Patent ID: 11872285
Assignee: LIFE TECHNOLOGIES CORPORATION
Field: Pharmaceuticals (Chemistry)
Classification: CPC A  C | IPC A  C

Claim 0:
1. A lipid aggregate comprising a first cationic lipid and at least a second cationic lipid, a first neutral lipid and optionally a second neutral lipid, wherein said lipid aggregate is suitable for forming a cationic complex with a nucleic acid under aqueous conditions, wherein said first and second cationic lipids are different from each other, and wherein said first or second cationic lipids have the structure:, , and salts thereof;
where:
R1 and R2, independently, are an alkyl, alkenyl or alkynyl groups, having from 8 to 30 carbon atoms;
an alkyl, alkenyl or alkynyl groups, having from 8 to 30 carbon atoms and optionally substituted by one or more of an alcohol, an aminoalcohol, an amine, an amide, an ether, a polyether, an ester, a mercaptan, alkylthio, or a carbamoyl group or where R1 is —(CH2)q—N(R6)tR7R8;
R3 and R4, independently, are hydrogens, —(CH2)p—NH2, an alkyl, an alkenyl or alkynyl groups substituted by one or more of an alcohol, an aminoalcohol, an amine, an amide, an ether, a polyether, an ester, a mercaptan, alkylthio, or a carbamoyl group;
R5-R8 are hydrogens;
R9 is a hydrogen, or an alkyl, alkenyl or alkynyl group, a carbohydrate or a peptide;
r, s and t are 1 or 0 to indicate the presence or absence of the indicated R group, when any of r, s or t are 1 the nitrogen to which the indicated R group is attached is positively charged and wherein at least one of r, s or t is 1;
p and q are independently an integer ranging from 1 to 6, inclusive;
Xv− is an anion, where v is the valency of the anion and A is the number of anions;
L is a divalent organic radical capable of covalently linking the two nitrogens selected from:
(CH2)n, where n is an integer ranging from 1 to 10, inclusive, which is optionally substituted with one or more ZR10 groups, where Z is O or S, and R10 is hydrogen or an alkyl, alkenyl or alkynyl group; or
{—(CH2)k—Y—(CH2)m}p—, where k and m, independently, are integers ranging from 1 to 10, inclusive, and p is an integer ranging from 1 to 6, inclusive, and Y is O, S, CO, COO, CONR11, NR11CO, or NR11COR11N where R11, independent of any other R11, is hydrogen or an alkyl group;

wherein one or more CH2 groups of the alkyl, alkenyl or alkynyl groups of R1-R4, R9 and R10 can be replaced with an O, S, S—S, CO, COO, NR12CO, NR12COO, or NR12CONR12 where R12, independent of any other R12, is hydrogen or an alkyl, alkenyl or alkynyl group; and
wherein the alkyl, alkenyl or alkynyl groups of R1-R4 and R9-R12 are optionally substituted with one or more OR13, CN, halogens, N(R13)2, peptide, or carbohydrate groups where R13 is hydrogen, and
wherein at least one of R3 and R4, when present as alkyl groups, are substituted with both OR13 and N(R13)2 groups.