Patents Assigned to Exelixis, Inc.
  • BENZOXAZEPINES AS INHIBITORS OF mTOR AND METHODS OF THEIR USE AND MANUFACTURE
    Publication number: 20140018347
    Abstract: The invention is directed to inhibitors of mTOR and pharmaceutically acceptable salts or solvates thereof, as well as methods of using them. The inhibitors are generally of structural Formula (I) wherein the variables are as defined herein.
    Type: Application
    Filed: November 23, 2011
    Publication date: January 16, 2014
    Applicant: Exelixis, Inc.
    Inventor: Kenneth Rice
  • Pyrido [2, 3-D] pyrimidin-7-one compounds as inhibitors of P13K-Alpha for the treament of cancer
    Publication number: 20130343988
    Abstract: The invention is directed to Compounds of Formula (I). The invention provides compounds that inhibit, regulate, and/or modulate P13K that are useful in the treatment of hyperproliferative diseases, such as cancer.
    Type: Application
    Filed: January 3, 2013
    Publication date: December 26, 2013
    Applicant: Exelixis, Inc.
    Inventor: Exelixis, Inc.
  • C-Met Modulator Pharmaceutical Compositions
    Publication number: 20130330377
    Abstract: Pharmaceutical compositions and unit dosage forms comprising Compound I are disclosed.
    Type: Application
    Filed: July 18, 2011
    Publication date: December 12, 2013
    Applicant: Exelixis Inc.
    Inventor: Jo Ann Wilson
  • c-Met Modulators and Method of Use
    Publication number: 20130252940
    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: September 26, 2013
    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
  • Azepinoindole derivatives as pharmaceutical agents
    Patent number: 8524704
    Abstract: Compounds, compositions and methods for modulating the activity of receptors are provided. In particular, compounds and compositions are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder directly or indirectly related to the activity of the receptors.
    Type: Grant
    Filed: August 4, 2009
    Date of Patent: September 3, 2013
    Assignee: Exelixis, Inc.
    Inventors: Brett Busch, Brenton T. Flatt, Xiao-Hui Gu, Richard Martin, Raju Mohan, Tie-Lin Wang, Jason H. Wu
  • Methods of treating cancer using pyridopyrimidinone inhibitors of PI3K alpha
    Patent number: 8513266
    Abstract: The present invention provides methods of treating cancer by administering a compound of Formula I, optionally as a pharmaceutically acceptable salt, solvate and/or hydrate thereof, in combination with other cancer treatments.
    Type: Grant
    Filed: April 9, 2008
    Date of Patent: August 20, 2013
    Assignee: Exelixis, Inc.
    Inventors: Peter Lamb, David Matthews
  • PFKs as Modifiers of the IGFR Pathway and Methods of Use
    Publication number: 20130212716
    Abstract: Human PFK genes are identified as modulators of the IGFR pathway, and thus are therapeutic targets for disorders associated with defective IGFR function. Methods for identifying modulators of IGFR, comprising screening for agents that modulate the activity of PFK are provided.
    Type: Application
    Filed: April 12, 2013
    Publication date: August 15, 2013
    Applicant: EXELIXIS, INC.
    Inventor: Exelixis, Inc.
  • C-met modulators and method of use
    Patent number: 8497284
    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: Grant
    Filed: September 30, 2011
    Date of Patent: July 30, 2013
    Assignee: Exelixis, Inc.
    Inventors: Lynne Canne Bannen, Diva Sze-Ming Chan, Jeff Chen, Lisa Esther Dalrymple, Timothy Patrick Forsyth, Tai Phat Huynh, Vasu Jammalamadaka, Richard George Khoury, James William Leahy, Morrison B. Mac, Grace Mann, Larry W. Mann, John M. Nuss, Jason Jevious Parks, Craig Stacy Takeuchi, Yong Wang, Wei Xu
  • Atropisomers of (hydroxyalkyl) pyrrole derivatives
    Patent number: 8487117
    Abstract: The present invention comprises a compound for the prevention and/or treatment of cardiovascular diseases. The compound is an atropisomer of a compound represented by the following general formula (I): wherein R1 represents a C1-C3 alkyl group; R2 represents a 2-hydroxy-C4-C6 alkyl group; 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 C1-C3 alkyl group; and R6 represents a hydrogen atom, a halogeno group and the like] or atropisomers thereof.
    Type: Grant
    Filed: October 7, 2009
    Date of Patent: July 16, 2013
    Assignee: Exelixis, Inc.
    Inventors: John Nuss, Matthew Williams, Raju Mohan, Richard Martin, Tie-Lin Wang, Kazumasa Aoki, Hiroyuki Tsuruoka, Noriyuki Hayashi, Tsuyoshi Homma
  • PIK4CA as modifier of the Rac pathway and methods of use
    Patent number: 8481269
    Abstract: Human PIK4CA genes are identified as modulators of the RAC pathway, and thus are therapeutic targets for disorders associated with defective RAC function. Methods for identifying modulators of RAC, comprising screening for agents that modulate the activity of PIK4CA are provided.
    Type: Grant
    Filed: September 15, 2005
    Date of Patent: July 9, 2013
    Assignee: Exelixis, Inc.
    Inventors: Lisa C. Kadyk, George Ross Francis, Lynn Margaret Bjerke, Timothy S. Heuer
  • Combination therapies comprising quinoxaline inhibitors of P13K-alpha for use in the treatment of cancer
    Patent number: 8481001
    Abstract: The present invention provides methods of treating cancer by administering a compound of Formula I, optionally as a pharmaceutically acceptable salt, solvate and/or hydrate thereof, in combination with other cancer treatments.
    Type: Grant
    Filed: April 8, 2008
    Date of Patent: July 9, 2013
    Assignee: Exelixis, Inc.
    Inventors: Peter Lamb, David Matthews
  • Methods of Treating Cancer Using Pyridopyrimidinone Inhibitors of PI3K and mTOR in Combination with Autophagy Inhibitors
    Publication number: 20130172371
    Abstract: The invention provides compounds of Formula I: that inhibit the PI3Ks and mTOR that are useful in the treatment of cancer in humans when used in combination with autophagy inhibitors.
    Type: Application
    Filed: February 9, 2011
    Publication date: July 4, 2013
    Applicant: EXELIXIS, INC
    Inventors: Dana T. Aftab, Wolfgang M. Korn, Olga K. Mirzoeva
  • c-Met modulators and method of use
    Patent number: 8476298
    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: Grant
    Filed: May 24, 2007
    Date of Patent: July 2, 2013
    Assignee: 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, Morrisson B. Mac, Larry W. Mann, John M. Nuss, Jason Jevious Parks, Craig Stacy Takeuchi, Yong Wang, Wie Xu
  • JAK1 Inhibitors
    Publication number: 20130165440
    Abstract: JAK1 inhibitors of structural formula (I), wherein Ar1, Ar2, Q, W, X, Y, and Z are defined in the specification, pharmaceutically acceptable salts thereof, compositions thereof, and use of the compounds and compositions for treating diseases. The invention also comprises use of the compounds in and for the manufacture of medicaments, particularly for treating diseases.
    Type: Application
    Filed: September 13, 2011
    Publication date: June 27, 2013
    Applicant: EXELIXIS, INC.
    Inventors: Neel Kumar Anand, S. David Brown, Zerom Tesfai, Cristiana A. Zaharia
  • Azepine derivatives as pharmaceutical agents
    Patent number: 8466143
    Abstract: Compounds, compositions and methods are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder related to the activity of the receptors.
    Type: Grant
    Filed: July 23, 2004
    Date of Patent: June 18, 2013
    Assignee: Exelixis, Inc.
    Inventors: Richard Martin, Tie-Lin Wang, Brenton T. Flatt, Xiao-Hui Gu
  • Hydrated Crystalline Forms of N-[3-fluoro-4-(oxy)phenyl]-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
    Publication number: 20130143881
    Abstract: This invention relates crystalline hydrates 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). 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 hydrate of Compound (I) and a pharmaceutically acceptable excipient.
    Type: Application
    Filed: March 11, 2011
    Publication date: June 6, 2013
    Applicant: Exelixis, Inc.
    Inventors: Hilary Cannon, Feirong Kang, Frederick G. Vogt
  • Substituted pyrimidine compositions and methods of use
    Patent number: 8455489
    Abstract: Novel compositions and methods of using substituted pyrimidines which have the general formula: (I).
    Type: Grant
    Filed: November 9, 2004
    Date of Patent: June 4, 2013
    Assignee: Exelixis, Inc.
    Inventors: Richard Martin, Raju Mohan, Peter Ordentlich
  • 4-aryl-2-amino-pyrimidines or 4-aryl-2-aminoalkyl-pyrimidines as JAK-2 modulators and methods of use
    Patent number: 8440663
    Abstract: This invention relates to certain pyrimidine derivative inhibitors of JAK-2, having Formula (I): wherein D, E, L, Z, R1, R2, R25, and n1 are as defined in the specification, pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Grant
    Filed: January 30, 2007
    Date of Patent: May 14, 2013
    Assignee: Exelixis, Inc.
    Inventors: Grace Mann, Naing Aay, Arlyn Arcalas, S. David Brown, Wai Ki Vicky Chan, Jeff Chen, Hongwang Du, Sergey Epshteyn, Timothy Patrick Forsyth, Adam A. Galan, Tai Phat Huynh, Mohamed Abdulkader Ibrahim, Henry William Beecroft Johnson, Brian Kane, Patrick Kearney, Byung Gyu Kim, Elena S. Koltun, James W. Leahy, Matthew Sangyup Lee, Gary L. Lewis, Lisa E. Meyr, Robin Tammie Noguchi, Michael Pack, Brian Hugh Ridgway, Xian Shi, John Woolfrey, Peiwen Zhou
  • RORS as modifiers of the p21 pathway and methods of use
    Patent number: 8426147
    Abstract: Human ROR genes are identified as modulators of the p21 pathway, and thus are therapeutic targets for disorders associated with defective p21 function. Methods for identifying modulators of p21, comprising screening for agents that modulate the activity of ROR are provided.
    Type: Grant
    Filed: December 1, 2008
    Date of Patent: April 23, 2013
    Assignee: Exelixis, Inc.
    Inventors: Helen Francis-Lang, Lori Friedman, Thomas Kidd, Siobhan Roche, Haiguang Zhang
  • Pyrazolo pyrimidines as casein kinase II (CK2) modulators
    Patent number: 8372851
    Abstract: A compound according to Formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R6, R7 and Z are as defined in the specification; pharmaceutical compositions thereof; and methods of use thereof.
    Type: Grant
    Filed: October 23, 2006
    Date of Patent: February 12, 2013
    Assignee: Exelixis, Inc.
    Inventors: Kenneth D. Rice, Joerg Bussenius, Simona Costanzo, Abigail R. Kennedy, Angie Inyoung Kim, Jean-Claire Limun Manalo, Csaba J. Peto