Abstract: Compounds of Formula I are useful for inhibiting AKT protein kinases. Methods of using compounds of Formula I and stereoisomers and pharmaceutically acceptable salts 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.
Type:
Grant
Filed:
October 24, 2014
Date of Patent:
May 3, 2016
Assignees:
GENENTECH, INC., ARRAY BIOPHARMA INC.
Inventors:
Anna Leivers, Josef R. Bencsik, James F. Blake, Martin F. Hentemann, Nicholas C. Kallan, Jun Liang, Ian S. Mitchell, Stephen T. Schlachter, Eli M. Wallace, Rui Xu, Tony P. Tang
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.
Type:
Grant
Filed:
May 17, 2013
Date of Patent:
April 12, 2016
Assignees:
ARRAY BIOPHARMA INC., GENENTECH, INC.
Inventors:
Jonathan W. Lane, Travis Remarchuk, Sagar Shakya, Keith L. Spencer, Peter J. Stengel
Abstract: The present invention provides compounds, including resolved enantiomers, 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.
Type:
Grant
Filed:
July 5, 2007
Date of Patent:
April 5, 2016
Assignee:
ARRAY BIOPHARMA INC.
Inventors:
Ian S. Mitchell, James F. Blake, Rui Xu, Nicholas C. Kallan, Dengming Xiao, Keith Lee Spencer, Josef R. Bencsik
Abstract: Provided herein is a hydrogen chloride salt of 1-(3-/t?r/-butyl-1-p-tolyl-1H-pyrazol-5-yl)-3-(5-fluoro-2-(1-(2-hydroxyethyl)-1H-indazol-5-yloxy)benzyl)urea, crystalline forms of 1-(3-½^butyl-1^-tolyl-1H-pyrazol-5-yl)-3-(5-fluoro-2-(1-(2-hydroxyethyl)-1H-indazol-5-yloxy)benzyl)urea hydrochloride, processes for the preparation of said crystalline forms, pharmaceutical compositions containing a crystalline form of 1-(3-r<i/-r-butyl-1-p-tolyl-1H-pyrazol-5-yl)-3-(5-fluoro-2-(1-(2-hydroxyethyl)-1H-indazol-5-yloxy)benzyl)urea hydrochloride Form B, processes for the preparation of said compositions, pharmaceutical compositions prepared by said methods, and the use of said compositions in the treatment of various diseases and disorders.
Type:
Grant
Filed:
February 27, 2013
Date of Patent:
March 8, 2016
Assignee:
ARRAY BIOPHARMA INC.
Inventors:
Alisha B. Arrigo, Donald T. Corson, Coralee G. Mannila
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.
Type:
Grant
Filed:
February 14, 2014
Date of Patent:
February 16, 2016
Assignees:
Array BioPharma Inc., Genentech, Inc.
Inventors:
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
Abstract: Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in treating or preventing disease, including cancer, autoimmune disease, infectious disease, inflammatory disorder, graft rejection, and graft-verses-host disease.
Type:
Grant
Filed:
September 3, 2013
Date of Patent:
January 26, 2016
Assignees:
VENTIRX PHARMACEUTICALS, INC., ARRAY BIOPHARMA, INC.
Inventors:
James Jeffry Howbert, Gregory Dietsch, Robert M. Hershberg, Laurence E. Burgess, George A. Doherty, C. Todd Eary, Robert D. Groneberg, Zachary Jones
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.
Type:
Grant
Filed:
October 18, 2013
Date of Patent:
January 19, 2016
Assignees:
Array BioPharma, Inc., Novartis AG
Inventors:
Christoph Max Krell, Marian Misun, Daniel Andreas Niederer, Werner Heinz Pachinger, Marie-Christine Wolf, Daniel Zimmermann, Weidong Liu, Peter J. Stengel, Paul Nichols
Abstract: Compounds useful in the treatment of fibrosis, bone-related diseases, cancer, autoimmune disorders, inflammatory diseases, cardiovascular diseases, pain and burns in a mammal.
Type:
Application
Filed:
September 18, 2015
Publication date:
January 7, 2016
Applicant:
ARRAY BIOPHARMA INC.
Inventors:
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
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.
Type:
Application
Filed:
February 27, 2014
Publication date:
January 7, 2016
Applicant:
Array BioPharma Inc.
Inventors:
Todd C. Eary, Bruno P. Hache, Derrick Juengst, Stacey Renee Spencer, Peter J. Stengel, Daniel John Watson
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.
Type:
Grant
Filed:
September 13, 2012
Date of Patent:
January 5, 2016
Assignee:
Array BioPharma, Inc.
Inventors:
Steven W. Andrews, Julia Haas, Yutong Jiang, Gan Zhang
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.
Type:
Grant
Filed:
March 19, 2015
Date of Patent:
December 29, 2015
Assignee:
Array BioPharma Inc.
Inventors:
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
Abstract: Compounds having the formula (I) wherein R1, R2, R3 and Ar as defined herein are inhibitors of ERK kinase. Also disclosed are compositions and methods for treating hyperproliferative disorders.
Type:
Grant
Filed:
August 3, 2012
Date of Patent:
November 17, 2015
Assignees:
Array BioPharma Inc., Genentech, Inc.
Inventors:
James F. Blake, Huifen Chen, Mark Joseph Chicarelli, Jason Demeese, Rustam Ferdinand Garrey, John Gaudino, Lewis Gazzard, Robert J. Kaus, Samuel Kintz, Peter J. Mohr, David A. Moreno, Jacob Schwarz, Christopher S. Siedem, Eli M. Wallace
Abstract: Compounds of Formula I are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula I and stereoisomers and pharmaceutically acceptable salts 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.
Type:
Application
Filed:
January 7, 2015
Publication date:
November 12, 2015
Applicant:
ARRAY BIOPHARMA INC.
Inventors:
Yvan Le Huerou, James F. Blake, Indrani W. Gunawardana, Peter J. Mohr, Eli M. Wallace, Bin Wang, Mark Joseph Chicarelli, Michael Lyon
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.
Type:
Grant
Filed:
December 13, 2011
Date of Patent:
November 3, 2015
Assignee:
Array BioPharma Inc.
Inventors:
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
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.
Type:
Grant
Filed:
October 12, 2012
Date of Patent:
October 27, 2015
Assignee:
Array BioPharma Inc.
Inventors:
Donald T. Corson, Christopher M. Lindemann, Daniel J. Watson
Abstract: The present invention relates to crystalline polymorph forms of (1S)-1-[5-({3-[(2-methylpyridin-3-yl)oxy]-5-(pyridin-2-ylsulfanyl)pyridin-2-yl}amino)-1,2,4-thiadiazol-3-yl]ethane-1,2-diol, to pharmaceutical compositions comprising such crystalline polymorph forms, and to processes for preparing them. The invention further relates to methods of treatment of diabetes related disorders comprising administering such solid-state forms or compositions thereof to a subject, and to use of such crystalline polymorph forms in the manufacture of medicaments.
Type:
Application
Filed:
November 8, 2013
Publication date:
October 22, 2015
Applicants:
Amgen Inc., Array BioPharma Inc.
Inventors:
Sylvie Asselin, Lisa Brett, Ying Chen, Donald T. Corson, Andrew Cosbie, Robert Farrell, Indrani W. Gunawardana, Jinkun Huang, Jonathan W. Lane, Dennis Lei, Christopher M. Lindemann, Van Luu, Coralee G. Mannila, Robert Milburn, Henry Morrison, Helming Tan, Jason Tedrow, Daniel J. Watson
Abstract: The present invention relates to Compound 1 hydrogen sulfate salt and solvates, crystalline forms and amorphous forms thereof, and to processes for their preparation.
Type:
Grant
Filed:
May 3, 2012
Date of Patent:
October 13, 2015
Assignees:
Array BioPharma, Inc., Astrazeneca AB
Inventors:
John DeMattei, Tsung-Hsun Chuang, Christopher John Squire, Ronald John Roberts, Gorkhn Sharma-Singh, Mohammed Pervez, James Gair Ford, Richard Anthony Storey, Paul Alfred Dickinson
Abstract: Compounds having the formula I wherein Z, Z1 Z2 Z3, R3a, R3b and Rb and as defined herein are inhibitors of ERK kinase. Also disclosed are compositions and methods for treating hyperproliferative disorders.
Type:
Grant
Filed:
February 28, 2012
Date of Patent:
September 15, 2015
Assignees:
ARRAY BIOPHARMA INC., GENENTECH, INC.
Inventors:
James F. Blake, Huifen Chen, Mark Joseph Chicarelli, Jason Demeese, Rustam Garrey, John J. Gaudino, Robert J. Kaus, Gabrielle R. Kolakowski, Allison L. Marlow, Peter J. Mohr, Li Ren, Jacob Schwarz, Christopher S. Siedem, Allen A. Thomas, Eli Wallace, Steven Mark Wenglowsky, Steven Boyd
Abstract: Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in treating or preventing disease, including cancer, autoimmune disease, infectious disease, inflammatory disorder, graft rejection, and graft-verses-host disease.
Type:
Grant
Filed:
February 14, 2014
Date of Patent:
September 8, 2015
Assignees:
VentiRx Pharmaceuticals, Inc., Array Biopharma, Inc.
Inventors:
James Jeffry Howbert, Gregory Dietsch, Robert Hershberg, Laurence E. Burgess, Joseph P. Lyssikatos, Brad Newhouse, Hong-Woon Yang