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: The invention provides anti-HER antibodies, including multispecific anti-HER antibodies, compositions comprising and methods of using these antibodies. Also provided herein are EGFR/HER3 multispecific antibodies that are less toxic than traditional EGFR antagonists.
Type:
Grant
Filed:
October 29, 2013
Date of Patent:
May 3, 2016
Assignee:
Genentech, Inc.
Inventors:
Germaine Fuh, Lauric Haber, Gabriele Schaefer, Mark X. Sliwkowski
Abstract: Cyclic ether pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein R2 is a cyclic ether and X is thiazolyl, pyrazinyl, pyridinyl, or pyrimidinyl, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I 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:
September 25, 2013
Date of Patent:
May 3, 2016
Assignee:
GENENTECH, INC.
Inventors:
Jason Burch, Minghua Sun, Xiaojing Wang, Wesley Blackaby, Alastair James Hodges, Andrew Sharpe
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: Heteroaryl pyridone and aza-pyridone amide compounds of Formula I are provided, and various substituents including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk, and for treating cancer and immune disorders such as inflammation mediated by Btk. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
Type:
Grant
Filed:
July 2, 2014
Date of Patent:
May 3, 2016
Assignee:
Genentech, Inc.
Inventors:
James John Crawford, Wendy Lee, Wendy B. Young
Abstract: The emergence of mutations in tyrosine kinases following treatment of cancer patients with molecular-targeted therapy represents a major mechanism of acquired drug resistance. Here, we describe a mutation in the serpentine receptor, Smoothened (SMO), which results in resistance to a Hedgehog (Hh) pathway inhibitor in medulloblastoma. A single amino acid substitution in a conserved aspartic acid residue of SMO maintains Hh signaling, but results in the inability of the Hh pathway inhibitor, GDC-0449, to bind SMO and suppress the pathway. This mutation was not only acquired in a GDC-0449-resistant mouse model of medulloblastoma, but was identified in a Medulloblastoma patient following relapse on GDC-0449. The invention provides screening methods to detect SMO mutations and methods to screen for drugs that specifically modulate mutant SMO exhibiting drug resistance.
Type:
Grant
Filed:
September 2, 2010
Date of Patent:
April 26, 2016
Assignees:
Genentech, Inc., Curis, Inc.
Inventors:
Frederic J. de Sauvage, Gerrit J.P. Dijkgraaf, Thomas Januario, Robert L. Yauch
Abstract: The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.
Type:
Grant
Filed:
December 18, 2014
Date of Patent:
April 26, 2016
Assignees:
CURIS, INC., GENENTECH, INC.
Inventors:
Janet L. Gunzner-Toste, Daniel Sutherlin, Mark S. Stanley, Liang Bao, Georgette M. Castanedo, Rebecca L. LaLonde, Shumei Wang, Mark E. Reynolds, Scott J. Savage, Kimberly Malesky, Michael S. Dina, Michael F. T. Koehler
Abstract: The invention provides methods and reagents useful for detecting anti-drug antibodies of IgE isotype to therapeutic anti-IgE antibodies, and methods for assessing risk of anaphylaxis to administration of a therapeutic anti-IgE antibody.
Type:
Grant
Filed:
October 26, 2010
Date of Patent:
April 19, 2016
Assignee:
Genentech, Inc.
Inventors:
Saloumeh Fischer, Dana L. Baker, Henry B. Lowman, Gerald R. Nakamura
Abstract: Novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies and have the general formula I: wherein R1, R2, R3, R4, R5 and R6 are as described herein.
Type:
Application
Filed:
December 18, 2015
Publication date:
April 14, 2016
Applicant:
GENENTECH, INC.
Inventors:
Frederick COHEN, Lewis J. GAZZARD, Vickie Hsiao-Wei TSUI, John A. FLYGARE
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 invention provides compounds of Formula I, stereoisomers or pharmaceutically acceptable salts thereof, wherein A, X, R1, R2, R4 and R5 are defined herein, a pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of using the compound or composition in therapy.
Type:
Grant
Filed:
May 16, 2013
Date of Patent:
April 12, 2016
Assignee:
GENENTECH, INC.
Inventors:
Toby Blench, Simon Goodacre, Yingjie Lai, Jun Liang, Calum Macleod, Steven Magnuson, Vickie Tsui, Karen Williams, Birong Zhang
Abstract: Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formulas I and II 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:
July 29, 2014
Date of Patent:
April 12, 2016
Assignees:
Genentech, Inc., Hoffmann-La Roche Inc.
Inventors:
Steven Do, Richard Goldsmith, Tim Heffron, Aleksandr Kolesnikov, Steven Staben, Alan G. Olivero, Michael Siu, Daniel P. Sutherlin, Bing-Yan Zhu, Paul Goldsmith, Tracy Bayliss, Adrian Folkes, Neil Pegg
Abstract: The invention relates to compounds of Formula (0): wherein Q, A1-A8, R4 and R5 and each has the meaning as described herein. Compounds of Formula (0) and pharmaceutical compositions thereof are useful in the treatment of diseases and disorders in which undesired or over-activation of NF-kB signaling is observed.
Type:
Application
Filed:
August 22, 2014
Publication date:
April 7, 2016
Applicant:
GENENTECH, INC.
Inventors:
Nicole Blaquiere, Georgette Castanedo, Jianwen A. Feng, Baihua Hu, Steven Staben, Po-wai Yuen, Guosheng Wu, Jason Burch
Abstract: Compounds of the formula Ia or Ib: or pharmaceutically acceptable salts thereof, wherein m, n, r, A, X1, X2, X3, X4, Y, Z, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
Type:
Grant
Filed:
December 10, 2013
Date of Patent:
April 5, 2016
Assignee:
Genentech, Inc.
Inventors:
Benjamin Fauber, Olivier Rene, Monique Bodil van Niel, Stuart Ward
Abstract: Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
Type:
Application
Filed:
December 9, 2015
Publication date:
March 31, 2016
Applicant:
Genentech, Inc.
Inventors:
Mehmet Kahraman, Steven P. Govek, Nicholas D. Smith, Jeffrey H. Hager, Edna Chow Maneval