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:
Application
Filed:
March 19, 2015
Publication date:
July 9, 2015
Applicant:
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: Provided are processes for the preparation of benzimidazole structures having Formula VIIIb-1: and salts and solvates thereof, wherein Z, X5, R2b, R2c and R10 are as defined herein. Compounds of Formula VIIIb-1 are useful for the preparation of benzimidazole derivatives.
Type:
Grant
Filed:
September 13, 2012
Date of Patent:
May 5, 2015
Assignee:
Array Biopharma Inc.
Inventors:
John DeMattei, Sagar Shakya, Anthony D. Piscopio, Bruno P. Hache, Matthew Charles Evans, James Gair Ford, Simon Mark Pointon, Koen Peeters, Timothy John Lilley, John Leonard
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:
Application
Filed:
August 3, 2012
Publication date:
March 26, 2015
Applicants:
GENENTECH, INC., ARRAY BIOPHARMA 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 Schwartz, Christopher S. Siedem, Eli M. Wallace
Abstract: Provided herein is a method of treating a PIM-1 and/or PIM-2 and/or PIM-3 kinase-mediated condition in a mammal, which comprises administering to said mammal a therapeutically effective amount of a compound of Formula I: in which A, B, R1, R1a, R2, R3, R4, R5, R6, and R7 have the meanings given in the specification.
Type:
Grant
Filed:
October 18, 2013
Date of Patent:
March 24, 2015
Assignee:
Array BioPharma Inc.
Inventors:
Shelley Allen, Laura L. Celeste, T. Gregg Davis, Robert Kirk DeLisle, Julie Marie Hicks, Stefan D. Gross, Erik James Hicken, Leila J. Jackson, Nicholas C. Kallan, Joseph P. Lyssikatos, Fredrik P. Marmsater, Mark C. Munson, Jed Pheneger, Bryson Rast, John E. Robinson, Stephen T. Schlachter, George T. Topalov, A. Dale Wright, Qian Zhao
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:
May 6, 2014
Date of Patent:
March 17, 2015
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: Compounds of Formula I: and stereoisomers and pharmaceutically acceptable salts and solvates thereof in which R1, R2, R3, R4, R5, R6, R7, X1 and X2 have the meanings given in the specification, are inhibitors of one or more JAK kinases and are useful in the treatment of autoimmune diseases, inflammatory diseases, rejection of transplanted organs, tissues and cells, as well as hematologic disorders and malignancies and their co-morbidities.
Type:
Grant
Filed:
April 11, 2011
Date of Patent:
February 24, 2015
Assignee:
Array BioPharma Inc.
Inventors:
Laurence E. Burgess, Mark Laurence Boys, Robert D. Groneberg, Darren M. Harvey, Timothy Kercher, Christopher F. Kraser, Ellen Laird, Eugene Tarlton, Qian Zhao, Lily Huang
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:
Application
Filed:
February 27, 2013
Publication date:
January 29, 2015
Applicant:
Array BioPharma Inc.
Inventors:
Alisha B. Arrigo, Donald T. Corson, Coralee G. Mannila
Abstract: Compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein ring A, ring B, W, m, D, R2, R2a, R3, R3a, and Z are as defined herein, are inhibitors of Trk kinases and are useful in the treatment of pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.
Type:
Grant
Filed:
May 13, 2011
Date of Patent:
January 13, 2015
Assignee:
Array BioPharma Inc.
Inventors:
Steven Wade Andrews, Kevin Ronald Condroski, Julia Haas, Yutong Jiang, Gabrielle R. Kolakowski, Jeongbeob Seo, HongWoon Yang, Qian Zhao
Abstract: Provided are compounds of Formula I wherein R1, R2, Y, Z and G are as defined herein, that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.
Type:
Grant
Filed:
October 24, 2006
Date of Patent:
January 13, 2015
Assignee:
Array BioPharma Inc.
Inventors:
Thomas D. Aicher, Ronald Jay Hinklin, Mark Joseph Chicarelli, Steven Armen Boyd, Kevin Ronald Condroski, Yi-Wen Yeh
Abstract: Provided herein are methods of treating diseases mediated by PIM-1 and/or PIM-2 and/or PIM-3 kinases by administering to a mammal in need thereof a therapeutically effective amount of a compound of Formula I: in which B, R1, R1a, R2, R3, R4, R5, R6, R7, R10 and R11 have the meanings given in the specification.
Type:
Grant
Filed:
October 15, 2013
Date of Patent:
November 25, 2014
Assignee:
Array BioPharma Inc.
Inventors:
Shelley Allen, Robert Kirk DeLisle, Julie Marie Hicks, Erik James Hicken, Joseph P. Lyssikatos, Fredrik P. Marmsater, Mark C. Munson, John E. Robinson, Qian Zhao
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:
November 15, 2012
Date of Patent:
November 25, 2014
Assignees:
Array Biopharma Inc., Genetech, Inc.
Inventors:
Anna Banka, 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: Compounds of Formula I: in which R1, R2, R3, R4 and R10 have the meanings given in the specification, are receptor tyrosine inhibitors useful in the treatment of diseases mediated by PIM-1 and/or PIM-2 and/or PIM-3 kinases.
Type:
Grant
Filed:
February 24, 2012
Date of Patent:
November 18, 2014
Assignee:
Array BioPharma Inc.
Inventors:
James F. Blake, Robert Kirk Delisle, Lisa A. De Meese, James M. Graham, Yvan Le Huerou, Michael Lyon, John E. Robinson, Eli M. Wallace, Bin Wang, Rui Xu
Abstract: Provided are compounds that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.
Type:
Grant
Filed:
November 5, 2012
Date of Patent:
November 11, 2014
Assignee:
Array BioPharma Inc.
Inventors:
Thomas Daniel Aicher, Steven Armen Boyd, Mark Joseph Chicarelli, Kevin Ronald Condroski, Ronald Jay Hinklin, Ajay Singh
Abstract: Compounds of Formula I: and salts thereof in which R1, R2, R2a, R3, n, X and ring B have the meanings given in the specification, are inhibitors of mTOR and are useful in the treatment of diseases which are sensitive to inhibition of mTOR, such as cancers.
Type:
Grant
Filed:
September 3, 2010
Date of Patent:
October 21, 2014
Assignee:
Array BioPharma Inc.
Inventors:
Steven W. Andrews, Kevin Ronald Condroski, Lisa A. De Meese, Jay Bradford Fell, John P. Fischer, John A. Josey, Kevin Koch, Yvan Le Huerou, Gregory F. Miknis, Martha E. Rodriguez, George T. Topalov, Eli M. Wallace, Rui Xu
Abstract: Provided herein are methods for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal, which comprises administering to said mammal in need thereof 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:
July 16, 2013
Date of Patent:
October 21, 2014
Assignee:
Array BioPharma Inc.
Inventors:
Julia Haas, Steven W. Andrews, Yutong Jiang, Gan Zhang
Abstract: The present invention provides a compound and pharmaceutically acceptable salts thereof, comprising the Formula I. Also provided are methods of using the compound of this invention as an AKT protein kinase inhibitor and for the treatment of hyperproliferative diseases such as cancer.
Type:
Grant
Filed:
January 9, 2009
Date of Patent:
October 7, 2014
Assignees:
Array BioPharma, Inc., Genentech, Inc.
Inventors:
Josef Bencsik, James F. Blake, Nicholas C. Kallan, Ian S. Mitchell, Keith L. Spencer, Dengming Xiao, Rui Xu, Christine Chabot, Steven Do, Jun Liang, Brian Safina, Birong Zhang, James Graham
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:
October 12, 2011
Date of Patent:
October 7, 2014
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. Banka, Jun Liang, Brian Safina, Birong Zhang, Christine Chabot, Steven Do
Abstract: Provided are compounds of Formula (I): wherein R2, R3, R13, L and D2 are as defined in the specification, which are useful in the treatment and/or prevention of diseases or disorders mediated by deficient levels of glucokinase activity or which can be treated by activating glucokinase including, but not limited to, diabetes mellitus, impaired glucose tolerance, IFG (impaired fasting glucose) and IFG (impaired fasting glycemia), as well as other diseases and disorders such as those discussed herein.
Type:
Grant
Filed:
June 11, 2012
Date of Patent:
October 7, 2014
Assignee:
Array BioPharma Inc.
Inventors:
Thomas Daniel Aicher, Steven Armen Boyd, Mark Joseph Chicarelli, Kevin Ronald Condroski, Jay Bradford Fell, John P. Fischer, Indrani W. Gunawardana, Ronald Jay Hinklin, Ajay Singh, Timothy M. Turner, Eli M. Wallace
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:
June 14, 2011
Date of Patent:
September 30, 2014
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. Banka, Jun Liang, Brian Safina, Jun Li, Christine Chabot
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:
January 29, 2013
Date of Patent:
September 30, 2014
Assignees:
Array BioPharma, Inc., Genentech, Inc.
Inventors:
Josef R. Bencsik, James F. Blake, Nicholas C. Kallan, Ian S. Mitchell, Keith L. Spencer, Dengming Xiao, Rui Xu, Christine Chabot, Jun Liang, Brian S. Safina