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.
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
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
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.
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.
Abstract: The present disclosure provides CD47 binding agents (e.g., antibodies, including multispecific antibodies, such as bispecific antibodies) and uses thereof.
Abstract: The present disclosure provides PD-L1 binding agents (e.g., antibodies, including multispecific antibodies, such as bispecific antibodies) and uses thereof.
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
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: 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: 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: 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.
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
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
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
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.