Abstract: Compounds of Formula I, stereoisomers, and pharmaceutically acceptable salts or prodrugs thereof, their preparation, and their uses for the treatment of hepatitis C viral infection are described:
Abstract: The present invention is directed toward the use of thyromimetic compounds that are thyroid receptor ligands, pharmaceutically acceptable salts thereof, and to prodrugs of these compounds for preventing, treating, or ameliorating fatty liver diseases such as steatosis, non-alcoholic fatty liver disease, and non-alcoholic steatohepatitis.
Abstract: Methods for the synthesis of cyclic phosphonic acid diesters from 1,3-diols are described, whereby cyclic phosphonic acid diesters are produced by reacting a chiral 1,3-diol and an activated phosphonic acid in the presence of a Lewis acid.
Abstract: Compounds of Formula I, their preparation and uses are described: wherein: M and V are cis to one another and MH is cytarabine; the 5? oxygen of said cytarabine is attached to the phosphorus; V is 4-pyridyl; and pharmaceutically acceptable prodrugs and salts thereof.
Abstract: Compounds of Formulae I-XVI, stereoisomers, and pharmaceutically acceptable salts or prodrugs thereof, their preparation, and their uses for the treatment of viral diseases including hepatitis C viral infection, cancer, diabetes, and other diseases are described: formula (I).
Abstract: The present invention relates to compounds of phosphonic acid-containing T3 mimetics and monoesters thereof, stereoisomers, pharmaceutically acceptable salts, co-crystals, and prodrugs thereof and pharmaceutically acceptable salts and co-crystals of the prodrugs, as well as their preparation and uses for preventing and/or treating metabolic diseases such as obesity, NASH, hypercholesterolemia and hyperlipidemia, as well as associated conditions such as atherosclerosis, coronary heart disease, impaired glucose tolerance, metabolic syndrome x and diabetes.
Type:
Grant
Filed:
May 26, 2005
Date of Patent:
April 7, 2009
Assignee:
Metabasis Therapeutics, Inc.
Inventors:
Mark D. Erion, Hongjian Jiang, Serge H. Boyer
Abstract: Compounds of Formula I, their preparation and synthetic intermediates, and their use in the synthesis of prodrugs: wherein: V and L are trans relative to one another; V is selected from group consisting of carbocyclic aryl, substituted carbocyclic aryl, heteroaryl, and substituted heteroaryl; and L is a leaving group selected from the group consisting of halogen, alkyl sulfonate, aryloxy optionally substituted with 1-2 substituents, N-containing heteroaryl, and N-hydroxy-nitrogen containing heteroaryl; and salts thereof.
Type:
Grant
Filed:
September 28, 2006
Date of Patent:
March 3, 2009
Assignee:
Metabasis Therapeutics, Inc.
Inventors:
K. Raja Reddy, William Craigo, Zhili Sun, Serge Boyer, Bheemarao G. Ugarkar
Abstract: Compounds and compositions are provided for modulating the activity of protein tyrosine phosphatases. In one embodiment, the compounds and compositions are thiazoles and thiadiazoles that inhibit the activity of protein tyrosine phosphatase 1B.
Type:
Grant
Filed:
September 2, 2005
Date of Patent:
June 3, 2008
Assignee:
Metabasis Therapeutics, Inc.
Inventors:
Zacharia S. Cheruvallath, Colin J. Loweth, Ruth F. Nutt, Darryl Rideout, Joseph E. Semple, Jing Wang, Feiyue Wu, Shankari Mylvaganam, Hengyi Zhu, Jianzhong Sun
Abstract: Novel FBPase inhibitors of the formula I are useful in the treatment of diabetes and other conditions associated with elevated blood glucose.
Type:
Grant
Filed:
January 25, 2005
Date of Patent:
May 13, 2008
Assignee:
Metabasis Therapeutics, Inc.
Inventors:
Brett C. Bookser, Qun Dang, K. Raja Reddy
Abstract: Prodrugs of formula I, their uses, their intermediates, and their method of manufacture are described: and pharmaceutically acceptable prodrugs and salts thereof.
Type:
Grant
Filed:
June 3, 2005
Date of Patent:
April 1, 2008
Assignee:
Metabasis Therapeutics, Inc.
Inventors:
Mark D. Erion, K. Raja Reddy, Edward D. Robinson, Bheemarao G. Ugarkar
Abstract: Compounds and compositions are provided for modulating the activity of protein tyrosine phosphatases. The compounds for use in the compositions and methods provided herein have formulae (I) Protein tyrosine phosaphatase, including PTB-IB, mediated diseases and disorders include diabetes including Type 1 and Type 2 diabetes (and associated complications such as hypertension, ischemic diseases of the large and small blood vessels, blindness, circulatory problems, kidney failure and atherosclerosis), syndrome X, metabolic syndrome, glucose intolerance, insulin resistance, obesity, cancer, and neurodegenerative diseases.
Type:
Application
Filed:
January 17, 2006
Publication date:
March 20, 2008
Applicant:
Metabasis Therapeutics, Inc.
Inventors:
Zacharia Cheruvallath, Joseph Semple, Vasanthakumar Rajappan, Darryl Rideout, Venkatachalapathi Yalamoori, Chung-Ying Tsai, Feiyue Wu, Lars Thoresen, Mark Shenderovich
Abstract: Novel FBPase inhibitors of the formula I and X are useful in the treatment of diabetes and other conditions associated with elevated blood glucose.
Type:
Application
Filed:
August 20, 2007
Publication date:
January 17, 2008
Applicant:
Metabasis Therapeutics, Inc.
Inventors:
Qun Dang, Srinivas Kasibhatla, K. Reddy, Mark Erion, M. Reddy, Atul Agarwal
Abstract: Pharmaceutical compositions containing an FBPase inhibitor and an insulin sensitizer are provided as well as methods for treating diabetes and diseases responding to increased glycemic control, an improvement in insulin sensitivity, a reduction in insulin levels, or an enhancement of insulin secretion.
Abstract: Novel FBPase inhibitors of the formula I and X are useful in the treatment of diabetes and other conditions associated with elevated blood glucose.
Type:
Grant
Filed:
August 6, 2003
Date of Patent:
December 25, 2007
Assignee:
Metabasis Therapeutics, Inc.
Inventors:
Qun Dang, Srinivas Rao Kasibhatla, K. Raja Reddy, Mark D. Erion, M. Rami Reddy, Atul Agurwal
Abstract: The present invention is directed towards novel cyclic phosph(oramid)ate prodrugs of alcohol-, amine-, and thiol-containing drugs, their preparation, their synthetic intermediates, and their uses. Another aspect of the invention is the use of the prodrugs to treat diseases that benefit from enhanced drug distribution to the liver and like tissues and cells that express cytochrome P450, including hepatitis, cancer, liver fibrosis, malaria, other viral and parasitic infections, and metabolic diseases where the liver is responsible for the overproduction of the biochemical end product, e.g. glucose (diabetes); cholesterol, fatty acids and triglycerides (hyperlipidemia) (atherosclerosis) (obesity). In one aspect, the invention is directed towards the use of the prodrugs to enhance oral drug delivery. In another aspect, the prodrugs are used to prolong pharmacodynamic half-life of the drug. In addition, the prodrug methodology of the current invention is used to achieve sustained delivery of the parent drug.
Abstract: Novel cyclic phosphoramidate prodrugs of drugs of formula I their use in delivery of drugs to the liver, their use in enhancing oral bioavailability, and their method of preparation are described.
Abstract: Novel purine compounds of Formula 1, pharmaceutically acceptable prodrugs and salts thereof, and their use as fructose 1,6-bisphosphatase inhibitors.
Type:
Grant
Filed:
April 7, 2005
Date of Patent:
October 23, 2007
Assignee:
Metabasis Therapeutics, Inc.
Inventors:
Qun Dang, Mark D. Erion, M. Rami Reddy, Edward D. Robinson, Srinivas Rao Kasibhatla, K. Raja Reddy
Abstract: Novel FBPase inhibitors of the formula I and X are useful in the treatment of diabetes and other conditions associated with elevated blood glucose.
Type:
Application
Filed:
April 30, 2007
Publication date:
October 4, 2007
Applicant:
Metabasis Therapeutics, Inc.
Inventors:
Qun Dang, Srinivas Kasibhatla, K. Reddy, Mark Erion, M. Reddy, Atul Agarwal