Cationic lipid compounds which comprise at least two cationic groups. The cationic lipid compounds are particularly suitable for use as carriers in the intracellular delivery of bioactive agents, including pharmaceuticals and genetic material. Compositions of the present cationic lipid compounds inc
Cationic lipid compounds which comprise at least two cationic groups. The cationic lipid compounds are particularly suitable for use as carriers in the intracellular delivery of bioactive agents, including pharmaceuticals and genetic material. Compositions of the present cationic lipid compounds include suspensions, emulsions, micelles and liposomes.
대표청구항▼
[ We claim:] [1.] A cationic lipid compound of the formula: [ STR 22 ] wherein: each of x, y and z is independently an integer from 0 to about 100;each X.sub.1 is independently --O--, --S--, --NR.sub.5 --, --C(.dbd.X.sub.2)--, --C(.dbd.X.sub.2)--N(R.sub.5)--, --N(R.sub.5)--C(.dbd.X.sub.2)--, --C(.db
[ We claim:] [1.] A cationic lipid compound of the formula: [ STR 22 ] wherein: each of x, y and z is independently an integer from 0 to about 100;each X.sub.1 is independently --O--, --S--, --NR.sub.5 --, --C(.dbd.X.sub.2)--, --C(.dbd.X.sub.2)--N(R.sub.5)--, --N(R.sub.5)--C(.dbd.X.sub.2)--, --C(.dbd.X.sub.2)--O--, --O--C(.dbd.X.sub.2)-- or --X.sub.2 --(R.sub.5 X.sub.2)P(.dbd.X.sub.2)--X.sub.2 --;each X.sub.2 is independently O or S;each Y.sub.1 is independently a phosphate residue, N(R.sub.6).sub.a --, S(R.sub.6).sub.a --, P(R.sub.6).sub.a -- or --CO.sub.2 R.sub.6, wherein a is an integer from 1 to 3;each Y.sub.2 is independently --N(R.sub.6).sub.b --, --S(R.sub.6).sub.b -- or --P(R.sub.6).sub.b --, wherein b is an integer from 0 to 2;each Y.sub.3 is independently a phosphate residue, N(R.sub.6).sub.a --, S(R.sub.6).sub.a --, P(R.sub.6).sub.a -- or --CO.sub.2 R.sub.6, wherein a is an integer from 1 to 3;each of R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is independently alkylene of 2 to about 20 carbons;each R.sub.5 is independently hydrogen or alkyl of 1 to about 10 carbons; andeach R.sub.6 is independently --[R.sub.7 --X.sub.3 ].sub.c --R.sub.8 or --R.sub.9 --[X.sub.4 --R.sub.10 ].sub.d --Q, wherein:each of c and d is independently an integer from 0 to about 100;each Q is independently a phosphate residue, --N(R.sub.11).sub.q, --S(R.sub.11).sub.q, --P(R.sub.11).sub.q or --CO.sub.2 R.sub.11, wherein q is an integer from 1 to 3;each of X.sub.3 and X.sub.4 is independently --O--, --S--, --NR.sub.5 --, --C(.dbd.X.sub.2)--, --C(.dbd.X.sub.2)--N(R.sub.5)--, --N(R.sub.5)--C(.dbd.X.sub.2)--, --C(.dbd.X.sub.2)--O--, --O--C(.dbd.X.sub.2)-- or --X.sub.2 --(R.sub.5 X.sub.2)P(.dbd.X.sub.2)--X.sub.2 --;each R.sub.7 is independently alkylene of 2 to about 20 carbons;each R.sub.8 is independently hydrogen or alkyl of 1 to about 60 carbons;each of R.sub.9 and R.sub.10 is independently alkylene of 2 to about 20 carbons; andeach R.sub.11 is independently --[R.sub.7 --X.sub.3 ].sub.c --R.sub.8 or --R.sub.9 --[X.sub.4 --R.sub.10 ].sub.d --W, wherein:each W is independently a phosphate residue, --N(R.sub.12).sub.w, --S(R.sub.12).sub.w, --P(R.sub.12).sub.w or --CO.sub.2 R.sub.12, wherein w is an integer from 1 to 3; andR.sub.12 is --[R.sub.7 --X.sub.3 ].sub.c --R.sub.8 ; with the proviso that the compound of formula (I) comprises at least two quaternary salts.
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