Patents Assigned to Exelixis, Inc.
  • Patent number: 12275706
    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-ffuorophenyl)cyclopropane-1,1-dicarboxamide.
    Type: Grant
    Filed: November 25, 2024
    Date of Patent: April 15, 2025
    Assignee: Exelixis, Inc.
    Inventors: Adrian St. Clair Brown, Peter Lamb, William P. Gallagher
  • Patent number: 12264161
    Abstract: Heterocyclic compounds useful as antagonists of adenosine receptors, and methods of treatment of diseases using antagonists of adenosine receptors are disclosed herein. Also disclosed herein are pharmaceutical compositions and methods of administration of heterocyclic antagonists of adenosine receptors and processes for producing heterocyclic antagonists of adenosine receptors.
    Type: Grant
    Filed: May 25, 2023
    Date of Patent: April 1, 2025
    Assignee: Exelixis, Inc.
    Inventors: Sunghoon Ma, Yong Wang, Wei Xu
  • Patent number: 12227481
    Abstract: The invention relates to novel crystalline solid forms of salts of the chemical compound N-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-N?-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide, 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 renal cell carcinoma (RCC) and medullary thyroid cancer (MTC).
    Type: Grant
    Filed: June 29, 2023
    Date of Patent: February 18, 2025
    Assignee: Exelixis, Inc.
    Inventor: Khalid Shah
  • Patent number: 12195475
    Abstract: Disclosed herein are compounds of Formula (I?). Compounds of Formula (I?) inhibit, regulate and/or modulate kinase receptor, particularly Axl and Mer 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: June 13, 2023
    Date of Patent: January 14, 2025
    Assignee: Exelixis, Inc.
    Inventors: Lynne Canne Bannen, Minna Bui, Faming Jiang, Yong Wang, Wei Xu
  • Patent number: 12128039
    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, CI, or X2 is H, Br, CI, or n1 is 1-2; and n2 is 1-2.
    Type: Grant
    Filed: February 8, 2024
    Date of Patent: October 29, 2024
    Assignee: Exelixis, Inc.
    Inventors: Jo Ann Wilson, Khalid Shah
  • Patent number: 12017995
    Abstract: The present invention relates to crystalline forms of the free base of the c-Met inhibitor, Compound 1. The invention also relates to crystalline forms of salts of Compound 1. The invention also relates to pharmaceutical compositions comprising the solid polymorphs of the free base and salts of Compound 1. The invention further relates to methods of treating a disease, disorder, or syndrome mediated at least in part by modulating in vivo activity of a protein kinase.
    Type: Grant
    Filed: December 12, 2019
    Date of Patent: June 25, 2024
    Assignee: Exelixis, Inc.
    Inventors: Frenel DeMorin, Khalid Shah, Sagar Shakya, Peter Wong, Courtney S. Johnson, Melanie Janelle Bevill, Stephan D. Parent
  • Patent number: 12016854
    Abstract: This invention relates to a liquid pharmaceutical composition comprising cabozantinib to treat locally advanced or metastatic solid tumors, particularly advanced urothelial cancer or renal cell carcinoma in patients in need thereof.
    Type: Grant
    Filed: October 28, 2022
    Date of Patent: June 25, 2024
    Assignee: Exelixis, Inc.
    Inventors: Khalid Shah, Gisela Schwab, Steven Lacy
  • Patent number: 11969419
    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: Grant
    Filed: February 21, 2023
    Date of Patent: April 30, 2024
    Assignee: Exelixis, Inc.
    Inventors: David Smith, Maha Hussain
  • Patent number: 11760726
    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: March 25, 2021
    Date of Patent: September 19, 2023
    Assignee: Exelixis, Inc.
    Inventors: Dana T. Aftab, Nathan Guz, Stephen Lau, Noel Hamill, Tracy Walker, Jana Galbraith, Simon Yau, Khalid Shah
  • Patent number: 11718622
    Abstract: Heterocyclic compounds useful as antagonists of adenosine receptors, and methods of treatment of diseases using antagonists of adenosine receptors are disclosed herein. Also disclosed herein are pharmaceutical compositions and methods of administration of heterocyclic antagonists of adenosine receptors and processes for producing heterocyclic antagonists of adenosine receptors.
    Type: Grant
    Filed: March 15, 2021
    Date of Patent: August 8, 2023
    Assignee: Exelixis Inc.
    Inventors: Sunghoon Ma, Yong Wang, Wei Xu
  • Patent number: 11673897
    Abstract: Disclosed herein are compounds of Formula I?. Compounds of Formula I? inhibit, regulate and/or modulate kinase receptor, particularly Axl and Mer 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: January 25, 2019
    Date of Patent: June 13, 2023
    Assignee: Exelixis, Inc.
    Inventors: Lynne Canne Bannen, Minna Bui, Faming Jiang, Yong Wang, Wei Xu
  • Patent number: 11612597
    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: Grant
    Filed: June 18, 2020
    Date of Patent: March 28, 2023
    Assignee: Exelixis, Inc.
    Inventors: David Smith, Maha Hussain
  • Patent number: 11597699
    Abstract: Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.
    Type: Grant
    Filed: April 20, 2020
    Date of Patent: March 7, 2023
    Assignee: Exelixis, Inc.
    Inventors: Naing Aay, Neel Kumar Anand, Charles M. Blazey, Owen Joseph Bowles, Joerg Bussenius, Simona Costanzo, Jeffry Kimo Curtis, Steven Charles DeFina, Larisa Dubenko, Anagha Abhijit Joshi, Abigail R. Kennedy, Angie Inyoung Kim, Elena S. Koltun, Jean-Claire Limun Manalo, Csaba J. Peto, Kenneth D. Rice, Tsze H. Tsang
  • Patent number: 11564915
    Abstract: This invention relates to a dosage form of cabozantinib and a method of employing the dosage form to treat cancer.
    Type: Grant
    Filed: April 4, 2014
    Date of Patent: January 31, 2023
    Assignee: Exelixis, Inc.
    Inventor: Aaron Weitzman
  • Patent number: 11542259
    Abstract: Disclosed herein are compounds of formula I. Compounds of formula I inhibit, regulate and/or modulate kinase receptor, particularly Axl and Mer 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: January 25, 2019
    Date of Patent: January 3, 2023
    Assignee: Exelixis, Inc.
    Inventors: Lynne Canne Bannen, Minna Bui, Faming Jiang, Kin Tso, Yong Wang, Wei Xu
  • Patent number: 11504362
    Abstract: This invention relates to a liquid pharmaceutical composition comprising cabozantinib to treat locally advanced or metastatic solid tumors, particularly advanced urothelial cancer or renal cell carcinoma in patients in need thereof.
    Type: Grant
    Filed: June 8, 2018
    Date of Patent: November 22, 2022
    Assignee: Exelixis, Inc.
    Inventors: Khalid Shah, Gisela Schwab, Steven Lacy
  • Patent number: 11504363
    Abstract: This invention is directed to the treatment of cancer, particularly lung cancer, breast cancer, melanoma, renal cell carcinoma, thyroid cancer that has metastasized to the bone. The invention is also directed to a method for treating bone cancer pain in an individual in need of such treatment comprising administering to the individual an effective amount of a compound of Formula I.
    Type: Grant
    Filed: February 11, 2020
    Date of Patent: November 22, 2022
    Assignee: Exelixis, Inc.
    Inventors: Gisela Schwab, Dana T. Aftab
  • Patent number: 11433064
    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: July 2, 2020
    Date of Patent: September 6, 2022
    Assignee: Exelixis, Inc.
    Inventors: Dana T. Aftab, Thomas Mueller, Aaron Weitzman, Jaymes Holland
  • Patent number: 11414396
    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 26, 2020
    Date of Patent: August 16, 2022
    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: 11298349
    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, CI, or X2 is H, Br, CI, or n1 is 1-2; and n2 is 1-2.
    Type: Grant
    Filed: February 8, 2021
    Date of Patent: April 12, 2022
    Assignee: Exelixis, Inc.
    Inventors: Jo Ann Wilson, Khalid Shah