Novel nucleotide analogues as percursor molecules for...

C - Chemistry – Metallurgy – 07 – F

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C07F 9/38 (2006.01) A61K 31/662 (2006.01) A61P 31/12 (2006.01)

Patent

CA 2669450

This invention relates to a purine or pyrimidine phosphonate compound of formula (I) or pharmaceutically acceptable salt thereof; wherein B, X, and R1-R3 are as defined in classes and subclasses herein. These compounds may be used as antiviral precursors. The invention also relates to therapeutic compositions of these compounds and their use for the preparation of a medication for treating and/or preventing a viral infection in a patient. The invention also provides methods for making these compounds. In particular, the invention provides an H- phosphinate precursor intermediate of formula (II) wherein B is a purine or pyrimidine base as defined herein and R1 is selected from the group comprising a hydrogen atom, and a methyl, ethyl, hydroxymethyl, hydroxyethyl and C1-6haloalkyl group.

La présente invention concerne un composé de phosphonate de purine ou de pyrimidine de formule (I) ou un sel pharmaceutiquement acceptable de celui-ci ; dans laquelle B, X et R1-R3 sont tels que définis dans les présentes classes et sous-classes. Ces composés peuvent être utilisés en tant que précurseurs d'antiviraux. L'invention concerne également des compositions thérapeutiques de ces composés et leur utilisation pour la préparation d'un médicament destiné au traitement et/ou à la prévention d'une infection virale chez un patient. L'invention concerne également des procédés de fabrication de ces composés. En particulier, L'invention concerne un intermédiaire précurseur de H-phosphinate de formule (II) dans laquelle B est une base purique ou pyrimidique telle que définie ici et R1 est choisi dans le groupe comprenant un atome d'hydrogène et un groupe méthyle, éthyle, hydroxyméthyle, hydroxyéthyle et haloalkyle en C1-6.

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