公开(公告)号：US10329288B2

公开(公告)日：2019-06-25

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

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

公开(公告)号：US20180282324A1

公开(公告)日：2018-10-04

申请号：US15806650

申请日：2017-11-08

Applicant: Genentech, Inc. ,  Array Biopharma Inc.

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

IPC: 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.

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：US20170231963A1

公开(公告)日：2017-08-17

申请号：US15445393

申请日：2017-02-28

Applicant: 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: A61K31/4184 ,  A61K9/00 ,  A61K9/20 ,  A61K45/06

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：US20160168104A1

公开(公告)日：2016-06-16

申请号：US15053441

申请日：2016-02-25

Applicant: Novartis Pharma 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: C07D235/08

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.

Abstract translation: 本发明涉及制备6-（4-溴-2-氟苯基氨基）-7-氟-3-甲基-3H-苯并咪唑-5-甲酸（2-羟基乙氧基） - 酰胺的方法， （4-溴-2-氟苯基氨基）-7-氟-3-甲基-3H-苯并咪唑-5-甲酸（2-羟基乙氧基） - 酰胺，以及有用的中间体。 本文还提供包含该结晶化合物的药物组合物。

公开(公告)号：US20160168102A1

公开(公告)日：2016-06-16

申请号：US14974588

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 ,  C30B29/54 ,  C30B7/08

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.

Abstract translation: 本发明涉及制备6-（4-溴-2-氟苯基氨基）-7-氟-3-甲基-3H-苯并咪唑-5-甲酸（2-羟基乙氧基） - 酰胺的方法， （4-溴-2-氟苯基氨基）-7-氟-3-甲基-3H-苯并咪唑-5-甲酸（2-羟基乙氧基） - 酰胺，以及有用的中间体。 本文还提供包含该结晶化合物的药物组合物。

公开(公告)号：US09238627B2

公开(公告)日：2016-01-19

申请号：US14057498

申请日：2013-10-18

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 ,  A61K47/26 ,  A61K47/38 ,  A61K9/20

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.

Abstract translation: 本发明涉及制备6-（4-溴-2-氟苯基氨基）-7-氟-3-甲基-3H-苯并咪唑-5-甲酸（2-羟基乙氧基） - 酰胺的方法， （4-溴-2-氟苯基氨基）-7-氟-3-甲基-3H-苯并咪唑-5-甲酸（2-羟基乙氧基） - 酰胺，以及有用的中间体。 本文还提供包含该结晶化合物的药物组合物。

公开(公告)号：US11807651B2

公开(公告)日：2023-11-07

申请号：US17401892

申请日：2021-08-13

Applicant: Loxo Oncology, Inc. ,  Array BioPharma Inc.

Inventor： Charles Todd Eary ,  Stacey Spencer ,  Zack Crane ,  Katelyn Chando ,  Sylvie Asselin ,  Weidong Liu ,  Mike Welch ,  Adam Cook ,  Gabrielle R. Kolakowski ,  Andrew T. Metcalf ,  David A. Moreno ,  Tony P. Tang

IPC: C07D519/00 ,  C07D471/04

CPC classification number: C07D519/00 ,  C07D471/04

Abstract: In some embodiments, provided herein is a process for preparing a compound of Formula I




or a pharmaceutically acceptable salt thereof, as disclosed herein.

公开(公告)号：US11098064B2

公开(公告)日：2021-08-24

申请号：US16902424

申请日：2020-06-16

Applicant: Loxo Oncology, Inc. ,  Array BioPharma Inc.

Inventor： Charles Todd Eary ,  Stacey Spencer ,  Zack Crane ,  Katelyn Chando ,  Sylvie Asselin ,  Weidong Liu ,  Mike Welch ,  Adam Cook ,  Gabrielle R. Kolakowski ,  Andrew T. Metcalf ,  David A. Moreno ,  Tony P. Tang

IPC: C07D519/00 ,  C07D471/04

Abstract: In some embodiments, provided herein is a process for preparing a compound of Formula I or a pharmaceutically acceptable salt thereof, as disclosed herein.

公开(公告)号：US10729678B2

公开(公告)日：2020-08-04

申请号：US16512823

申请日：2019-07-16

Applicant: 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 ,  A61K31/4184 ,  A61K9/20 ,  A61K9/00 ,  C07D235/08 ,  A61K47/12 ,  A61K47/02 ,  C30B29/54 ,  C30B7/08 ,  A61K47/38 ,  A61K47/26 ,  A61K45/06

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.