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.
Type:
Grant
Filed:
November 21, 2013
Date of Patent:
August 9, 2016
Assignees:
ARRAY BIOPHARMA INC., GENENTECH, INC.
Inventors:
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
Abstract: The invention provides processes of preparation thereof useful in the preparation of compounds that can be used as CHK1 inhibitors.
Type:
Application
Filed:
August 21, 2014
Publication date:
July 14, 2016
Applicants:
Genentech, Inc., Array BioPharma Inc.
Inventors:
Chong HAN, Keena GREEN, Francis GOSSELIN, Michelangelo SCALONE, Paul J. NICHOLS, Weidong LIU, Keith L. SPENCER, Zackary D. CRANE, Peter J. STENGEL, Sagar SHAKYA
Abstract: Compounds having the formula I wherein R2, X and Z as defined herein are inhibitors of ERK kinase. Also disclosed are compositions and methods for treating hyperproliferative disorders.
Type:
Grant
Filed:
August 27, 2013
Date of Patent:
July 12, 2016
Assignees:
GENETECH, INC., ARRAY BIOPHARMA INC.
Inventors:
Jim Blake, Huifen Chen, Mark Chicarelli, John Gaudino, Lewis Gazzard, Sam Kintz, Pete Mohr, Kirk Robarge, Jacob Schwarz, Aihe Zhou
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:
December 18, 2015
Date of Patent:
July 5, 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: 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:
Application
Filed:
October 26, 2015
Publication date:
June 23, 2016
Applicant:
ARRAY BIOPHARMA INC.
Inventors:
Donald T. Corson, Christopher M. Lindemann, Daniel J. Watson
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:
Grant
Filed:
January 7, 2015
Date of Patent:
June 14, 2016
Assignee:
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: 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.
Type:
Grant
Filed:
August 12, 2014
Date of Patent:
June 7, 2016
Assignees:
Array BioPharma Inc., Genentech, Inc.
Inventors:
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
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.
Type:
Application
Filed:
January 31, 2014
Publication date:
June 2, 2016
Applicant:
Array BioPharma, Inc.
Inventors:
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
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.
Type:
Application
Filed:
November 21, 2013
Publication date:
June 2, 2016
Applicants:
Array BioPharma Inc., Genentech, Inc.
Inventors:
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
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.
Type:
Grant
Filed:
November 14, 2012
Date of Patent:
May 24, 2016
Assignee:
ARRAY BIOPHARMA INC.
Inventors:
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
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:
Application
Filed:
October 13, 2015
Publication date:
May 19, 2016
Applicants:
VENTIRX PHARMACEUTICALS, INC., ARRAY BIOPHARMA, INC.
Inventors:
James Jeffry Howbert, Gregory N. Dietsch, Robert Hershberg, Laurence E. Burgess, George A. Doherty, C. Todd Eary, Robert D. Groneberg, Zachery Jones
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:
Application
Filed:
January 12, 2016
Publication date:
May 5, 2016
Applicants:
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: 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