Patents Assigned to Exelixis, Inc.
  • Patent number: 11141413
    Abstract: The present disclosure relates to a method of treating advanced renal cell carcinoma (RCC) in human patients who have received prior anti-angiogenic therapy using CABOMETYX, a kinase inhibitor.
    Type: Grant
    Filed: April 17, 2017
    Date of Patent: October 12, 2021
    Assignee: Exelixis, Inc.
    Inventors: Dana T. Aftab, Gisela Schwab, Colin Hessel, Christian Scheffold, Steven Lacy, Dale Miles, Alan Arroyo, Mark Dean
  • Patent number: 11124481
    Abstract: The present invention relates to a method of preparing Cabozantinib (Cyclopropane-1,1-dicarboxylic acid [4-(6,7-dimethoxy-quinolin-4-yloxy)-phenylo]amide(4-fluoro-phenyl)amide) and 18F labeled Cabozantinib.
    Type: Grant
    Filed: July 31, 2015
    Date of Patent: September 21, 2021
    Assignee: Exelixis, Inc.
    Inventors: Wei Xu, David J. Donnelly, Patrick L. Chow, Benjamin J. Henley
  • Patent number: 11123338
    Abstract: Pharmaceutical compositions and unit dosage forms comprising Compound (I) are disclosed.
    Type: Grant
    Filed: December 20, 2019
    Date of Patent: September 21, 2021
    Assignee: Exelixis, Inc.
    Inventors: Jo Ann Wilson, Khalid Shah
  • Patent number: 11124482
    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, KDR, 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: August 28, 2017
    Date of Patent: September 21, 2021
    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
  • Patent number: 11116759
    Abstract: This invention is directed to the treatment of cancer, particularly ocular melanoma, with a dual inhibitor of MET and VEGF such as Compound 1.
    Type: Grant
    Filed: September 26, 2018
    Date of Patent: September 14, 2021
    Assignee: Exelixis, Inc.
    Inventors: Dana T. Aftab, Frauke Schimmoller
  • Patent number: 11098015
    Abstract: Disclosed are malate salts of N-(4-{[6,7-bis(methyloxy)-quinolin-4-yl]oxy}phenyl)-N?-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, including a (L)-malate salt, a (D)-malate salt, a (DL) malate salt, and mixtures thereof; and crystalline and amorphous forms of the malate salts. Also disclosed are pharmaceutical compositions comprising at least one malate salts of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N?-(4-fluorophenyl)-cyclopropane-1,1-dicarboxamide; and methods of treating cancer comprising administering at least one malate salt of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N?-(4-fluorophenyl)cyclopropane-1, 1-dicarboxamide.
    Type: Grant
    Filed: February 9, 2021
    Date of Patent: August 24, 2021
    Assignee: Exelixis, Inc.
    Inventors: Adrian St. Clair Brown, Peter Lamb, William P. Gallagher
  • Patent number: 11091439
    Abstract: Disclosed are malate salts of N-(4-{[6,7-bis(methyloxy)-quinolin-4-yl]oxy}phenyl)-N?-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, including a (L)-malate salt, a (D)-malate salt, a (DL) malate salt, and mixtures thereof; and crystalline and amorphous forms of the malate salts. Also disclosed are pharmaceutical compositions comprising at least one malate salts of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N?-(4-fluorophenyl)-cyclopropane-1,1-dicarboxamide; and methods of treating cancer comprising administering at least one malate salt of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N?-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide.
    Type: Grant
    Filed: October 14, 2020
    Date of Patent: August 17, 2021
    Assignee: Exelixis, Inc.
    Inventors: Adrian St. Clair Brown, Peter Lamb, William P. Gallagher
  • Patent number: 11091440
    Abstract: Disclosed are malate salts of N-(4-{[6,7-bis(methyloxy)-quinolin-4-yl]oxy}phenyl)-N?-(4-fluorophenyl)cyclo-propane-1,1-dicarboxamide, including a (L)-malate salt, a (D)-malate salt, a (DL) malate salt, and mixtures thereof; and crystalline and amorphous forms of the malate salts. Also disclosed are pharmaceutical compositions comprising at least one malate salts of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N?-(4-fluorophenyl)-cyclopropane-1,1-dicarboxamide; and methods of treating cancer comprising administering at least one malate salt of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N?-(4-fluorophenyl)cyclopropane-1, 1-dicarboxamide.
    Type: Grant
    Filed: January 14, 2021
    Date of Patent: August 17, 2021
    Assignee: Exelixis, Inc.
    Inventors: Adrian St. Clair Brown, Peter Lamb, William P. Gallagher
  • Patent number: 11065240
    Abstract: This invention relates to the combination of a C-Met inhibitor and a proteasome inhibitor to treat cancer, particularly multiple myeloma.
    Type: Grant
    Filed: August 5, 2015
    Date of Patent: July 20, 2021
    Assignee: Exelixis, Inc.
    Inventors: Dana T. Aftab, Peter Lamb
  • Publication number: 20210155692
    Abstract: Anti-ROR antibody constructs, pharmaceutical compositions comprising the constructs, and methods of use thereof are presented.
    Type: Application
    Filed: April 18, 2019
    Publication date: May 27, 2021
    Applicant: EXELIXIS, INC.
    Inventors: Lucas BAILEY, Qufei LI, Malgorzata Agnieszka NOCULA-LUGOWSKA, Bryan GLASER
  • Publication number: 20210030737
    Abstract: Disclosed is a method of treating triple negative breast cancer in a human patient, comprising administering to the patient an amount of cabozantinib or a pharmaceutically acceptable salt thereof, wherein the amount of cabozantinib is sufficient to activate the immune system.
    Type: Application
    Filed: April 18, 2017
    Publication date: February 4, 2021
    Applicant: Exelixis, Inc.
    Inventors: Sara M. TOLANEY, Dan G. DUDA
  • Patent number: 10851061
    Abstract: The invention relates to novel crystalline solid forms of the chemical compound N-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-N?-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide (Compound 1), and solvates thereof, including hydrates, that are useful for the treatment of cancer. Also disclosed are pharmaceutical compositions comprising the crystalline solid forms and processes for making the crystalline solid forms, as well as methods of using them for the treatment of cancer, particularly thyroid cancer, prostate cancer, hepatocellular cancer, renal cancer, and non-small cell lung carcinoma. The crystalline solid forms can be used to make the L-malate salt of cabozantinib.
    Type: Grant
    Filed: November 1, 2019
    Date of Patent: December 1, 2020
    Assignee: Exelixis, Inc.
    Inventors: Dana T. Aftab, Nathan Guz, Stephen Lau, Noel Hamill, Tracy Walker, Jana Galbraith, Simon Yau, Khalid Shah
  • Patent number: 10793541
    Abstract: Disclosed herein is a process of making a compound of formula I The compound of formula I is an inhibitor of MEK and thus can be used to treat cancer.
    Type: Grant
    Filed: February 8, 2019
    Date of Patent: October 6, 2020
    Assignees: Exelixis, Inc., Genentech, Inc.
    Inventors: Sriram Naganathan, Nathan Guz, Matthew Pfeiffer, C. Gregory Sowell, Tracy Bostick, Jason Yang, Amit Srivastava, Neel Kumar Anand
  • Patent number: 10736886
    Abstract: Methods of treating cancer by administering a compound of Formula I, or a pharmaceutically acceptable salt or solvate thereof, in combination with other cancer treatments are described, wherein R1 is halo; R2 is halo; and Q is CH or N.
    Type: Grant
    Filed: January 18, 2019
    Date of Patent: August 11, 2020
    Assignee: Exelixis, Inc.
    Inventors: Dana T. Aftab, Thomas Mueller, Aaron Weitzman, Jaymes Holland
  • Patent number: 10590102
    Abstract: This disclosure relates to the crystalline fumarate salt of (S)-[3,4-difluoro-2-(2-fluoro-4-iodophenylamino)phenyl] [3-hydroxy-3-(piperidin-2-yl) azetidin-1-yl]-methanone. The disclosure also relates to pharmaceutical compositions comprising the crystalline fumarate salt of (S)-[3,4-difluoro-2-(2-fluoro-4-iodophenylamino)phenyl] [3-hydroxy-3-(piperidin-2-yl) azetidin-1-yl]-methanone. The disclosure also relates to methods of treating cancers comprising administering to a patient in need thereof the crystalline fumarate salt of (S)-[3,4-difluoro-2-(2-fluoro-4-iodophenylamino)phenyl] [3-hydroxy-3-(piperidin-2-yl) azetidin-1-yl]-methanone.
    Type: Grant
    Filed: December 22, 2017
    Date of Patent: March 17, 2020
    Assignee: EXELIXIS, INC.
    Inventor: Adrian St. Clair Brown
  • Patent number: 10543206
    Abstract: The present invention is directed to processes for making and compositions containing quinolines such as formula I or pharmaceutically acceptable salts thereof wherein: X1 is H, Br, Cl, or X2 is H, Br, Cl, or n1 is 1-2; and n2 is 1-2.
    Type: Grant
    Filed: October 4, 2018
    Date of Patent: January 28, 2020
    Assignee: Exelixis, Inc.
    Inventors: Jo Ann Wilson, Khalid Shah
  • Patent number: 10501418
    Abstract: The invention relates to novel crystalline solid forms of the chemical compound N-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-N?-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide (Compound 1), and solvates thereof, including hydrates, that are useful for the treatment of cancer. Also disclosed are pharmaceutical compositions comprising the crystalline solid forms and processes for making the crystalline solid forms, as well as methods of using them for the treatment of cancer, particularly thyroid cancer, prostate cancer, hepatocellular cancer, renal cancer, and non-small cell lung carcinoma. The crystalline solid forms can be used to make the L-malate salt of cabozantinib.
    Type: Grant
    Filed: February 16, 2015
    Date of Patent: December 10, 2019
    Assignee: Exelixis, Inc.
    Inventors: Dana T. Aftab, Nathan Guz, Stephen Lau, Noel Hamill, Tracy Walker, Jana Galbraith, Simon Yau, Khalid Shah
  • Patent number: 10328069
    Abstract: Methods are provided for treating a lymphoproliferative malignancy to a patient in need of such treatment, comprising administering to the patient an effective amount of compound A as described herein.
    Type: Grant
    Filed: May 19, 2017
    Date of Patent: June 25, 2019
    Assignee: EXELIXIS, INC.
    Inventors: Arthur DeCillis, Joanne Lager
  • Patent number: 10273211
    Abstract: The invention relates to metabolites of cabozantinib (I) as well as uses thereof.
    Type: Grant
    Filed: March 17, 2014
    Date of Patent: April 30, 2019
    Assignee: Exelixis, Inc.
    Inventors: Dana T. Aftab, Sriram Naganathan, Wei Xu, Steven Lacy, Linh Nguyen
  • Patent number: 10239858
    Abstract: Disclosed herein is a process of making a compound of formula I The compound of formula I is an inhibitor of MEK and thus can be used to treat cancer.
    Type: Grant
    Filed: August 25, 2017
    Date of Patent: March 26, 2019
    Assignees: EXELIXIS, INC., GENENTECH, INC.
    Inventors: Sriram Naganathan, Nathan Guz, Matthew Pfeiffer, C. Gregory Sowell, Tracy Bostick, Jason Yang, Amit Srivastava, Neel Kumar Anand