TH5481A - Antiviral compounds - Google Patents

Abstract

This invention concerns pyrimidine nucleosides substituted at position 5 and their pharmacologically acceptable derivatives, and their uses in the treatment or prevention of varicella zoster virus, sitomegalovirus, and Epstein-Barr virus infections. Furthermore, it reveals the pharmaceutical formulations and methods for preparing the various compounds described in this invention.

Claims (5)

1. The process for preparing compound formula I (chemical formula) involves condensing compound formula II (chemical formula) to form compound formula III (chemical formula) to obtain compound formula IV (chemical formula) to obtain compound formula V (chemical formula): i) eliminate any remaining protective groups; ii) when the resulting compound is compound formula (I), transform it into a pharmacopoeia acceptable derivative of those substances, or when the resulting compound is a pharmacopoeia acceptable derivative, transform it into another pharmacopoeia acceptable derivative or compound formula I. 2. Procedure for preparing the compounds under claim 1, where R3 is benzoyl, X is ethinyl, R2 is methyl, and R1 is oxide. 3. Procedure for preparing the compounds under claim 1, where X is ethinyl, R2 is methyl, and R1 is imino. 4. Preparation methods for a) 2-deoxy-5-(1-propineyl)citidine and/or b) 3-n-benzoyl-2-deoxy-5-propineyluricin 5. The procedure for preparing a pharmaceutical compound consisting of compounds of formula Ia (chemical formula), condensing compounds of formula II (chemical formula) (formula), and compounds of formula IV (chemical formula) to obtain compounds of formula V (chemical formula): i. Eliminate all remaining protective groups; ii. When the compounds of formula Ia are converted to pharmaceutically acceptable derivatives of those compounds, or when the compounds of which are pharmaceutically acceptable derivatives are converted to another pharmaceutically acceptable derivative or compounds of formula Ia, and (2) combine the resulting compounds of formula Ia with at least one other drug compound to obtain the aforementioned pharmaceutical compound. (Clause 5, page 7, 0 figures)