Neutral-cationic lipid for nucleic acid and drug delivery

C - Chemistry – Metallurgy – 07 – D

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C07D 233/54 (2006.01) A61K 9/127 (2006.01) A61K 47/00 (2006.01) A61K 48/00 (2006.01) A61P 43/00 (2006.01) C07C 271/28 (2006.01) C07H 5/06 (2006.01)

Patent

CA 2386164

A lipid represented by formula (I), wherein each of R1 and R2 is an alkyl or alkenyl chain having between about 8 to about 24 carbon atoms; n = 1-20; L is selected from the group consisting of (i) -X-(C=O)-Y-CH2-, (ii) -X-(C=O)-, and (iii) -X-CH2-, wherein X and Y are independently selected from oxygen, NH and a direct bond; and Z is a weakly basic moiety that has a pK of less than about 7.4 and greater than about 4.0 is described.

L'invention concerne un lipide correspondant à la formule (I) dans laquelle chacun des R¿1? et R¿2? est une chaîne alkyle ou alcényle possédant entre 8 et environ 24 atomes de carbone; n=1-20; L est sélectionné dans le groupe constitué de (i) -X-(C=O)-Y-CH¿2?-, (ii) -X-(C=O)- et (iii) -X-CH¿2?- dans lequel X et Y sont indépendamment sélectionnés parmi l'oxygène, NH et un lien direct; et Z est un groupe fonctionnel basique faible qui possède un pK inférieur à environ 7,4 mais supérieur à environ 4,0.

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