Amine-containing lipids and uses thereof

Details Amine-containing lipids and uses thereof Amine-containing lipids and uses thereof

C - Chemistry, Metallurgy

07

C

C07C 229/12 (2006.01) A61K 9/107 (2006.01) A61K 9/127 (2006.01) A61K 47/34 (2006.01) C07C 229/16 (2006.01) C07C 237/06 (2006.01) C07D 233/61 (2006.01) C07K 17/02 (2006.01) C12N 15/87 (2006.01) C12N 15/88 (2006.01) A61K 48/00 (2006.01)

Patent

CA 2611944

Nitrogen-containing lipids prepared from the conjugate addition of amines to acrylates, acrylamides, or other carbon-carbon double bonds conjugated to electron-withdrawing groups are described. Methods of preparing these lipids from commercially available starting materials are also provided. These amine- containing lipids or salts forms of these lipids are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the amino moiety of these lipids, they are particularly suited for the delivery of polynucleotides. Complexes or nanoparticles containing the inventive lipid and polynucleotide have been prepared. The inventive lipids may also be used to in preparing microparticle for drug delivery. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings.

Lipides contenant de l'azote élaborés à partir de l'adjonction conjuguée d'amines à des acrylates, acrylamides, ou autres liaisons doubles carbone-carbone en conjugaison avec des groupes de retrait d'électron. Procédés d'élaboration de ces lipides à partir de matériaux de départ disponibles dans le commerce. De préférence, ces lipides ou sels correspondants sont biodégradables et biocompatibles et peuvent être utilisés dans une variété de systèmes de délivrance de médicaments. Compte tenu de leur fraction amino, ces lipides sont particulièrement appropriés à la délivrance de polynucléotides. On a élaboré des complexes ou nanoparticules contenant les lipides considérés, qui peuvent aussi être utilisés dans la fabrication de microparticules pour la délivrance de médicaments. Ils sont particulièrement utiles pour la délivrance d'agents labiles compte tenu de leur capacité à tamponner le pH environnant.

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