Patents Assigned to Metabasis Therapeutics, Inc.
  • Publication number: 20070179114
    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:
    Type: Application
    Filed: November 6, 2006
    Publication date: August 2, 2007
    Applicants: Metabasis Therapeutics, Inc., Merck & Co., Inc.
    Inventors: Mark Erion, K. Reddy, Malcolm MacCoss, David Olsen
  • Patent number: 7214668
    Abstract: Prodrugs of Formula I, their uses, their intermediates, and their method of manufacture are described: wherein: M and V are cis to one another and MPO3H2 is a phosphonic acid selected from the group consisting of 9-(2-phosphonylmethoxyethyl)adenine, (R)-9-(2-phosphonylmethoxy propyl)adenine, 9-(2-phosphonylmethoxyethyl)guanine, 9-(2-phosphonylmethoxy ethyloxy)adenine, 9-(2-phosphonylmethoxyethyl)-2,6-diaminopurine, (S)-1-(3-hydroxy-2-phosphonylmethoxypropyl)cytosine, (S)-9-(3-hydroxy-2-phosphonylmethoxypropyl)adenine, 9-(3-hydroxy-2-phosphonylmethoxypropyl)guanine, and (S)-9-(3-fluoro-2-phosphonyl methoxypropyl)adenine; V is selected from a group consisting of phenyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-furanyl, 3-furanyl, 2-thienyl, and 3-thienyl, all optionally substituted with 1-3 substituents selected from a group consisting of F, Cl, Br, C1-C3 alkyl, CF3 and OR6; R6 is selected from the group consisting of C1-C3 alkyl, and CF3; and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: May 12, 2003
    Date of Patent: May 8, 2007
    Assignee: Metabasis Therapeutics, Inc.
    Inventors: K. Raja Reddy, Mark D. Erion, Michael C. Matelich, Joseph J. Kopcho
  • Patent number: 7205404
    Abstract: Novel cyclic phosphoramidate prodrugs of drugs of formula I in their use in delivery of drugs to the liver, their use in enhancing oral bioavailability, and their method of preparation are described.
    Type: Grant
    Filed: March 3, 2000
    Date of Patent: April 17, 2007
    Assignee: Metabasis Therapeutics, Inc.
    Inventors: Mark D. Erion, K. Raja Reddy, Serge H. Boyer
  • Patent number: 7193081
    Abstract: The method of preparing compounds of Formula I is described: wherein: M and V are cis to one another and MPO3H2 is a phosphonic acid selected from the group consisting of 9-(2-phosphonylmethoxyethyl)adenine, and (R)-9-(2-phosphonylmethoxypropyl)adenine; wherein V is phenyl, optionally substituted with 1–2 substituents selected from a group consisting of fluoro, chloro, and bromo; comprising: coupling a chiral 1-phenylpropane-1,3-diol, wherein the phenyl may be optionally substituted, with MPOCl2 or an N-6 substituted analogue thereof. Additionally, methods and salt forms are described that enable isolation and purification of the desired isomer.
    Type: Grant
    Filed: May 12, 2003
    Date of Patent: March 20, 2007
    Assignee: Metabasis Therapeutics, Inc.
    Inventors: Joseph J. Kopcho, K. Raja Reddy, Michael C. Matelich, Bheemarao G. Ugarkar
  • Publication number: 20070042989
    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:
    Type: Application
    Filed: October 30, 2006
    Publication date: February 22, 2007
    Applicant: Metabasis Therapeutics, Inc.
    Inventors: K. Reddy, Mark Erion
  • Patent number: 7151092
    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.
    Type: Grant
    Filed: October 31, 2003
    Date of Patent: December 19, 2006
    Assignee: Metabasis Therapeutics, Inc.
    Inventors: Serge Boyer, Mark D. Erion
  • Patent number: 7148349
    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: October 31, 2003
    Date of Patent: December 12, 2006
    Assignee: Metabasis Therapeutics, Inc.
    Inventors: K. Raja Reddy, William Craigo, Zhili Sun, Serge Boyer, Bheemarao G. Ugarkar
  • Patent number: 6967193
    Abstract: Novel purine compounds of the Formula 1, pharmacuetically acceptable prodrugs and salts thereof, and their use as fructose 1,6-bisphosphatase inhibitors
    Type: Grant
    Filed: July 7, 2003
    Date of Patent: November 22, 2005
    Assignee: Metabasis Therapeutics, Inc.
    Inventors: Qun Dang, Mark D. Erion, M. Rami Reddy, Edward D. Robinson, Srinivas Rao Kasibhatla, K. Raja Reddy
  • Patent number: 6965033
    Abstract: Novel bisamidate phosphonate prodrugs of FBPase inhibitors of the Formula IA: and their use in the treatment of diabetes and other conditions associated with elevated blood glucose.
    Type: Grant
    Filed: December 22, 2000
    Date of Patent: November 15, 2005
    Assignee: Metabasis Therapeutics, Inc.
    Inventors: Tao Jiang, Srinivas Rao Kasibhatla, K. Raja Reddy
  • Patent number: 6946115
    Abstract: Prodrugs of formula I, their uses, their intermediates, and their method of manufacturing are described: and pharmaceutically acceptable prodrugs and salts thereof.
    Type: Grant
    Filed: October 15, 2001
    Date of Patent: September 20, 2005
    Assignee: Metabasis Therapeutics, Inc.
    Inventors: Mark D. Erion, K. Raja Reddy, Edward D. Robinson, Bheemarao G. Ugarkar
  • Patent number: 6919322
    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: March 7, 2001
    Date of Patent: July 19, 2005
    Assignee: Metabasis Therapeutics, Inc.
    Inventors: Brett C. Bookser, Qun Dang, K. Raja Reddy
  • Patent number: 6756360
    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.
    Type: Grant
    Filed: December 22, 1999
    Date of Patent: June 29, 2004
    Assignee: Metabasis Therapeutics, Inc.
    Inventors: Mark D. Erion, Paul D. van Poelje
  • Patent number: 6752981
    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 responsible for the overproduction of the biochemical end product, e.g. glucose (diabetes); cholesterol, fatty acids and triglycerides (hyperlipidemia) (atherosclerosis) (obesity). In one apsect, 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.
    Type: Grant
    Filed: September 8, 2000
    Date of Patent: June 22, 2004
    Assignee: Metabasis Therapeutics, Inc.
    Inventors: Mark D. Erion, K. Raja Reddy
  • Patent number: 6680379
    Abstract: This invention relates to novel human organic anion transporter polypeptides and genes encoding such polypeptides. The invention is directed towards the isolation, characterization and use of human organic anion transporter polypeptides for pharmacological screening of substrates, analogues of substrates, and modulators of human organic anion proteins. This invention also provides cell cultures, which stably contain nucleic acid sequences encoding human organic anion transport polypeptides. Such cell lines are useful for screening compounds in vitro to identify and characterize modulators, inhibitors and substrates of human organic anion transporter polypeptides.
    Type: Grant
    Filed: July 12, 2000
    Date of Patent: January 20, 2004
    Assignee: Metabasis Therapeutics, Inc.
    Inventor: William Sun
  • Patent number: 6489476
    Abstract: FBPase inhibitors of the formula I and X are useful in the treatment of diabetes and other conditions associated with elevated blood glucose or excess glycogen storage.
    Type: Grant
    Filed: September 3, 1999
    Date of Patent: December 3, 2002
    Assignee: Metabasis Therapeutics, Inc.
    Inventors: Qun Dang, Srinivas Rao Kasibhatla, K. Raja Reddy, Mark D. Erion, M. Rami Reddy, Atul Agarwal
  • Publication number: 20020173490
    Abstract: Novel bisamidate phosphonate prodrugs of FBPase inhibitors of the Formula IA: 1
    Type: Application
    Filed: December 22, 2000
    Publication date: November 21, 2002
    Applicant: METABASIS THERAPEUTICS, INC.
    Inventors: Tao Jiang, Srinivas Rao Kasibhatla, K. Raja Reddy
  • Patent number: 6399782
    Abstract: Novel benzimidazole compounds of the following structure and their use as fructose-1,6-bisphosphatase inhibitors is described
    Type: Grant
    Filed: April 11, 2000
    Date of Patent: June 4, 2002
    Assignee: Metabasis Therapeutics, Inc.
    Inventors: Srinivas Rao Kasibhatla, K. Raja Reddy, Mark D. Erion, Qun Dang, Gerard R. Scarlato, M. Rami Reddy
  • Publication number: 20020040014
    Abstract: Novel FBPase inhibitors of the formula I 1
    Type: Application
    Filed: March 7, 2001
    Publication date: April 4, 2002
    Applicant: Metabasis Therapeutics, Inc.
    Inventors: Brett C. Bookser, Qun Dang, K. Raja Reddy
  • Patent number: 6312662
    Abstract: Prodrugs of formula I, their uses, their intermediates, and their method of manufacture are described:
    Type: Grant
    Filed: September 8, 1999
    Date of Patent: November 6, 2001
    Assignee: Metabasis Therapeutics, Inc.
    Inventors: Mark D. Erion, K. Raja Reddy, Edward D. Robinson, Bheemarao G. Ugarkar
  • Patent number: 6294672
    Abstract: The present invention is directed towards novel azaindole compounds which bind to the AMP site and are potent FBPase inhibitors. The present invention also is directed towards the clinical use of the novel FBPase inhibitors as a method of treatment or prevention of diseases responsive to lowered blood glucose levels.
    Type: Grant
    Filed: January 5, 2000
    Date of Patent: September 25, 2001
    Assignee: Metabasis Therapeutics, Inc.
    Inventors: K. Raja Reddy, Gerard R. Scarlato, Qun Dang, Mark D. Erion, Srinivas Rao Kasibhatla, M. Rami Reddy