Abstract: The present disclosure provides NKG2A binding agents (e.g, antibodies, including monospecific and multispecific antibodies such as bispecific antibodies) and uses thereof.
Abstract: The present disclosure provides multispecific binding agents that bind to NKG2A and PD-L1 (e.g., multispecific antibodies such as bispecific antibodies) and uses thereof.
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:
May 7, 2024
Date of Patent:
July 14, 2026
Assignee:
Exelixis, Inc.
Inventors:
Frenel DeMorin, Khalid Shah, Sagar Shakya, Peter Wong, Courtney S. Johnson, Melanie Janelle Bevill, Stephan D. Parent
Abstract: The present disclosure provides PD-L1 binding agents (e.g., antibodies, including multispecific antibodies, such as bispecific antibodies) and uses thereof.
Abstract: The present invention relates to combinations comprising a checkpoint inhibitor and a c-Met inhibitor, Compound 1. The invention also relates to crystalline forms of the free base of Compound 1, as well as crystalline forms of salts of Compound 1, in combination with a checkpoint inhibitor. The invention further relates to methods of treating cancer by administering Compound 1 as a single agent or a combination described herein.
Type:
Grant
Filed:
July 29, 2021
Date of Patent:
July 7, 2026
Assignee:
Exelixis, Inc.
Inventors:
Gisela Schwab, Christian Scheffold, Colin Chong, Ssucheng Jeff Hsu, Peter Lamb, Peiwen Yu
Abstract: The present disclosure provides 4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine compounds of formula (I), which are therapeutically useful as USP1 inhibitors. These compounds are useful in the treatment and/or prevention of diseases and/or disorders responsive to the inhibition of USP1 proteins and USP1 activity. Compounds of the present disclosure are especially useful for treating cancer. The present disclosure also provides processes for preparation of the compounds and pharmaceutical formulations comprising at least one of the compounds of formula (I) or a pharmaceutically acceptable salt or a stereoisomer thereof.
Type:
Application
Filed:
October 20, 2023
Publication date:
June 4, 2026
Applicant:
EXELIXIS, INC.
Inventors:
Chandrasekhar ABBINENI, Susanta SAMAJDAR, Madhu AELURI, Scott SIMONOVICH
Abstract: Disclosed herein are compounds of Formula (I) which inhibit, regulate and/or modulate tyrosine kinase receptors, particularly Axl and Mer signal transduction pathways related to the changes in cellular activities, compositions containing the compounds, methods of using the compounds to treat kinase-dependent diseases and conditions, and methods for making the compounds.
Type:
Grant
Filed:
June 3, 2020
Date of Patent:
December 23, 2025
Assignee:
Exelixis, Inc.
Inventors:
Lynne Canne Bannen, Minna Bui, Faming Jiang, Kin Tso, Yong Wang, Wei Xu
Abstract: The present invention relates to processes for the synthetic preparation of c-Met inhibitors of Formula I, or pharmaceutically acceptable salts thereof. The present invention further relates to processes for the synthetic preparation of the c-Met inhibitor, Compound 1, or a pharmaceutically acceptable salt thereof. The present invention also relates to processes for the synthetic preparation of Compound 1·hemifumarate. The invention further relates to large scale processes for the synthetic preparation of the c-Met inhibitor, Compound 1 and Compound 1·hemifumarate.
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:
August 2, 2023
Date of Patent:
December 2, 2025
Assignee:
Exelixis, Inc.
Inventors:
Dana T. Aftab, Nathan Guz, Stephen Lau, Noel Hamill, Tracy Walker, Jana Galbraith, Simon Yau, Khalid Shah
Abstract: The present disclosure provides 5T4 binding agents (e.g., antibodies, including multispecific antibodies such as bispecific antibodies, and antibody-drug conjugates) and uses thereof.
Type:
Application
Filed:
May 10, 2023
Publication date:
October 23, 2025
Applicant:
EXELIXIS, INC.
Inventors:
Bonnie HAMMER, Jeffrey N. HIGAKI, Seema KANTAK, Charles KAPLAN
Abstract: The present disclosure relates generally to compounds and pharmaceutical compositions suitable as modulators of protein kinases, and methods for their use in treating disorders mediated, at least in part by, protein kinases.
Type:
Grant
Filed:
September 25, 2020
Date of Patent:
July 29, 2025
Assignee:
Exelixis, Inc.
Inventors:
Lynne Bannen, Minna Bui, Faming Jiang, Jack Maung, Andrew Raub, Justin Salvant, Benjamin Spangler, Kin Tso, Yong Wang, Wei Xu
Abstract: The present disclosure provides multispecific binding agents (e.g., antibodies, such as bispecific antibodies) that have a first binding domain that binds to CD47, including human CD47, and one or more additional binding domains that bind to one or more targets that are not CD47, such as PD-L1 and uses thereof.
Type:
Application
Filed:
February 8, 2023
Publication date:
June 19, 2025
Applicant:
EXELIXIS, INC.
Inventors:
Bryan GLASER, Bonnie HAMMER, Seema KANTAK, Bee-Cheng SIM, Justin A. WETTER
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
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.
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).
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.
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.