Cationic lipids and methods of use therefor

C - Chemistry – Metallurgy – 12 – N

Patent

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Details

C12N 15/88 (2006.01) A61K 9/127 (2006.01) A61K 31/7088 (2006.01) A61K 47/24 (2006.01) A61K 47/44 (2006.01) A61K 47/48 (2006.01) A61K 48/00 (2006.01)

Patent

CA 2268900

The present invention relates generally to a non-toxic lipid conjugated with a cationic amino acid containing a guanidino group. Specifically, the naturally- occurring lipid DOPE is combined with the naturally-occurring amino acid Arginine. These compounds are useful for encapsulating and delivering pharmaceuticals and poly and oligonucleotides. These compound improve over current compounds, because they are composed of non-toxic and, in the case of Arg-DOPE, natural components, and therefore result in minimal unwwanted side effects. Methods of use of the cationic lipids are also claimed.

La présente invention concerne généralement un lipide non toxique conjugué avec un acide aminé cationique contenant un groupe guanidino. Spécifiquement, le lipide d'origine naturelle dioléoylphosphatidyléthanolamine (DOPE) est combiné avec l'acide aminé d'origine naturelle arginine. Lesdits composés sont utiles pour enrober et administrer des substances pharmaceutiques et des polynucléotides et oligonucléotides. Ils présentent une amélioration par rapport aux composés actuels parce qu'ils sont composés de composants non toxiques, et naturels dans le cas de Arg-DOPE, et entraînent donc des effets secondaires non désirés minimes. Des procédés d'utilisation desdits lipides cationiques sont également décrits.

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