College Place, NJ, United States
College Place, NJ, United States

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Sofia M.J.,Pharmasset Inc.
Antiviral chemistry & chemotherapy | Year: 2011

HCV infection is a significant worldwide health problem and is a major cause of hepatocellular carcinoma. The current standard of care, interferon and ribavirin, is only effective against a proportion of the patient population infected with HCV. To address the shortcomings of existing therapy, the development of direct acting antiviral agents is under investigation. The HCV RNA dependent RNA polymerase is an essential enzyme for viral replication and is therefore a logical target against which to develop novel anti-HCV agents. Nucleosides have been shown to be effective as antiviral agents for other viral diseases and therefore, have been investigated as inhibitors of HCV replication. The development of prodrugs of nucleoside 5'-monophosphates has been pursued to address limitations associated with poor nucleoside phosphorylation. This is required to produce the nucleoside 5'-triphosphate which is the anabolite that is the actual inhibitor of the polymerase enzyme. Prodrugs of nucleoside 5'-monophosphates have been developed that enable their delivery into cells and in vivo into the liver. The implementation of these prodrug strategies has ultimately led to the identification of several prodrugs of nucleoside 5'-monophosphates that are potent inhibitors of HCV replication in vitro. They have progressed into the clinic and the early data demonstrate greatly reduced viral load levels in HCV-infected patients. This review will survey the state of nucleotide prodrugs for the treatment of HCV.


Patent
Pharmasset Inc. | Date: 2011-07-20

The disclosed invention provides compositions and methods of treating a Flaviviridae infection, including hepatitis C virus, West Nile Virus, yellow fever virus, and a rhinovirus infection in a host, including animals, and especially humans, using a (2R)-2-deoxy-2-fluoro-2-C-methyl nucleosides, or a pharmaceutically acceptable salt or prodrug thereof.


Patent
Pharmasset Inc. | Date: 2012-01-19

Disclosed herein are compounds useful for treating a viral infection, such as HCV.


Patent
Pharmasset Inc. | Date: 2012-02-13

The present invention is directed to a method and composition of treating or preventing viral infections, in particular, human immunodeficiency virus (HIV) and hepatitis B virus (HBV) infections, in human patients or other animal hosts, comprising the administration of N.sup.4-acyl-2,3-dideoxy-5-fluorocytidine or N.sup.4-acyl-2,3-didehyd-ro-2,3-dideoxy-5-fluorocytidine, and pharmaceutically acceptable salts, prodrugs, and other derivatives thereof.


Disclosed herein is a method for administering an abbreviated hepatitis C virus (HCV) treatment regimen for an HCV-infected, rs12979860 single nucleotide polymorphism (SNP) (C/C) patient, which comprises: administering to said patient an effective amount of each of a direct-acting antiviral, pegylated interferon alfa-2a, and ribavirin; wherein the abbreviated HCV treatment regimen is less than 48 weeks. Also disclosed herein is a method of detecting an rs12979860 single nucleotide polymorphism (SNP) in a hepatitis C virus (HCV) infected patient comprising: detecting the rs12979860 SNP of chromosome 19 in a biological sample from a patient, wherein an rs12979860 SNP C/C patient is administered an abbreviated treatment regimen with a direct-acting antiviral agent in combination with peginterferon alfa-2a and ribavirin; and wherein the abbreviated HCV treatment regimen is less than 48 weeks.


Patent
Pharmasset Inc. | Date: 2011-07-20

The disclosed invention provides compositions and methods of treating a Flaviviridae infection, including hepatitis C virus, West Nile Virus, yellow fever virus, and a rhinovirus infection in a host, including animals, and especially humans, using a (2R)-2-deoxy-2-fluoro-2-C-methyl nucleosides, or a pharmaceutically acceptable salt or prodrug thereof.


The present invention provides a method to prepare anti-HCV nucleosides containing the 2-deoxy-2-fluoro-2-C-methyl--D-ribofuranosyl nucleosides from a preformed, preferably naturally-occurring, nucleoside.


Patent
Pharmasset Inc. | Date: 2011-07-20

The disclosed invention provides compositions and methods of treating a Flaviviridae infection, including hepatitis C virus, West Nile Virus, yellow fever virus, and a rhinovirus infection in a host, including animals, and especially humans, using a (2R)-2-deoxy-2-fluoro-2-C-methyl nucleosides, or a pharmaceutically acceptable salt or prodrug thereof.


Patent
Pharmasset Inc. | Date: 2011-03-31

Disclosed herein are phosphorus-containing actives, their use as actives for treating diseases, and a stereoselective process for preparing the same. Also disclosed herein are useful synthetic intermediates and processes for preparing the same.


Patent
Pharmasset Inc. | Date: 2011-03-31

Disclosed herein are nucleoside phosphoramidates and their use as agents for treating viral diseases. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful as inhibitors of HCV NS5B polymerase, as inhibitors of HCV replication and for treatment of hepatitis C infection in mammals.

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