Abstract: Provided herein are substituted imidazo[1,2-a]pyridines useful as inhibitors of BMP signaling. The invention further provides pharmaceutical compositions of the compounds of the invention. The invention also provides medical uses of substituted imidazo[1,2-a]pyridines.
Type:
Grant
Filed:
March 14, 2019
Date of Patent:
August 18, 2020
Assignees:
Vanderbuilt University, La Jolla Pharmaceuticals Company
Inventors:
Corey R. Hopkins, Matthew Ritter, Charles C. Hong, Anish Vadukoot, Darren W. Engers, Craig W. Lindsley
Abstract: This invention provides compounds, compositions, and methods for treating a disorder selected from cancer, hyperinsulinemia, hypoglycemia, hyperinsulinemia with hypoglycemia, atypical Parkinson's disease, Huntington's disease, multiple systems atrophy, GM3 synthase deficiency, GM2 synthase deficiency or tauopathy.
Abstract: The present invention relates to a novel endoglycoceramidase whose hydrolytic activity has been substantially reduced or eliminated, such that the enzyme is useful for synthesis of glycolipids from a monosaccharide or oligosaccharide and a ceramide. More specifically, the endoglycoceramidase is a mutant version of a naturally occurring endoglycoceramidase, preferably comprising a mutation within the active site or the nucleophilic site of the enzyme and more preferably comprising a substitution mutation of the Glu residue within the active site or the nucleophilic site. Also disclosed are a method for generating the mutant endoglycoceramidase and a method for enzymatically synthesizing glycolipids using this mutant enzyme.
Type:
Grant
Filed:
June 29, 2015
Date of Patent:
May 21, 2019
Assignees:
La Jolla Pharmaceutical Company, The University of British Columbia
Inventors:
Karl F. Johnson, Shawn Defrees, Stephen Withers, Mark Vaughan
Abstract: The invention provides methods for the treatment of diseases and conditions relating to galectin 3 using a galectin-3 inhibitor, such as a modified pectin (e.g., GCS-100). Also described are methods for conjoint therapy, and methods for assessing and/or monitoring the effects of a galectin-3 inhibitor, e.g., to adapt the dosing regimen of the inhibitor during therapy.
Abstract: The present disclosure relates to the use of angiotensin II in therapeutic methods for the treatment of renal failure, especially renal failure associated with cirrhosis.
Abstract: The present disclosure relates to the use of angiotensin II in therapeutic methods for the treatment of renal failure, especially renal failure associated with cirrhosis.
Abstract: The present invention is directed to methods and compositions for augmenting treatment of cancers and other proliferative disorders. In particular embodiments, the invention combines the administration of an agent that inhibits the anti-apoptotic activity of galectin-3 (e.g., a “galectin-3 inhibitor”) so as to potentiate the toxicity of a chemotherapeutic agent. In certain preferred embodiments, the conjoint therapies of the present invention can be used to improve the efficacy of those chemotherapeutic agents whose cytotoxicity is influenced by the status of an anti-apoptotic Bcl-2 protein for the treated cell. For instance, galectin-3 inhibitors can be administered in combination with a chemotherapeutic agent that interferes with DNA replication fidelity or cell-cycle progression of cells undergoing unwanted proliferation.