BIODEGRADABLE COMPOUND, LIPID PARTICLE, COMPOSITION CONTAINING LIPID PARTICLE, AND KIT
First Claim
Patent Images
1. A compound represented by the following formula (1):
-
Q-L-CHR2 (1)(wherein,Q is a non-cationic aliphatic group that does not contain nitrogen but contains oxy;
L is a single bond or an aliphatic group containing no nitrogen;
Rs are C12-C24 aliphatic groups, the same or different; and
at least one R contains, in the main chain or side chain thereof, a linking group LR selected from the group consisting of —
C(═
O)—
O—
, —
O—
C(═
O)—
, —
O—
C(═
O)—
O—
, —
S—
C(═
O)—
, —
C(═
O)—
S—
, —
C(═
O)—
NH—
, and —
NH—
C(═
O)—
).
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Accused Products
Abstract
The compound according to the present embodiment is represented by the following formula (1):
Q-L—CHR2 (1)
(wherein,
- Q is a non-cationic aliphatic group that does not contain nitrogen but contains oxy;
- L is a single bond or an aliphatic group containing no nitrogen; Rs are C12-C24 aliphatic group, the same or different; and at least one R contains, in the main chain or side chain thereof, a linking group LR selected from the group consisting of —C(═O)—O—, —O—C(═O)—, —O—C(═O)—O—, —S—C(═O)—, —C(═O)—S—, —C(═O)—NH—, and —NH—C(═O)—).
-
Citations
21 Claims
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1. A compound represented by the following formula (1):
-
Q-L-CHR2 (1)(wherein, Q is a non-cationic aliphatic group that does not contain nitrogen but contains oxy; L is a single bond or an aliphatic group containing no nitrogen; Rs are C12-C24 aliphatic groups, the same or different; and
at least one R contains, in the main chain or side chain thereof, a linking group LR selected from the group consisting of —
C(═
O)—
O—
, —
O—
C(═
O)—
, —
O—
C(═
O)—
O—
, —
S—
C(═
O)—
, —
C(═
O)—
S—
, —
C(═
O)—
NH—
, and —
NH—
C(═
O)—
).- View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21)
(wherein LA is alkylene or cycloalkylene that is optionally substituted independently with oxygen; LO is an ester structure selected from the group consisting of —
C(═
O)—
O—
, —
O—
C(═
O)—
O—
, —
O—
C(═
O)—
O—
, —
S—
C(═
O)—
, and —
C(═
O)—
S—
, and a is independently a number from 0 to
6).
-
-
4. The compound according to claim 3, wherein the Q is represented by the following formula (1B-1):
-
QO—
[(CH2)b1—
O—
]2-
(1B-1)(wherein QO is hydrogen, halogen, alkyl, or alkenyl; b1 is a number from 0 to 3; b2 is a number from 1 to 3; and the total number of carbon atoms contained in the formula (1B) is 6 or less).
-
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5. The compound according to claim 3, wherein the Q is represented by the following formula (1B-2):
-
Q1-LB-
(1B-2)(wherein, Q1 is a cyclo ether; and LB is alkylene.)
-
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6. The compound according to claim 1, wherein the at least one R is represented by the following formula (1C):
-
—
LC1—
C(═
O)—
O-LC2
(1C)(wherein, LC1 is alkylene; and LC2 is alkenyl).
-
-
7. The compound according to claim 6, wherein the LC1 and the LC2 are represented by the following formulae (1C-1) and (1C-2) respectively:
-
—
(CH2)c1—
(1C-1)
—
CH2—
CH═
CH—
(CH2)c2—
H
(1C-2)(wherein c1 is a number from 1 to 10; and c2 is a number from 1 to 10.)
-
-
8. The compound according to claim 7, wherein the c1 is a number from 4 to 8.
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9. The compound according to claim 1, wherein the longest molecular chain contained in the R has 8 or more atoms.
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10. The compound according to claim 1, presented by the following formulae (1-01) to (1-20).
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11. A lipid particle comprising the compound according to claim 1.
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12. The lipid particle according to claim 11, further comprising a membrane-forming lipid and an aggregation-reducing lipid.
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13. The lipid particle according to claim 12, wherein the membrane-forming lipid is selected from the group consisting of
1,2-dioleoyl-sn-glycero-3-phosphoethanol amine (DOPE), 1,2-stearoyl-sn-glycero-3-phosphoethanol amine (DSPE), 1,2-dipalmitoyl-sn-glycero-3-phosphatidylcholine (DPPC), 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphatidylcholine (POPC), 1,2-di— - O—
octadecyl-3-trimethylammonium propane (DOTMA),1,2-dioleoyl-3-dimethylammonium propane (DODAP), 1,2-dimyristoyl-3-di methylammonium propane (14;
0 DAP),1,2-dipalmitoyl-3-dimethylammonium propane (16;
0 DAP),1,2-distearoyl-3-dimethylammonium propane (18;
0 DAP),N-(4-carboxybenzyl)-N,N-dimethyl-2,3-bis(oleoyloxy)propane (DOBAQ), 1,2-dioleoyl-3-trimethylammonium propane (DOTAP), 1,2-dioleoyl-sn-glycero-3-phosphochlorine (DOPC), 1,2-dilinoleoyl-sn-glycero-3-phosphochlorine (DLPC), 1,2-dioleoyl-sn-glycero-3-phospho-L-serine (DOPS), cholesterol, and the like; and wherein the aggregation-reducing lipid is a polyethylene glycol (PEG)-modified lipid.
- O—
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14. The lipid particle according to claim 11, further comprising an active agent.
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15. The lipid particle according to claim 14, wherein the active agent is a nucleic acid selected from the group consisting of plasmids, oligonucleotides, polynucleotides, siRNAs, micro RNAs, DNAs, aptamers, and ribozymes.
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16. The lipid particle according to claim 15, further comprising a compound that binds to a nucleic acid.
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17. The lipid particle according to claim 16, wherein the compound that binds to a nucleic acid is a basic protein or a basic peptide.
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18. The lipid particle according to claim 16, wherein the compound that binds to a nucleic acid is a protamine or a histone.
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19. The lipid particle according to claim 16, further comprising a compound that regulates the expression of a nucleic acid in a cell.
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20. A composition comprising the lipid particle according to claim 11 and a carrier.
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21. A kit comprising the lipid particle according to claim 11 and a composition containing an incorporation agent for incorporating the lipid particle into a cell.
Specification