Polyethyleneglycol-modified lipid compounds and uses thereof
View Patent ↗The present invention provides compositions comprising polytheylyene-dialkyloxypropyl conjugates (PEG-DAA), liposomes, SNALP, and SPLP comprising such compositions, and methods of using such compositions, liposomes, SNALP, and SPLP.
1. A compound of Formula I:
wherein:
R 1 and R 2 are independently selected and are alkyl groups having from about 10 to about 20 carbon atoms;
PEG is a polyethyleneglycol, wherein the terminal hydroxyl group is substituted with a methyl group; and
L is a carbamate linker moiety.
2. The compound in accordance with claim 1 , wherein R 1 and R 2 are selected from the group consisting of lauryl (C12), myristyl (C14), palmityl (C16), stearyl (C18) and icosyl (C20).
3. The compound in accordance with claim 1 , wherein R 1 and R 2 are the same.
4. The compound in accordance with claim 3 , wherein R 1 and R 2 are both myristyl (C14).
5. The compound in accordance with claim 3 , wherein R 1 and R 2 are both palmityl (C16).
6. The compound in accordance with claim 3 , wherein R 1 and R 2 are both stearyl (C18).
7. The compound in accordance with claim 1 , wherein said alkyl groups are saturated.
8. The compound in accordance with claim 1 , wherein said alkyl groups are unsaturated.
9. The compound in accordance with claim 1 , wherein said PEG has an average molecular weight ranging from about 550 daltons to about 10,000 daltons.
10. The compound in accordance with claim 9 , wherein said PEG has an average molecular weight ranging from about 750 to about 5,000 daltons.
11. The compound in accordance with claim 9 , wherein said PEG has an average molecular weight ranging from about 1,000 to about 5,000 daltons.
12. The compound in accordance with claim 9 , wherein said PEG has an average molecular weight ranging from about 1,500 to about 3,000 daltons.
13. The compound in accordance with claim 9 , wherein said PEG has an average molecular weight of about 2,000 daltons.
14. The compound in accordance with claim 1 , having the formula
wherein PEG is a polyethyleneglycol, wherein the terminal hydroxyl group is substituted with a methyl group.
15. The compound in accordance with claim 14 , wherein L has a formula selected from the group consisting of:
wherein the dashed line indicates the point of attachment to the PEG terminal oxygen and the wavy line indicates the point of attachment to the rest of the compound.