Patents Assigned to Exelixis, Inc.
  • Method for treating osteoporosis
    Patent number: 10166225
    Abstract: This invention is directed to the treatment of osteoporosis using N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N?-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide.
    Type: Grant
    Filed: September 20, 2012
    Date of Patent: January 1, 2019
    Assignee: Exelixis, Inc.
    Inventors: Dana T. Aftab, Douglas Clary
  • Dosing of cabozantinib formulations
    Patent number: 10159666
    Abstract: The invention relates to administration of various pharmaceutical formulations of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N?-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, (cabozantinib) a c-Met inhibitor, and its metabolites, to achieve desirable pharmacokinetic and pharmacodynamic effects.
    Type: Grant
    Filed: March 17, 2015
    Date of Patent: December 25, 2018
    Assignee: Exelixis, Inc.
    Inventors: Dana T. Aftab, Sriram Naganathan, Wei Xu, Steven Lacy
  • Processes for preparing quinoline compounds and pharmaceutical compositions containing such compounds
    Patent number: 10123999
    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: November 10, 2016
    Date of Patent: November 13, 2018
    Assignee: Exelixis, Inc.
    Inventor: Jo Ann Wilson
  • Inhibitors of PI3K-delta and methods of their use and manufacture
    Patent number: 10053470
    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: April 27, 2017
    Date of Patent: August 21, 2018
    Assignee: Exelixis, Inc.
    Inventor: James William Leahy
  • C-Met modulator pharmaceutical compositions
    Patent number: 10039757
    Abstract: Pharmaceutical compositions and unit dosage forms comprising Compound I are disclosed.
    Type: Grant
    Filed: February 7, 2017
    Date of Patent: August 7, 2018
    Assignee: Exelixis, Inc.
    Inventors: Jo Ann Wilson, Khalid Shah
  • ROR? modulators
    Patent number: 10035790
    Abstract: Described are RORy modulators of the formula (I), and N-oxides thereof, and pharmaceutically acceptable salts thereof, and solvates and hydrates thereof, wherein R1, R2, R3, R4, R5, R6, Ra, x, y, L, G, Z, the bond denoted by “q”, the ring system denoted by “A” and the ring system denoted by “B” are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORy activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORy activity, for example, autoimmune and/or inflammatory disorders.
    Type: Grant
    Filed: October 17, 2013
    Date of Patent: July 31, 2018
    Assignees: Exelixis, Inc., Bristol-Myers Squibb Co.
    Inventors: Wei Xu, Yong Wang, Sunghoon Ma, Elena S. Koltun, Byung Gyu Kim, Joon Won Jeong, T. G. Murali Dhar, Lynne Canne Bannen
  • C-met modulator pharmaceutical compositions
    Patent number: 10034873
    Abstract: Pharmaceutical compositions and unit dosage forms comprising Compound I are disclosed.
    Type: Grant
    Filed: June 2, 2017
    Date of Patent: July 31, 2018
    Assignee: Exelixis, Inc.
    Inventors: Jo Ann Wilson, Khalid Shah
  • Process for preparing quinoline derivatives
    Patent number: 9969692
    Abstract: A process for preparing a compound of Formula I is disclosed, comprising the steps: wherein: R1 is halo; R2 is halo; R3 is (C1-C6)alkyl or (C1-C6)alkyl optionally substituted with heterocycloalkyl; R4 is (C1-C6)alkyl; and Q is CH or N; comprising: (a) contacting 1,1-cyclopropane dicarboxylic acid with thionyl chloride in a polar aprotic solvent; (b) adding and a tertiary amine base to the mixture of step (a) to form a compound of Formula A; and (c) coupling a compound of Formula A with an amine of Formula B to form a compound of Formula I.
    Type: Grant
    Filed: April 20, 2016
    Date of Patent: May 15, 2018
    Assignee: Exelixis, Inc.
    Inventors: Jo Ann Wilson, Sriram Naganathan, Neil G. Andersen, Matthew Pfeiffer
  • Method of treating cancer
    Patent number: 9861624
    Abstract: This invention is directed to the treatment of cancer, particularly castration-resistant prostate cancer and osteolytic bone metastases, with a dual inhibitor of MET and VEGF.
    Type: Grant
    Filed: May 2, 2013
    Date of Patent: January 9, 2018
    Assignee: Exelixis, Inc.
    Inventor: Dana T. Aftab
  • Malate salt of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N?(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, and crystalline forms therof for the treatment of cancer
    Patent number: 9809549
    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: July 25, 2014
    Date of Patent: November 7, 2017
    Assignee: Exelixis, Inc.
    Inventors: Adrian St. Clair Brown, Peter Lamb, William P. Gallagher
  • Process for making compounds for use in the treatment of cancer
    Patent number: 9771347
    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: April 13, 2015
    Date of Patent: September 26, 2017
    Assignee: Exelixis, Inc.
    Inventors: Sriram Naganathan, Nathan Guz, Matthew Pfeiffer, C. Gregory Sowell, Tracy Bostick, Jason Yang, Amit Srivastava
  • Inhibitors of PI3K-Delta and Methods of Their Use and Manufacture
    Publication number: 20170226131
    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: April 27, 2017
    Publication date: August 10, 2017
    Applicant: Exelixis, Inc.
    Inventor: James William Leahy
  • Drug Combination to Treat Melanoma
    Publication number: 20170224670
    Abstract: This invention relates to the combination of vemurafenib and the heat shock protein 90 (HSP90) inhibitor XL888 to treat melanoma, particularly BRAF V600 mutant melanoma in patients in need of such treatment.
    Type: Application
    Filed: October 14, 2015
    Publication date: August 10, 2017
    Applicant: Exelixis, Inc.
    Inventor: Keiran Smalley
  • C-met modulator pharmaceutical compositions
    Patent number: 9724342
    Abstract: Pharmaceutical compositions and unit dosage forms comprising Compound I are disclosed.
    Type: Grant
    Filed: July 18, 2011
    Date of Patent: August 8, 2017
    Assignee: Exelixis, Inc.
    Inventors: Jo Ann Wilson, Khalid Shah
  • Processes for preparing quinoline compounds and pharmaceutical compositions containing such compounds
    Patent number: 9717720
    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 10, 2012
    Date of Patent: August 1, 2017
    Assignee: Exelixis, Inc.
    Inventors: Jo Ann Wilson, Khalid Shah
  • Inhibitors of PI3K-delta and methods of their use and manufacture
    Patent number: 9670212
    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: September 14, 2011
    Date of Patent: June 6, 2017
    Assignee: Exelixis, Inc.
    Inventor: James William Leahy
  • Crystalline Solid Forms of N--N'-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide, Processes for Making, and Methods of Use
    Publication number: 20170044106
    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: Application
    Filed: February 16, 2015
    Publication date: February 16, 2017
    Applicant: Exelixis, Inc.
    Inventors: Dana T. Aftab, Nathan Guz, Stephen Lau, Noel Hamill, Tracy Walker, Jana Galbraith, Simon Yau, Khalid Shah
  • Process for preparing quinoline derivatives
    Patent number: 9365516
    Abstract: A process for preparing a compound of Formula I is disclosed: wherein: R1 is halo; R2 is halo; R3 is (C1-C6)alkyl or (C1-C6)alkyl optionally substituted with heterocycloalkyl; R4 is (C1-C6)alkyl; and Q is CH or N; comprising: (a) contacting 1,1-cyclopropane dicarboxylic acid with thionyl chloride in a polar aprotic solvent; (b) adding and a tertiary amine base to the mixture of step (a) to form a compound of Formula A; and (c) coupling a compound of Formula A with an amine of Formula B to form a compound of Formula I.
    Type: Grant
    Filed: October 22, 2012
    Date of Patent: June 14, 2016
    Assignee: Exelixis, Inc.
    Inventors: Jo Ann Wilson, Sriram Naganathan, Neil G. Andersen, Matthew Pfeiffer
  • Inhibitors of PI3K-delta and methods of their use and manufacture
    Patent number: 9346807
    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: September 14, 2011
    Date of Patent: May 24, 2016
    Assignee: Exelixis, Inc.
    Inventor: Patrick Kearney
  • Cabozantinib Dosage Form and Use in the Treatment of Cancer
    Publication number: 20160022662
    Abstract: This invention relates to a dosage form of cabozantinib and a method of employing the dosage form to treat cancer.
    Type: Application
    Filed: April 4, 2014
    Publication date: January 28, 2016
    Applicant: Exelixis, Inc.
    Inventor: Arthur DeCillis