Patents Assigned to Exelixis, Inc.
  • c-Met Modulators and Method of Use
    Publication number: 20140155378
    Abstract: The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.
    Type: Application
    Filed: May 7, 2013
    Publication date: June 5, 2014
    Applicant: Exelixis, Inc.
    Inventors: Lynne Canne Bannen, Diva Sze-ming Chan, Jeff Chen, Timothy Patrick Forsyth, Tai Phat Huynh, Vasu Jammalamadaka, Richard George Khoury, James William Leahy, Morrison B. Mac, Larry W. Mann, John M. Nuss, Jason Jevious Parks, Craig Stacy Takeuchi, Yong Wang, Wei Xu
  • METHOD OF TREATING LUNG ADENOCARCINOMA
    Publication number: 20140121239
    Abstract: This invention is directed to the treatment of cancer in a patient, particularly a patient with lung adenocarcinoma, and more particularly a patient with KIF5B-RET fusion-positive non-small cell lung cancer, with an inhibitor of MET, VEGF, and RET which is a compound of Formula I: or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: September 9, 2013
    Publication date: May 1, 2014
    Applicant: EXELIXIS, INC.
    Inventor: DANA T. AFTAB
  • Pyrazole kinase modulators and methods of use
    Patent number: 8710038
    Abstract: The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinases. Methods of using the compounds and pharmaceutical compositions thereof to treat kinase-dependent diseases and conditions are also an aspect of the invention.
    Type: Grant
    Filed: September 15, 2005
    Date of Patent: April 29, 2014
    Assignee: Exelixis, Inc.
    Inventors: Tae-Gon Baik, Chris A. Buhr, Sunghoon Ma, John M. Nuss, Zerom Tesfai, Longcheng Wang, Bryan K. S. Yeung
  • Benzoxazepines as Inhibitors of PI3K/mTOR and Methods of Their Use and Manufacture
    Publication number: 20140107100
    Abstract: The invention is directed 10 Compound's of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds.
    Type: Application
    Filed: November 23, 2011
    Publication date: April 17, 2014
    Applicant: EXELIXIS, INC.
    Inventors: Kenneth Rice, Paul Foster
  • Raf modulators and methods of use
    Patent number: 8697737
    Abstract: The present invention relates to compounds of the Formula I, wherein G, A, X1, X2, X3, Z, E, Y, and X are defined herein. The compounds modulate protein kinase enzymatic activity to modulate cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinases, particularly Raf. Methods of using and preparing the compounds, and pharmaceutical compositions thereof, to treat kinase-dependent diseases and conditions are also an aspect of the invention.
    Type: Grant
    Filed: October 12, 2010
    Date of Patent: April 15, 2014
    Assignee: Exelixis, Inc.
    Inventors: Neel Kumar Anand, Charles M. Blazey, Owen Joseph Bowles, Joerg Bussenius, Simona Costanzo, Jeffry Kimo Curtis, Larisa Dubenko, Abigail R. Kennedy, Steven Charles Defina, Angie I. Kim, Jean-Claire L. Manalo, Csaba J. Peto, Kenneth D. Rice, Tsze H. Tsang, Anagha Abhijit Joshi
  • Methods of Using PI3K and MEK Modulators
    Publication number: 20140100215
    Abstract: The invention provides methods of treating cancer with a combination of compounds which inhibit kinases, more specifically MEK and PI3K.
    Type: Application
    Filed: December 7, 2013
    Publication date: April 10, 2014
    Applicant: Exelixis, Inc.
    Inventors: Dana T. Aftab, A. Douglas Laird, Peter Lamb, Jean-Francois A. Martini
  • EEF2K as modifiers of the PTEN/AKT pathway and methods of use
    Patent number: 8679763
    Abstract: Human EEF2K genes are identified as modulators of the PTEN/AKT pathway and thus are therapeutic targets for disorders associated with defective PTEN/AKT function. Methods for identifying modulators of PTEN/AKT comprising screening for agents that modulate the activity of EEF2K are provided.
    Type: Grant
    Filed: March 10, 2006
    Date of Patent: March 25, 2014
    Assignee: Exelixis, Inc.
    Inventors: Arthur Brace, Robert A. Blake, Lori S. Friedman, Lynn Margaret Bjerke, Kevin M. Ward, Susana Nieto-Bergman
  • Benzoxazepines as Inhibitors of PI3K/mTOR and Methods of Their Use and Manufacture
    Publication number: 20140080810
    Abstract: The invention is directed to Compounds of Formula I: (I) and pharmaceutically acceptable salts or solvates thereof, as well as methods of treating using the compounds, methods for screening for inhibitor compounds and methods for identifying treatment regimens.
    Type: Application
    Filed: November 15, 2011
    Publication date: March 20, 2014
    Applicant: Exelixis, Inc.
    Inventors: Kenneth D. Rice, David Markby
  • Crystalline Forms on N-[3-fluoro-4-({6-(methyloxy)-7-[(3-morpholin-4-ylpropyl)oxy]-quinolin-4-yl}oxy)phenyl]-N?-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
    Patent number: 8673912
    Abstract: This invention relates to three crystalline forms of N-[3-fluoro-4-((6-(methyloxy)-7-[(3-morpholin-4-ylpropyl)oxy]quinolin-4-yl|oxy)phenyl]-N?-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide. Compound (I), designated as Form A, Form B, and Form C. The invention provides methods for treatment of cancer by exploiting the modulation of protein kinase activity. The invention also provides pharmaceutical compositions containing a crystalline form of Compound (I) and a pharmaceutically acceptable excipient.
    Type: Grant
    Filed: July 16, 2010
    Date of Patent: March 18, 2014
    Assignee: Exelixis, Inc.
    Inventors: Hilary Cannon, David Igo, Tri Tran
  • Benzoxazepines as Inhibitors of PI3K/mTOR and Methods of Their Use and Manufacture
    Publication number: 20140066431
    Abstract: The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of treating using the compounds, methods for screening for inhibitor compounds and methods for identifying treatment regimens.
    Type: Application
    Filed: November 15, 2011
    Publication date: March 6, 2014
    Applicant: Exelixis, Inc.
    Inventors: Kenneth D. Rice, David Markby
  • Method of Treating Cancer
    Publication number: 20140066444
    Abstract: This invention is directed to the treatment of cancer, particularly castration-resistant prostate cancer and osteoblastic bone metastases, with a dual inhibitor of MET and VEGF.
    Type: Application
    Filed: September 26, 2011
    Publication date: March 6, 2014
    Applicant: Exelixis, Inc.
    Inventors: David C. Smith, Maha Hussain
  • Method of Treating Cancer
    Publication number: 20140057908
    Abstract: This invention is directed to the treatment of cancer, particularly castration-resistant prostate cancer and osteoblastic bone metastases, with a dual inhibitor of MET and VEGF.
    Type: Application
    Filed: September 26, 2011
    Publication date: February 27, 2014
    Applicant: Exelixis, Inc.
    Inventors: David C. Smith, Maha Hussain
  • Inhibitors of PI3K-Delta and Methods of Their Use and Manufacture
    Publication number: 20140058103
    Abstract: The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds.
    Type: Application
    Filed: September 14, 2011
    Publication date: February 27, 2014
    Applicant: Exelixis, Inc.
    Inventor: Patrick Kearney
  • Inhibitors of PI3K-Delta and Methods of Their Use and Manufacture
    Publication number: 20140045825
    Abstract: The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds.
    Type: Application
    Filed: September 14, 2011
    Publication date: February 13, 2014
    Applicant: Exelixis, Inc.
    Inventor: James William Leahy
  • Benzoxazepines as inhibitors of PI3K/mTOR and methods of their use and manufacture
    Patent number: 8648066
    Abstract: The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds.
    Type: Grant
    Filed: May 20, 2010
    Date of Patent: February 11, 2014
    Assignee: Exelixis, Inc.
    Inventors: Neel Kumar Anand, Charles M. Blazey, Owen Joseph Bowles, Chris Allen Buhr, Joerg Bussenius, Jeffry Kimo Curtis, Steven Charles DeFina, Larisa Dubenko, Jason R. Harris, Eileen E. Jackson-Ugueto, Anagha Joshi, Angie Inyoung Kim, Amy Lew Tsuhako, Sunghoon Ma, Jean-Claire Limun Manalo, Stephanie Ng, Csaba J. Peto, Kenneth D. Rice, Tsze H. Tsang, Cristiana A. Zaharia
  • Method of using PI3K and MEK modulators
    Patent number: 8642584
    Abstract: The invention provides methods of treating cancer with a combination of compounds which inhibit kinases, more specifically MEK and PI3K.
    Type: Grant
    Filed: August 7, 2012
    Date of Patent: February 4, 2014
    Assignee: Exelixis, Inc.
    Inventors: Dana T. Aftab, A. Douglas Laird, Peter Lamb, Jean-Francois A. Martini
  • 1-phenylpyrrole derivatives
    Patent number: 8642640
    Abstract: The present invention comprises a compound for the prevention and/or treatment of cardiovascular diseases, nephropathy, fibrosis, primary aldosteronism or edema. The compound is of the following general formula (I): wherein R1 represents a C1-C3 alkyl group; R2 represents a hydroxy-C1-C4 alkyl group and the like; R3 represents a halogeno group, a halogeno-C1-C3 alkyl group and the like; R4 represents a hydrogen atom, a halogeno group and the like, —R5 represents a sulfamoyl group or a C1-C3 alkylsulfonyl group; R6 represents a hydrogen atom, a halogeno group and the like] or an N-oxide, atropisomer of the foregoing, or pharmaceutically acceptable salt of the foregoing.
    Type: Grant
    Filed: October 7, 2009
    Date of Patent: February 4, 2014
    Assignees: Exelixis, Inc., Daiichi Sankyo Company, Limited
    Inventors: John Nuss, Matthew Williams, Raju Mohan, Richard Martin, Tie-Lin Wang, Hiroyuki Tsuruoka, Kazumasa Aoki, Masatoshi Honzumi, Yusuke Asoh, Keiji Saito, Tsuyoshi Homma
  • Benzoxazepines as inhibitors of PI3K/mTOR and methods of their use and manufacture
    Patent number: 8637499
    Abstract: The invention is directed to Compounds of Formula (I): the invention provides compounds that inhibit, regulate, and/or modulate P13K and/or mTOR that are useful in the treatment of hyperproliferative diseases, such as cancer, in mammals. This invention also provides methods of making the compound methods of using such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and to pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: May 25, 2010
    Date of Patent: January 28, 2014
    Assignee: Exelixis, Inc.
    Inventors: Naing Aay, Arlyn Arcalas, Joerg Bussenius, Steven Charles DeFina, Larisa Dubenko, Jason R. Harris, Eileen E. Jackson-Ugueto, Angie Inyoung Kim, Jean-Claire Limun Manalo, Michael Pack, Csaba J. Peto, Kenneth D. Rice, Tsze H. Tsang, Owen Joseph Bowles, Jeffry Kimo Curtis
  • Benzoxazepines as Inhibitors of PI3K/mTOR and Methods of Their use and Manufacture
    Publication number: 20140024637
    Abstract: The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds.
    Type: Application
    Filed: November 23, 2011
    Publication date: January 23, 2014
    Applicant: Exelixis, Inc.
    Inventor: Kenneth D. Rice
  • PLKS as modifiers of the beta catenin pathway and methods of use
    Patent number: 8632962
    Abstract: Human PLK genes are identified as modulators of the beta catenin pathway, and thus are therapeutic targets for disorders associated with defective beta catenin function. Methods for identifying modulators of beta catenin, comprising screening for agents that modulate the activity of PLK are provided.
    Type: Grant
    Filed: November 23, 2004
    Date of Patent: January 21, 2014
    Assignee: Exelixis, Inc.
    Inventors: Helen Francis-Lang, Christopher G. Winter, Richard Benn Abegania Ventura, Lynn Margaret Bjerke, Timothy S. Heuer