公开(公告)号：US09447104B2

公开(公告)日：2016-09-20

申请号：US14490460

申请日：2014-09-18

Applicant: Array BioPharma Inc.

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

IPC: C07D487/04 ,  C07D519/00 ,  C07D471/04 ,  A61K31/519

CPC classification number: C07D487/04 ,  A61K9/0053 ,  A61K31/519 ,  A61K31/5377 ,  A61K45/06 ,  A61P29/00 ,  C07D471/04 ,  C07D519/00

Abstract: Compounds useful in the synthesis of compounds for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal.

Abstract translation: 用于合成用于治疗哺乳动物疼痛，癌症，炎症，神经变性疾病或克氏锥虫感染的化合物的化合物。

公开(公告)号：US20160251350A1

公开(公告)日：2016-09-01

申请号：US15054611

申请日：2016-02-26

Applicant: Genentech, Inc. ,  Array Biopharma Inc.

Inventor： Jeffrey Stults ,  Christopher M. Lindemann ,  Keith L. Spencer ,  Weidong Liu ,  Joseph Lubach

IPC: C07D471/04 ,  A61K45/06 ,  A61K31/437

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

Abstract: Disclosed are crystalline forms of (R)—N-(4-(3-aminopiperidin-1-yl)-5-bromo-1H-pyrrolo[2,3-b]pyridin-3-yl)cyclopropanecarboxamide, and salts, solvates, and hydrates thereof, and pharmaceutical compositions, formulations and a process of manufacturing thereof.

Abstract translation: 公开了（R）-N-（4-（3-氨基哌啶-1-基）-5-溴-1H-吡咯并[2,3-b]吡啶-3-基）环丙烷甲酰胺和盐，溶剂化物的结晶形式 及其水合物，以及药物组合物，制剂及其制造方法。

公开(公告)号：US20160235754A1

公开(公告)日：2016-08-18

申请号：US15140874

申请日：2016-04-28

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: A61K31/517

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 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: 本发明提供包括拆分的对映异构体，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，其包含式还提供使用本发明化合物作为AKT蛋白激酶抑制剂和治疗过度增殖性疾病如癌症的方法。

公开(公告)号：US09409886B2

公开(公告)日：2016-08-09

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 ,  C07D401/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/12 ,  C07D403/14 ,  A61P35/02 ,  A61P35/04 ,  A61P29/00 ,  A61P9/00 ,  A61P25/28 ,  A61P35/00 ,  A61P25/16 ,  A61P31/04 ,  A61P37/06 ,  A61P37/08 ,  A61P17/06 ,  A61P11/06

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：US09382212B1

公开(公告)日：2016-07-05

申请号：US14974588

申请日：2015-12-18

Applicant: Novartis AG ,  Array BioPharma, Inc.

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 ,  C30B7/08 ,  C30B29/54

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：US20160175309A1

公开(公告)日：2016-06-23

申请号：US14923172

申请日：2015-10-26

Applicant: Array BioPharma Inc.

Inventor： Donald T. Corson ,  Christopher M. Lindemann ,  Daniel J. Watson

IPC: A61K31/517 ,  A61K45/06

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.

Abstract translation: N 4 - （4 - （[1,2,4]三唑并[1,5-a]吡啶-7-基氧基）-3-甲基苯基）-N6-（4,4-二甲基-4,5-二氢恶唑-2-基） 吡啶-2-基）喹唑啉-4,6-二胺。 还公开了制备多晶型物的方法和包含多晶型物的药物组合物。

公开(公告)号：US20160152606A9

公开(公告)日：2016-06-02

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: C07D413/12 ,  C07D401/12 ,  C07D409/14 ,  C07D407/12 ,  C07D409/12 ,  C07D239/70 ,  C07D403/12

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：US20160152576A9

公开(公告)日：2016-06-02

申请号：US14170272

申请日：2014-01-31

Applicant: Array BioPharma, Inc.

Inventor： Ian S. Mitchell ,  Keith L. Spencer ,  Peter Stengel ,  Yongxin Han ,  Nicolas C. Kallan ,  Mark Munson ,  Guy P.A. Vigers ,  James Blake ,  Anthony Piscopio ,  John Josey ,  Scott Miller ,  Dengming Xiao ,  Rui Xu ,  Chang Rao ,  Bing Wang ,  April L. Bernacki

IPC: C07D239/94 ,  C07D403/12 ,  C07D495/04 ,  C07D491/048 ,  C07D231/56 ,  C07D401/12 ,  C07D409/04 ,  C07D401/04 ,  C07D409/12 ,  C07D487/04

CPC classification number: C07D239/94 ,  B41M3/008 ,  B44F1/10 ,  C07D231/56 ,  C07D237/28 ,  C07D239/42 ,  C07D239/47 ,  C07D239/48 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D409/04 ,  C07D409/12 ,  C07D471/04 ,  C07D487/04 ,  C07D491/048 ,  C07D495/04 ,  G09F13/16 ,  Y10T428/24802 ,  Y10T428/24851 ,  Y10T428/25 ,  Y10T428/31507 ,  Y10T428/31551 ,  Y10T428/31786 ,  Y10T428/31855

Abstract: The present invention provides compounds, including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula: A-L-CR where CR is a cyclical core group, L is a linking group and A is as defined herein. 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: 本发明提供包括分解对映异构体，非对映异构体，溶剂化物和药学上可接受的盐的化合物，其包含式为：A-L-CR，其中CR为环状核心基团，L为连接基团，A如本文所定义。 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过度增殖性疾病如癌症的方法。

公开(公告)号：US09259470B2

公开(公告)日：2016-02-16

申请号：US14181418

申请日：2014-02-14

Applicant: Array BioPharma Inc. ,  Genentech, Inc.

Inventor： James F. Blake ,  Mark Joseph Chicarelli ,  Rustam Ferdinand Garrey ,  John Gaudino ,  Jonas Grina ,  David A. Moreno ,  Peter J. Mohr ,  Li Ren ,  Jacob Schwarz ,  Huifen Chen ,  Kirk Robarge ,  Aihe Zhou

IPC: A61K45/06 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D401/04 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04 ,  A61K31/506 ,  C07F9/6558 ,  C07D403/04 ,  A61K31/513 ,  A61K31/53 ,  A61K31/444

CPC classification number: C07D401/04 ,  A61K31/444 ,  A61K31/506 ,  A61K31/513 ,  A61K31/53 ,  A61K45/06 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07F9/65586

Abstract: Compounds of Formula I or a stereoisomer, tautomer, prodrug 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, prodrug 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，前药或其药学上可接受的盐，其可用于治疗过度增生，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，前药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：US20160002232A1

公开(公告)日：2016-01-07

申请号：US14858029

申请日：2015-09-18

Applicant: ARRAY BIOPHARMA INC.

Inventor： Mark Laurence Boys ,  Robert Kirk DeLisle ,  Erik James Hicken ,  April L. Kennedy ,  David A. Mareska ,  Fredrik P. Marmsater ,  Mark C. Munson ,  Brad Newhouse ,  Bryson Rast ,  James P. Rizzi ,  Martha E. Rodriguez ,  George T. Topalov ,  Qian Zhao

IPC: C07D471/04 ,  A61K45/06 ,  A61K31/496

CPC classification number: C07D471/04 ,  A61K31/496 ,  A61K45/06

Abstract: Compounds useful in the treatment of fibrosis, bone-related diseases, cancer, autoimmune disorders, inflammatory diseases, cardiovascular diseases, pain and burns in a mammal.

Abstract translation: 用于治疗哺乳动物纤维化，骨相关疾病，癌症，自身免疫疾病，炎性疾病，心血管疾病，疼痛和灼伤的化合物。