jonathan W. Lane ,  Travis Remarchuk ,  Sagar Shakya ,  C. Gregory Sowell ,  Keith L. Spencer ,  Peter J. Stengel

IPC: C07D239/02 ,  C07D239/42 ,  C07D239/30 ,  C07D403/04 ,  C07D239/70

CPC classification number: C07D239/42 ,  C07D239/30 ,  C07D239/70 ,  C07D403/04

Abstract: The invention provides processes for preparing a compound of formula I and salts thereof, wherein R1 is defined herein, and compounds and intermediates of said formula.

Abstract translation: 本发明提供制备式I化合物及其盐的方法，其中R 1在本文中定义，以及所述式的化合物和中间体。

公开(公告)号：US20160200723A1

公开(公告)日：2016-07-14

申请号：US14913635

申请日：2014-08-21

Applicant: GENENTECH, INC. ,  ARRAY BIOPHARMA INC.

Inventor： Chong HAN ,  Keena GREEN ,  Francis GOSSELIN ,  Michelangelo SCALONE ,  Paul J. NICHOLS ,  Weidong LIU ,  Keith L. SPENCER ,  Zackary D. CRANE ,  Peter J. STENGEL ,  Sagar SHAKYA

IPC: C07D471/04

CPC classification number: C07D471/04

Abstract: The invention provides processes of preparation thereof useful in the preparation of compounds that can be used as CHK1 inhibitors.

Abstract translation: 本发明提供了可用于制备可用作CHK1抑制剂的化合物的制备方法。

公开(公告)号：US20160168103A1

公开(公告)日：2016-06-16

申请号：US14974655

申请日：2015-12-18

Applicant: Array BioPharma, Inc. ,  Novartis Pharma AG

Inventor： Christoph Max Krell ,  Marian Misun ,  Daniel Andreas Niederer ,  Werner Heinz Pachinger ,  Marie-Christine Wolf ,  Daniel Zimmermann ,  Weidong Liu ,  Peter J. Stengel ,  Paul Nichols

IPC: C07D235/06 ,  A61K47/12 ,  A61K47/02 ,  A61K47/26 ,  A61K47/38

CPC classification number: A61K31/4184 ,  A61K9/0053 ,  A61K9/2009 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2054 ,  A61K45/06 ,  A61K47/02 ,  A61K47/12 ,  A61K47/26 ,  A61K47/38 ,  C07B2200/13 ,  C07D235/06 ,  C07D235/08 ,  C30B7/08 ,  C30B29/54

Abstract: The present invention relates to processes for preparing 6-(4-bromo-2-fluorophenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxyethyoxy)-amide, processes for preparing crystallized 6-(4-bromo-2-fluorophenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxyethyoxy)-amide, and intermediates useful therefore. Also provided herein are pharmaceutical compositions comprising this crystallized compound.

公开(公告)号：US09346805B2

公开(公告)日：2016-05-24

申请号：US13676963

申请日：2012-11-14

Applicant: Array BioPharma Inc.

Inventor： Anna Banka ,  Josef R. Bencsik ,  James F. Blake ,  Kin Chiu Fong ,  Martin F. Hentemann ,  Ian S. Mitchell ,  Douglas McCord Sammond ,  Tony P. Tang ,  Eli M. Wallace ,  Rui Xu ,  James Graham

IPC: C07D471/10 ,  C07D487/10

CPC classification number: C07D471/10 ,  C07D487/10

Abstract: The present invention provides compounds of Formula I including tautomers, resolved enantiomers, resolved 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 Akt-mediated diseases, for example, hyperproliferative diseases such as cancer.

Abstract translation: 本发明提供式I化合物，其包括互变异构体，拆分的对映异构体，拆分的非对映体，溶剂合物，代谢物，盐和药学上可接受的前药。 还提供了使用本发明化合物作为Akt蛋白激酶抑制剂和治疗Akt介导的疾病例如过度增殖性疾病如癌症的方法。

公开(公告)号：US09309204B2

公开(公告)日：2016-04-12

申请号：US14401091

申请日：2013-05-17

Applicant: Array BioPharma Inc. ,  Genentech, Inc.

Inventor： Jonathan W. Lane ,  Travis Remarchuk ,  Sagar Shakya ,  Keith L. Spencer ,  Peter J. Stengel

IPC: C07D403/04 ,  C07D239/70 ,  C07D239/42

CPC classification number: C07D239/70 ,  C07D239/42 ,  C07D403/04

Abstract: The invention provides new processes for making and purifying hydroxylated cyclopenta[d]pyrimidine compounds, which are useful for the treatment of diseases such as cancer as AKT protein kinase inhibitors, including the compound (S)-2-(4-chlorophenyl)-1-(4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazin-1-yl)-3-(isopropylamino)propan-1-one.

Abstract translation: 本发明提供了用于制备和纯化羟基化环戊二烯并[d]嘧啶化合物的新方法，其可用于治疗诸如癌症的疾病作为AKT蛋白激酶抑制剂，包括化合物（S）-2-（4-氯苯基）-1 - （4 - （（5R，7R）-7-羟基-5-甲基-6,7-二氢-5H-环戊二烯并[d]嘧啶-4-基）哌嗪-1-基）-3-（异丙基氨基） -1。

公开(公告)号：US09221841B2

公开(公告)日：2015-12-29

申请号：US14663286

申请日：2015-03-19

Applicant: Array BioPharma Inc.

Inventor： Jeremy Hans ,  Eli M. Wallace ,  Qian Zhao ,  Shelley Allen ,  Ellen Laird ,  Joseph P. Lyssikatos ,  John E. Robinson ,  Christopher P. Corrette ,  Robert Kirk DeLisle ,  Walter C. Voegtli

IPC: C07D417/04 ,  C07D417/14 ,  C07D285/12 ,  C07D471/04 ,  C07D419/04 ,  C07D487/04 ,  C07D513/04 ,  C07D495/04 ,  C07F9/6539 ,  C07D497/04

CPC classification number: C07D513/04 ,  C07D285/12 ,  C07D417/04 ,  C07D417/14 ,  C07D419/04 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D497/04 ,  C07F9/65395

Abstract: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.

Abstract translation: 本发明涉及有丝分裂驱动蛋白抑制剂，特别是KSP，以及制备这些抑制剂的方法。 本发明还提供包含本发明抑制剂的药物组合物和利用抑制剂和药物组合物治疗和预防各种疾病的方法。