The hepatitis B virus–trimera mouse: A model for human HBV infection and evaluation of anti-HBV therapeutic agents

A method and composition for the treatment of HIV and HBV infections in humans is disclosed that includes administering an effective amount of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane, a pharmaceutically acceptable derivative thereof, including a 5' or N4 alkylated or acylated derivative, or a pharmaceutically acceptable salt thereof, in a pharmaceutically acceptable carrier. A process for the resolution of a racemic mixture of nucleoside enantiomers is also disclosed that includes the step of exposing the racemic mixture to an enzyme that preferentially catalyzes a reaction in one of the enantiomers.

Antiviral activity and resolution of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane

The present invention relates to a method of preparing the antiviral compounds 2'-deoxy-5-fluoro-3'thiacytidine (FTC) and various prodrug analogues of FTC from inexpensive precursors with the option of introducing functionality as needed; methods of using these compounds, particularly in the prevention and treatment of AIDS; and the compounds themselves. This synthetic route allows the stereoselective preparation of the biologically active isomer of these compounds and related compounds.

Method for the synthesis, compositions and use of 2'-deoxy-5-fluoro-3'-thiacytidine and related compounds

The present invention relates to a method of preparing BCH-189 and various analogs of BCH-189 from inexpensive precursors with the option of introducing functionality as needed. This synthetic route allows the stereoselective preparation of the biologically active isomer of these compounds, β-BCH-189 and related compounds. Furthermore, the steochemistry at the nucleoside 4' position can be controlled to produce enantiomerically-enriched β-BCH-189 and its analogs.

Method and compositions for the synthesis of bch-189 and related compounds

https://aasldpubs.onlinelibrary.wiley.com/doi/epdf/10.1053/jhep.2000.9632

Preclinical evaluation of two human anti-hepatitis B virus (HBV) monoclonal antibodies in the HBV-trimera mouse model and in HBV chronic carrier chimpanzees.

Disclosed are processes for preparing compounds of the formula (I) and pharmaceutically acceptable salts or esters thereof: ##STR1## wherein R2 is a purine or pyrimidine base or an analogue or derivative thereof; and Z is S, S═O or SO2. The invention also relates to intermediates of use in the preparation of these compounds.

Processes for preparing substituted 1,3-oxathiolanes with antiviral properties

The present invention relates to highly diastereoselective processes for production of cis-nucleosides and nucleoside analogues and derivatives in high optical purity and intermediates useful in those processes.

Processes for the diastereoselective synthesis of nucleosides

The present invention relates to highly diastereoselective processes for production of cis-nucleotides and nucleoside analogues and derivatives in high optical purity and intermediates useful in those processes.

Processes for the diastereo-selective synthesis of nucleosides

The present invention relates to highly diastereoselective processes for production of cis-nucleosides and nucleoside analogues and derivatives in high optical purity, and intermediates useful in those processes.

Processes for the diastereoselective synthesis of nucleoside analogues

Disclosed are processes for preparing compounds of formula (I) and pharmaceutically acceptable salts or esters thereof, wherein R2 is a purine or pyrimidine base or an analogue or derivative thereof; and Z is S, S = O or SO2. The invention also relates to intermediates of use in the preparation of these compounds.

Tse Allan H L

Papers

Processes for preparing substituted 1,3-oxathiolanes with antiviral properties

Processes for the diastereoselective synthesis of nucleosides

Processes for the diastereo-selective synthesis of nucleosides

Processes for the diastereoselective synthesis of nucleoside analogues

Process for Preparing Substituted 1,3-Oxathiolanes with Antiviral Properties