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US 2026/0184669 A1Published application
Lipid compound and composition for delivery of active substance
AssigneeKorea Research Institute of Bioscience and Biotechnology
InventorsYoonkyung KIM, Hae-Geun JEON, Hye-youn JUNG, Viet Cuong HO, Ji Yoon LEE
Life of this patent
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Abstract
Disclosed are a new lipid compound and a new lipid nanoparticle (LNP) composition comprising the lipid compound. The lipid compound according to the present disclosure may enhance the structural stability of an active substance by directly or indirectly binding to the active substance through multivalent interactions to encapsulate the active substance. In addition, the lipid nanoparticle composition comprising the lipid compound may significantly improve the intracellular delivery efficiency and activity of the active substance, therefore may be useful for the treatment and prevention of the disease.
Claims13
1:
- A lipid compound of the following Formula 1, an isomer thereof, or a salt thereof:
- wherein,
- R1 is hydrogen, hydroxy, C1-6 alkyl, C2-6 alkenyl, C1-6 alkoxy, C2-6 alkenyloxy, —CN, —NO2, —N(R)2, —C(═O)R, —C(═O)OR, —OC(═O)R, —C(═O)N(R)2, —NRC(═O)R, —NRC(═O)N(R)2, —NRC(═S)N(R)2, C3-14 cycloalkyl, 5- to 10-membered heteroaryl, 3- to 14-membered heterocyclyl, —O-5- to 10-membered heteroaryl, or —O-3- to 14-membered heterocyclyl, wherein C1-6 alkyl, C2-6 alkenyl, C1-6 alkoxy, C2-6 alkenyloxy, C3-14 cycloalkyl, 5- to 10-membered heteroaryl, 3- to 14-membered heterocyclyl, —O-5- to 10-membered heteroaryl or —O-3- to 14-membered heterocyclyl are each independently unsubstituted or substituted with 1 to 3 halogens or C1-6 alkyl;
- X1 is a simple bond, —CO—C1-6 alkyl, —CO—C2-6 alkenyl, —C(═O)NR—, —NRC(═O)—, —NRC(═O)NR—, —NRC(═S)NR—, C6-10 aryl, C3-14 cycloalkyl, 5- to 10-membered heteroaryl, 3- to 14-membered heterocyclyl, nucleobases, an amino acid monomer, or an amino acid oligomer, wherein —CO—C1-6 alkyl, —CO—C2-6 alkenyl, C6-10 aryl, C3-14 cycloalkyl, 5- to 10-membered heteroaryl, 3- to 14-membered heterocyclyl, a nucleobase, an amino acid monomer, and an amino acid oligomer are each independently unsubstituted or substituted with 1 to 3 halogens or C1-6 alkyl;
- L1 is C1-14 alkylene, C2-14 alkenylene, M, RaM, MRa, MRaM1, or RaMRb;
- n is an integer from 1 to 5, and in case n being from 2 to 5, X1 and L1 are each independently selected;
- L2 is C1-14 alkylene, C2-14 alkenylene, M, RaM, MRa, MRaM1, or RaMRb, and L2 is the same as or different from L1;
- Y is hydrogen, —(CH2)m OH, —(CH2)m SH or —(CH2)m SeH, wherein m is an integer from 0 to 5;
- R2 and R3 are each independently C1-30 alkyl, C2-30 alkenyl, or RcMRd wherein C1-30 alkyl and C2-30 alkenyl are each independently unsubstituted or substituted with 1 to 3 C1-16 alkyl or C2-16 alkenyl;
- M and M1 are each independently —NHC(═O)—, —C(═O)NH—, —C(═O)O—, —OC(═O)—, —C(═O)—, —NH—, —S—, —SS—, —O—, —S(═O)2-, —C(═O)S—, —SC(═O)—, —NHC(═O)NH—, —NHC(═O)O—, or —OC(═O)NH—;
- R is each independently hydrogen, C1-6 alkyl, C2-6 alkenyl, C3-14 cycloalkyl, 5- to 10-membered heteroaryl, or 3- to 14-membered heterocyclyl;
- Ra and Rb are independently —(CH2)l-, —C3-20 cycloalkyl-(CH2)l-, —(CH2)l-C3-20 cycloalkyl-, —C6-20 aryl-(CH2)l-, —(CH2)l-C6-20 aryl-, —NH—(CH2)l-, or —(CH2)—, wherein 1 is an integer from 0 to 10;
- Rc is C1-14 alkylene or C2-14 alkenylene;
- Rd is C1-20 alkyl, C2-20 alkenyl, or hydrogen, wherein C1-20 alkyl and C2-20 alkenyl are each independently unsubstituted or substituted with 1 to 3 C1-20 alkyl or C2-20 alkenyl;
- the heteroaryl is an aromatic heterocycle compromising 1 to 6 heteroatoms selected from N, O, and S, and the heterocycle is an aliphatic heterocycle compromising 1 to 6 heteroatoms selected from N, O, and S.
12 more elements
2:
- The lipid compound, an isomer thereof, or a salt thereof of claim 1, wherein
- the compound of the Formula 1 is a compound of Formula 2:
- wherein,
- j and k are independently an integer of 1 to 12;
- M2 and M3 are each independently —NHC(═O)—, —C(═O)NH—, —C(═O)O—, —OC(═O)—, —C(═O)—, —NH—, —S—, —SS—, —O—, —S(O)2-, —C(═O)S—, —SC(═O)—, —NHC(═O)NH—, —NHC(═O)O—, or —OC(═O)NH;
- and
- R4, R5, R6, and R7 are each independently hydrogen, C1-24 alkyl, or C2-24 alkenyl, wherein the C1-24 alkyl and C2-24 alkenyl are each independently unsubstituted or substituted with 1 to 3 C1-20 alkyl or C2-20 alkenyl.
4 more elements
3:
- The lipid compound, an isomer thereof, or a salt thereof of claim 1, wherein
- R1 is hydrogen, hydroxy, C1-6 alkyl, C1-6 alkoxy, —CN, —NO2, —NH2, —C(═O)—C1-3 alkyl, —C(═O)NH2, —NHC(═O)—C1-3 alkyl, —NHC(═O)NH2, or —NHC(═S)NH2;
- X1 is a simple bond, —CO—C1-6 alkyl-, —CO—C2-6 alkenyl-, —C(═O)NH—, —C(═O)N(CH3)—, —NHC(═O)—, —N(CH3)C(═O)—, —NHC(═O)NH—, —N(CH 3)C(═O)NH—, —NHC(═S)NH—, or —N(CH3)C(═S)NH—, pyrrolyl, furanyl, thiophenyl, pyrazolyl, imidazolyl, isoxazolyl, oxazolyl, isothiazolyl, thiazolyl, 1,2,3-triazolyl, 1,3,4-triazolyl, 1-oxa-2,3-diazolyl, 1-oxa-2,4-diazolyl, 1-oxa-2,5-diazolyl, 1-oxa-3,4-diazolyl, 1-thia-2,3-diazolyl, 1-thia-2,4-diazolyl, 1-thia-2,5-diazolyl, 1-thia-3,4-diazolyl, tetrazolyl, pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl, indolyl, isoindolyl, benzofuranyl, benzothiophenyl, indazolyl, benzimidazolyl, benzotriazolyl, pyrrolo[2,3-b]pyridinyl, pyrrolo[2,3-c]pyridinyl, pyrrolo[3,2-c]pyridinyl, pyrrolo[3,2-b]pyridinyl, imidazo[4,5-b]pyridinyl, imidazo[4,5-c]pyridinyl, pyrazolo[4,3-d]pyridinyl, pyrazolo[4,3-c]pyridinyl, pyrazolo[3,4-c]pyridinyl, pyrazolo[3,4-b]pyridinyl, purinyl, indolizinyl, imidazo[1,2-a]pyridinyl, imidazo[1,5-a]pyridinyl, pyrazolo[1,5-a]pyridinyl, pyrrolo[1,2-b]pyridazinyl, imidazo[1,2-c]pyrimidinyl, quinolinyl, isoquinolinyl, cinnolinyl, azaquinazolinyl, quinoxalinyl, phthalazinyl, 1,6-naphthyridinyl, 1,7-naphthyridinyl, 1,8-naphthyridinyl, 1,5-naphthyridinyl, 2,6-naphthyridinyl, 2,7-naphthyridinyl, pyrido[3,2-d]pyrimidinyl, pyrido[4,3-d]pyrimidinyl, pyrido[3,4-d]pyrimidinyl, pyrido[2,3-b]pyrimidinyl, pyrido[2,3-b]pyrazinyl, pyrido[3,4-b]pyrazinyl, pyrimido[5,4-d]pyrimidinyl, pyrazino[2,3-b]pyrazinyl, pyrimido[4,5-d]pyrimidinyl, nucleobase, amino acid monomer or amino acid oligomer.
4:
- The lipid compound, an isomer thereof, or a salt thereof of claim 1, wherein
- the lipid compound is selected from the group consisting of below:
- (1) Heptadecan-9-yl 8-((6-acetamido-2-hydroxyhexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (2) Heptadecan-9-yl 8-((2-hydroxy-6-ureidohexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (3) Heptadecan-9-yl 8-((2-hydroxy-6-(3-methylureido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (4) Heptadecan-9-yl 17-hydroxy-3,11-dioxo-19-(6-oxo-6-(undecyloxy)hexyl)-7-oxa-2,4,10,12,19-pentaazaheptacosan-27-oate;
- (5) Heptadecan-9-yl 25-hydroxy-3,11,19-trioxo-27-(6-oxo-6-(undecyloxy)hexyl)-7,15-dioxa-2,4,10,12,18,20,27-heptaazapentatriacontan-35-oate;
- (6) Heptadecan-9-yl 8-((2-hydroxy-6-(3-methylthioureido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (7) Heptadecan-9-yl 8-((6-(cyclopentanecarboxamido)-2-hydroxyhexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (8) Heptadecan-9-yl 8-((2-hydroxy-6-((R)-pyrrolidine-3-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (9) Heptadecan-9-yl 8-((2-hydroxy-6-((S)-pyrrolidine-3-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (10) Heptadecan-9-yl 8-((2-hydroxy-6-((R)-1-methylpyrrolidine-3-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (11) Heptadecan-9-yl 8-((2-hydroxy-6-((S)-1-methylpyrrolidine-3-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (12) Heptadecan-9-yl 8-((6-(cyclohexanecarboxamido)-2-hydroxyhexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (13) Heptadecan-9-yl 8-((2-hydroxy-6-(piperazine-2-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (14) Heptadecan-9-yl 8-((6-(1,4-dimethylpiperazine-2-carboxamido)-2-hydroxyhexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (15) Heptadecan-9-yl 8-((6-(2-(1,4-dimethylpiperazine-2-yl)acetamido)-2-hydroxyhexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (16) Heptadecan-9-yl 8-((2-hydroxy-6-(1H-pyrrole-2-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (17) Heptadecan-9-yl 8-((2-hydroxy-6-(1H-pyrrole-3-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (18) Heptadecan-9-yl 8-((2-hydroxy-6-(1-methyl-1H-pyrrole-2-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (19) Heptadecan-9-yl 8-((2-hydroxy-6-(1-methyl-1H-pyrrole-3-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (20) Heptadecan-9-yl 8-((2-hydroxy-6-(4-nitro-1H-pyrrole-2-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (21) Heptadecan-9-yl 8-((2-hydroxy-6-(3-hydroxy-1H-pyrrole-2-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (22) Heptadecan-9-yl 8-((2-hydroxy-6-(4-hydroxy-1H-pyrrole-2-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (23) Heptadecan-9-yl 8-((2-hydroxy-6-(5-hydroxy-1H-pyrrole-2-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (24) Heptadecan-9-yl 8-((2-hydroxy-6-(3-hydroxy-1-methyl-1H-pyrrole-2-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (25) Heptadecan-9-yl 8-((2-hydroxy-6-(4-hydroxy-1-methyl-1H-pyrrole-2-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (26) Heptadecan-9-yl 8-((2-hydroxy-6-(5-hydroxy-1-methyl-1H-pyrrole-2-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (27) Heptadecan-9-yl 8-((2-hydroxy-6-(4-hydroxy-1H-pyrrole-3-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (28) Heptadecan-9-yl 8-((2-hydroxy-6-(5-hydroxy-1H-pyrrole-3-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (29) Heptadecan-9-yl 8-((2-hydroxy-6-(2-hydroxy-1H-pyrrole-3-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (30) Heptadecan-9-yl 8-((2-hydroxy-6-(4-hydroxy-1-methyl-1H-pyrrole-3-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (31) Heptadecan-9-yl 8-((2-hydroxy-6-(5-hydroxy-1-methyl-1H-pyrrole-3-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (32) Heptadecan-9-yl 8-((2-hydroxy-6-(2-hydroxy-1-methyl-1H-pyrrole-3-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (33) Heptadecan-9-yl 8-((2-hydroxy-6-(1H-imidazole-2-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (34) Heptadecan-9-yl 8-((2-hydroxy-6-(1H-imidazole-4-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (35) Heptadecan-9-yl 8-((2-hydroxy-6-(2-hydroxy-1H-imidazole-4-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (36) Heptadecan-9-yl 8-((2-hydroxy-6-(1-methyl-1H-imidazole-2-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (37) Heptadecan-9-yl 8-((2-hydroxy-6-(1-methyl-1H-imidazole-4-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (38) Heptadecan-9-yl 8-((2-hydroxy-6-(1-methyl-1H-imidazole-5-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (39) Heptadecan-9-yl 8-((2-hydroxy-6-(2-hydroxy-1-methyl-1H-imidazole-4-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (40) Heptadecan-9-yl 8-((2-hydroxy-6-(2-hydroxy-1-methyl-1H-imidazole-5-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (41) Heptadecan-9-yl 8-((2-hydroxy-6-(1H-pyrazole-4-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (42) Heptadecan-9-yl 8-((2-hydroxy-6-(1H-pyrazole-5-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (43) Heptadecan-9-yl 8-((2-hydroxy-6-(1-methyl-1H-pyrazole-4-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (44) Heptadecan-9-yl 8-((2-hydroxy-6-(1-methyl-1H-pyrazole-5-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (45) Heptadecan-9-yl 8-((2-hydroxy-6-(1-methyl-1H-pyrazole-3-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (46) Heptadecan-9-yl 8-((2-hydroxy-6-(isoxazole-5-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl) amino)octanoate;
- (47) Heptadecan-9-yl 8-((2-hydroxy-6-(isoxazole-4-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (48) Heptadecan-9-yl 8-((2-hydroxy-6-(oxazole-5-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (49) Heptadecan-9-yl 8-((2-hydroxy-6-(oxazole-4-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (50) Heptadecan-9-yl 8-((6-(furan-3-carboxamido)-2-hydroxyhexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (51) Heptadecan-9-yl 8-((2-hydroxy-6-(thiophene-3-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (52) Heptadecan-9-yl 8-((2-hydroxy-6-(picolinamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (53) Heptadecan-9-yl 8-((2-hydroxy-6-(nicotinamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (54) Heptadecan-9-yl 8-((2-hydroxy-6-(isonicotinamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (55) Heptadecan-9-yl 8-((2-hydroxy-6-(pyridazine-3-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (56) Heptadecan-9-yl 8-((2-hydroxy-6-(pyridazine-4-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (57) Heptadecan-9-yl 8-((2-hydroxy-6-(pyrazine-2-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (58) Heptadecan-9-yl 8-((2-hydroxy-6-(pyrimidine-4-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (59) Heptadecan-9-yl 8-((2-hydroxy-6-(pyrimidine-5-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (60) Heptadecan-9-yl 8-((2-hydroxy-6-(pyrimidine-2-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (61) Heptadecan-9-yl 8-((2-hydroxy-6-(1H-indole-2-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (62) Heptadecan-9-yl 8-((2-hydroxy-6-(1-methyl-1H-indole-2-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (63) Heptadecan-9-yl 8-((2-hydroxy-6-(1H-indole-3-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (64) Heptadecan-9-yl 8-((2-hydroxy-6-(1-methyl-1H-indole-3-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (65) Heptadecan-9-yl 8-((6-(4-amino-2-oxo-1,2-dihydropyrimidine-1-carboxamido)-2-hydroxyhexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (66) Heptadecan-9-yl 8-((6-(2,4-dioxo-1,2,3,4-tetrahydropyrimidine-1-carboxamido)-2-hydroxyhexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (67) Heptadecan-9-yl 8-((6-(6-amino-9H-purine-9-carboxamido)-2-hydroxyhexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (68) Heptadecan-9-yl 8-((6-(2-amino-6-oxo-6,9-dihydro-1H-purine-9-carboxamido)-2-hydroxyhexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (69) Heptadecan-9-yl 8-((6-(2-(4-amino-2-oxopyrimidin-1(2H)-yl)acetamido)-2-hydroxyhexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (70) Heptadecan-9-yl 8-((6-(2-(2,4-dioxo-3,4-dihydropyrimidine-1(2H)-yl)acetamido)-2-hydroxyhexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (71) Heptadecan-9-yl 8-((6-(2-(6-amino-9H-purin-9-yl)acetamido)-2-hydroxyhexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (72) Heptadecan-9-yl 8-((6-(2-(2-amino-6-oxo-1,6-dihydro-9H-purin-9-yl)acetamido)-2-hydroxyhexyl)(6-oxo-6-(undecyloxy)hexyl) amino)octanoate;
- (73) Heptadecan-9-yl 8-((6-((S)-2-amino-5-guanidinopentanamido)-2-hydroxyhexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (74) Heptadecan-9-yl 8-((6-((S)-2-acetamido-5-guanidinopentanamido)-2-hydroxyhexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (75) Heptadecan-9-yl 8-((6-((S)-2-amino-3-(1H-imidazol-5-yl)propanamido)-2-hydroxyhexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (76) Heptadecan-9-yl 8-((6-((S)-2-acetamido-3-(1H-imidazol-5-yl)propanamido)-2-hydroxyhexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (77) Heptadecan-9-yl 8-((6-((S)-2-amino-3-(1H-indole-3-yl)propanamido)-2-hydroxyhexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (78) Heptadecan-9-yl 8-((6-((S)-2-acetamido-3-(1H-indole-3-yl)propanamido)-2-hydroxyhexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (79) Heptadecan-9-yl 8-((2-hydroxy-6-((S)-pyrrolidine-2-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (80) Heptadecan-9-yl 8-((2-hydroxy-6-((S)-1-methylpyrrolidine-2-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (81) Heptadecan-9-yl (6S,9S)-1,6-diamino-9-(3-guanidinopropyl)-16-hydroxy-1-imino-7,10-dioxo-18-(6-oxo-6-(undecyloxy)hexyl)-2,8,11,18-tetraazahexacosan-26-oate;
- (82) Heptadecan-9-yl 8-((6-((S)-2-((S)-2-amino-3-(1H-imidazol-5-yl)propanamido)-5-guanidinopentanamido)-2-hydroxyhexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (83) Heptadecan-9-yl 8-((6-((S)-2-((S)-2-amino-3-(1H-imidazol-5-yl)propanamido)-3-(1H-imidazol-5-yl)propanamido)-2-hydroxyhexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (84) Heptadecan-9-yl (6R,9S)-9-((1H-imidazol-5-yl)methyl)-1,6-diamino-16-hydroxy-1-imino-7,10-dioxo-18-(6-oxo-6-(undecyloxy)hexyl)-2,8,11,18-tetraazahexacosan-26-oate;
- (85) Heptadecan-9-yl (6R,9S,12S)-1,6-diamino-9,12-bis(3-guanidinopropyl)-19-hydroxy-1-imino-7,10,13-trioxo-21-(6-oxo-6-(undecyloxy)hexyl)-2,8,11,14,21-pentaazanonacosan-29-oate;
- (86) Heptadecan-9-yl (6S,9S)-1-amino-6-((R)-2-amino-3-(1H-imidazol-5-yl)propanamido)-9-(3-guanidinopropyl)-16-hydroxy-1-imino-7,10-dioxo-18-(6-oxo-6-(undecyloxy)hexyl)-2,8,11,18-tetraazahexacosan-26-oate;
- (87) Heptadecan-9-yl (2R,5S,8S)-5-((1H-imidazol-5-yl)methyl)-2-amino-8-(3-guanidinopropyl)-15-hydroxy-1-(1H-imidazol-5-yl)-3,6,9-trioxo-17-(6-oxo-6-(undecyloxy)hexyl)-4,7,10,17-tetraazapentacosan-25-oate;
- (88) Heptadecan-9-yl (6R,9S,12S)-9-((1H-imidazol-5-yl)methyl)-1,6-diamino-12-(3-guanidinopropyl)-19-hydroxy-1-imino-7,10,13-trioxo-21-(6-oxo-6-(undecyloxy)hexyl)-2,8,11,14,21-pentaazanonacosan-29-oate;
- (89) Heptadecan-9-yl (2R,5S,8S)-5,8-bis((1H-imidazol-5-yl)methyl)-2-amino-15-hydroxy-1-(1H-imidazol-5-yl)-3,6,9-trioxo-17-(6-oxo-6-(undecyloxy)hexyl)-4,7,10,17-tetraazapentacosan-25-oate;
- (90) Heptadecan-9-yl (6R,9S,12S)-9,12-bis((1H-imidazol-5-yl)methyl)-1,6-diamino-19-hydroxy-1-imino-7,10,13-trioxo-21-(6-oxo-6-(undecyloxy)hexyl)-2,8,11,14,21-pentaazanonacosan-29-oate;
- (91) Heptadecan-9-yl (6R,9S,12S)-12-((1H-imidazol-5-yl)methyl)-1,6-diamino-9-(3-guanidinopropyl)-19-hydroxy-1-imino-7,10,13-trioxo-21-(6-oxo-6-(undecyloxy)hexyl)-2,8,11,14,21-pentaazanonacosan-29-oate;
- (92) Heptadecan-9-yl (6S,9S)-9-((1H-imidazol-5-yl)methyl)-1-amino-6-((R)-2-amino-3-(1H-imidazol-5-yl)propanamido)-16-hydroxy-1-imino-7,10-dioxo-18-(6-oxo-6-(undecyloxy)hexyl)-2,8,11,18-tetraazahexacosan-26-oate;
- (93) Heptadecan-9-yl 1-(4-amino-2-oxopyrimidin-1(2H)-yl)-9-(2-(6-amino-9H-purin-9-yl)acetyl)-3-(2-aminoethyl)-17-hydroxy-2,5,11-trioxo-19-(6-oxo-6-(undecyloxy)hexyl)-3,6,9,12,19-pentaazaheptacosan-27-oate;
- (94) Heptadecan-9-yl 9-(2-(4-amino-2-oxopyrimidin-1(2H)-yl)acetyl)-1-(2-amino-6-oxo-1,6-dihydro-9H-purin-9-yl)-15-(2-(6-amino-9H-purin-9-yl)acetyl)-3-(2-aminoethyl)-23-hydroxy-2,5,11,17-tetraoxo-25-(6-oxo-6-(undecyloxy)hexyl)-3,6,9,12,15,18,25-heptaazatritriacontan-23-oate;
- (95) Heptadecan-9-yl 15-(2-(4-amino-2-oxopyrimidin-1(2H)-yl)acetyl)-9-(2-(2-amino-6-oxo-1,6-dihydro-9H-purin-9-yl)acetyl)-21-(2-(6-amino-9H-purin-9-yl)acetyl)-3-(2-aminoethyl)-1-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-29-hydroxy-2,5,11,17,23-pentaoxo-31-(6-oxo-6-(undecyloxy)hexyl)-3,6,9,12,15,18,21,24,31-nonaazanonatriacontan-39-oate;
- (96) Heptadecan-9-yl 21-(2-(4-amino-2-oxopyrimidin-1(2H)-yl)acetyl)-15-(2-(2-amino-6-oxo-1,6-dihydro-9H-purin-9-yl)acetyl)-1-(2-(6-amino-9H-purin-9-yl)-27-(2-(6-amino-9H-purin-9-yl)acetyl)-3-(2-aminoethyl)-9-(2-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)acetyl)-35-hydroxy-2,5,11,17,23,29-hexaoxo-37-(6-oxo-6-(undecyloxy)hexyl)-3,6,9,12,15,18,21,24,27,30,37-undecaazapentatetracontan-45-oate;
- (97) Heptadecan-9-yl 8-((6-(4-(4-amino-1-methyl-1H-pyrrole-2-carboxamido)-1-methyl-1H-pyrrole-2-carboxamido)-2-hydroxyhexyl)(6-oxo-6-(undecyloxy) hexyl)amino)octanoate;
- (98) Heptadecan-9-yl 8-((6-(4-(4-(4-amino-1-methyl-1H-imidazole-2-carboxamido)-1-methyl-1H-pyrrole-2-carboxamido)-1-methyl-1H-pyrrole-2-carboxamido)-2-hydroxyhexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (99) Heptadecan-9-yl 8-((2-hydroxy-6-(1-methyl-4-(1-methyl-4-(1-methyl-4-(1-methyl-1H-imidazole-2-carboxamido)-1H-imidazole-2-carboxamido)-1H-pyrrole-2-carboxamido)-1H-pyrrole-2-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (100) Heptadecan-9-yl 8-((2-hydroxy-4-(3-methylureido)butyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (101) Heptadecan-9-yl 8-((2-hydroxy-5-(3-methylureido)pentyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (102) Heptadecan-9-yl 8-((2-hydroxy-7-(3-methylureido)heptyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (103) Heptadecan-9-yl 8-((2-hydroxy-8-(3-methylureido)octyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (104) Heptadecan-9-yl 9-hydroxy-3-oxo-11-(6-oxo-6-(undecyloxy)hexyl)-7-oxa-2,4,11-triazanonadecan-19-oate;
- (105) Heptadecan-9-yl 12-hydroxy-3-oxo-14-(6-oxo-6-(undecyloxy)hexyl)-7,10-dioxa-2,4,14-triazadocosan-22-oate;
- (106) Heptadecan-9-yl 15-hydroxy-3-oxo-17-(6-oxo-6-(undecyloxy)hexyl)-7,10,13-trioxa-2,4,17-triazapentacosan-25-oate;
- (107) Heptadecan-9-yl 8-((2-(hydroxymethyl)-6-(3-methylureido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (108) Heptadecan-9-yl 8-((2-(2-hydroxyethyl)-6-(3-methylureido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (109) Heptadecan-9-yl 8-((2-(3-hydroxypropyl)-6-(3-methylureido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (110) (6Z,9Z,28Z,31Z)-heptatriaconta-6,9,28,31-tetraen-19-yl 4-((2-hydroxy-6-(3-methylureido)hexyl)(methyl)amino)butanoate;
- (111) Heptadecan-9-yl 8-((2-hydroxy-6-(piperazine-1-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (112) Heptadecan-9-yl 8-((2-hydroxy-6-(4-methylpiperazine-1-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (113) Heptadecan-9-yl 8-((2-hydroxy-6-(2-(piperazin-1-yl)acetamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (114) Heptadecan-9-yl 8-((2-hydroxy-6-(2-(4-methylpiperazin-1-yl)acetamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (115) Heptadecan-9-yl 8-((6-(furan-2-carboxamido)-2-hydroxyhexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (116) Heptadecan-9-yl8-((2-hydroxy-6-(thiophene-2-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (117) Heptadecan-9-yl 8-((6-(3-methylureido)hexyl)(6-oxo-6-(undecyloxy) hexyl)amino)octanoate;
- (118) Heptadecan-9-yl 8-((6-(dodecan-2-yloxy)-6-oxohexyl)(2-hydroxy-6-(3-methylureido)hexyl)amino)octanoate;
- (119) Heptadecan-9-yl 8-((2-hydroxy-6-(3-methylureido)hexyl)(6-oxo-6-(tridecan-3-yloxy)hexyl) amino)octanoate;
- (120) 5-((8-(Heptadecan-9-yloxy)-8-oxooctyl)(2-hydroxy-6-(3-methylureido)hexyl)amino)pentyl dodecanoate;
- (121) (9Z,28Z)-heptatriaconta-9,28-dien-19-yl 4-((2-hydroxy-6-(3-methylureido)hexyl)(methyl)amino)butanoate;
- (122) Heptadecan-9-yl 8-((2-hydroxy-6-(1,3,5-triazine-2-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (123) Heptadecan-9-yl 8-((2-hydroxy-4-(1H-pyrrole-3-carboxamido)butyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (124) Heptadecan-9-yl 8-((2-hydroxy-5-(1H-pyrrole-3-carboxamido)pentyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (125) Heptadecan-9-yl 8-((2-hydroxy-7-(1H-pyrrole-3-carboxamido)heptyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (126) Heptadecan-9-yl 8-((2-hydroxy-8-(1H-pyrrole-3-carboxamido)octyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (127) Heptadecan-9-yl 8-((3-(2-(1H-pyrrole-3-carboxamido)ethoxy)-2-hydroxypropyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (128) Heptadecan-9-yl 10-hydroxy-1-oxo-12-(6-oxo-6-(undecyloxy)hexyl)-1-(1H-pyrrol-3-yl)-5,8-dioxa-2,12-diazacosan-20-oate;
- (129) Heptadecan-9-yl 13-hydroxy-1-oxo-15-(6-oxo-6-(undecyloxy)hexyl)-1-(1H-pyrrol-3-yl)-5,8,11-trioxa-2,15-diazatricosan-23-oate;
- (130) Heptadecan-9-yl 8-((2-(hydroxymethyl)-6-(1H-pyrrole-3-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (131) Heptadecan-9-yl 8-((2-(2-hydroxyethyl)-6-(1H-pyrrole-3-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (132) Heptadecan-9-yl 8-((2-(3-hydroxypropyl)-6-(1H-pyrrole-3-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (133) Heptadecan-9-yl 8-((6-(1H-pyrrole-3-carboxamido)hexyl)(6-oxo-6-(undecyloxy)hexyl)amino)octanoate;
- (134) Heptadecan-9-yl 8-((6-(dodecan-2-yloxy)-6-oxohexyl)(2-hydroxy-6-(1H-pyrrole-3-carboxamido)hexyl)amino)octanoate;
- (135) Heptadecan-9-yl 8-((2-hydroxy-6-(1H-pyrrole-3-carboxamido)hexyl)(6-oxo-6-(tridecan-3-yloxy)hexyl)amino)octanoate;
- (136) 5-((8-(Heptadecan-9-yloxy)-8-oxooctyl)(2-hydroxy-6-(1H-pyrrole-3-carboxamido)hexyl)amino)pentyl dodecanoate;
- (137) (9Z,28Z)-heptatriaconta-9,28-dien-19-yl 4-((2-hydroxy-6-(1H-pyrrole-3-carboxamido)hexyl)(methyl) amino)butanoate;
- (138) (6Z,9Z,28Z,31Z)-heptatriaconta-6,9,28,31-tetraen-19-yl 4-((2-hydroxy-6-(1H-pyrrole-3-carboxamido)hexyl)(methyl)amino)butanoate;
- (139) Heptadecan-9-yl 8-((6-(heptan-2-yloxy)-6-oxohexyl)(2-hydroxy-6-(1H-pyrrole-3-carboxamido)hexyl)amino)octanoate;
- (140) Heptadecan-9-yl 8-((2-hydroxy-6-(1H-pyrrole-3-carboxamido)hexyl)(6-(octan-2-yloxy)-6-oxohexyl)amino)octanoate;
- (141) Heptadecan-9-yl 8-((2-hydroxy-6-(1H-pyrrole-3-carboxamido)hexyl)(6-(nonan-2-yloxy)-6-oxohexyl)amino)octanoate;
- (142) Heptadecan-9-yl 8-((2-hydroxy-6-(1H-pyrrole-3-carboxamido)hexyl)(6-oxo-6-(tridecan-2-yloxy)hexyl)amino)octanoate;
- (143) Heptadecan-9-yl 8-((2-hydroxy-6-(1H-pyrrole-3-carboxamido)hexyl)(6-oxo-6-(tetradecan-2-yloxy)hexyl)amino)octanoate;
- (144) Heptadecan-9-yl 8-((2-hydroxy-6-(1H-pyrrole-3-carboxamido)hexyl)(6-(octan-3-yloxy)-6-oxohexyl)amino)octanoate;
- (145) Heptadecan-9-yl 8-((2-hydroxy-6-(1H-pyrrole-3-carboxamido)hexyl)(6-oxo-6-(undecan-3-yloxy)hexyl)amino)octanoate;
- (146) Heptadecan-9-yl 8-((2-hydroxy-6-(1H-pyrrole-3-carboxamido)hexyl)(6-(nonan-4-yloxy)-6-oxohexyl)amino)octanoate;
- (147) Heptadecan-9-yl 8-((2-hydroxy-6-(1H-pyrrole-3-carboxamido)hexyl)(6-oxo-6-(undecan-4-yloxy)hexyl)amino)octanoate;
- (148) Heptadecan-9-yl 8-((6-(decan-5-yloxy)-6-oxohexyl)(2-hydroxy-6-(1H-pyrrole-3-carboxamido)hexyl)amino)octanoate;
- (149) Heptadecan-9-yl 8-((2-hydroxy-6-(1H-pyrrole-3-carboxamido)hexyl)(6-oxo-6-(undecan-5-yloxy)hexyl)amino)octanoate;
- (150) Heptadecan-9-yl 8-((2-hydroxy-6-(1H-pyrrole-3-carboxamido)hexyl)(6-oxo-6-(undecan-6-yloxy)hexyl)amino)octanoate;
- (151) Heptadecan-9-yl 8-((2-hydroxy-6-(1H-pyrrole-3-carboxamido)hexyl)(6-((2-methylpentyl)oxy)-6-oxohexyl)amino)octanoate;
- (152) Heptadecan-9-yl 8-((2-hydroxy-6-(1H-pyrrole-3-carboxamido)hexyl)(6-((2-methyloctyl)oxy)-6-oxohexyl)amino)octanoate;
- (153) Heptadecan-9-yl 8-((2-hydroxy-6-(1H-pyrrole-3-carboxamido)hexyl)(6-((2-methylnonyl)oxy)-6-oxohexyl)amino)octanoate;
- (154) Heptadecan-9-yl 8-((2-hydroxy-6-(1H-pyrrole-3-carboxamido)hexyl)(6-((2-methyldecyl)oxy)-6-oxohexyl)amino)octanoate;
- (155) Heptadecan-9-yl 8-((2-hydroxy-6-(1H-pyrrole-3-carboxamido)hexyl)(6-((2-methylundecyl)oxy)-6-oxohexyl)amino)octanoate;
- (156) Heptadecan-9-yl 8-((2-hydroxy-6-(1H-pyrrole-3-carboxamido)hexyl)(6-((2-methyldodecyl)oxy)-6-oxohexyl)amino)octanoate;
- (157) Heptadecan-9-yl 8-((2-hydroxy-6-(1H-pyrrole-3-carboxamido)hexyl)(6-((2-methyltridecyl)oxy)-6-oxohexyl)amino)octanoate;
- (158) Heptadecan-9-yl 8-((2-hydroxy-6-(1H-pyrrole-3-carboxamido)hexyl)(6-((2-methyltetradecyl)oxy)-6-oxohexyl)amino)octanoate;
- (159) Heptadecan-9-yl 8-((6-((2-ethylhexyl)oxy)-6-oxohexyl)(2-hydroxy-6-(1H-pyrrole-3-carboxamido)hexyl)amino)octanoate;
- (160) Heptadecan-9-yl 8-((6-((2-butyloctyl)oxy)-6-oxohexyl)(2-hydroxy-6-(1H-pyrrole-3-carboxamido)hexyl)amino)octanoate;
- (161) Heptadecan-9-yl 8-((6-((2-hexyloctyl)oxy)-6-oxohexyl)(2-hydroxy-6-(1H-pyrrole-3-carboxamido)hexyl)amino)octanoate;
- (162) Heptadecan-9-yl 8-((2-hydroxy-6-(1H-pyrrole-3-carboxamido)hexyl)(6-((2-octyldodecyl)oxy)-6-oxohexyl)amino)octanoate;
- (163) Heptadecan-9-yl 8-((2-hydroxy-6-(1H-pyrrole-3-carboxamido)hexyl)(6-((6-methylnonyl)oxy)-6-oxohexyl)amino)octanoate;
- (164) Heptadecan-9-yl 8-((2-hydroxy-6-(1H-pyrrole-3-carboxamido)hexyl)(6-((6-methyloctyl)oxy)-6-oxohexyl)amino)octanoate;
- (165) Heptadecan-9-yl 8-((2-hydroxy-6-(1H-pyrrole-3-carboxamido)hexyl)(6-((7-methylnonyl)oxy)-6-oxohexyl)amino)octanoate;
- (166) Heptadecan-9-yl 8-((2-hydroxy-6-(1H-pyrrole-3-carboxamido)hexyl)(6-((8-methyldecyl)oxy)-6-oxohexyl)amino)octanoate;
- (167) Heptadecan-9-yl 8-((2-hydroxy-6-(1H-pyrrole-3-carboxamido)hexyl)(6-((7-methyloctyl)oxy)-6-oxohexyl)amino)octanoate;
- (168) Heptadecan-9-yl 8-((2-hydroxy-6-(1H-pyrrole-3-carboxamido)hexyl)(6-((8-methylnonyl)oxy)-6-oxohexyl)amino)octanoate;
- (169) Heptadecan-9-yl 8-((2-hydroxy-6-(1H-pyrrole-3-carboxamido)hexyl)(6-((9-methyldecyl)oxy)-6-oxohexyl)amino)octanoate;
- (170) Heptadecan-9-yl 8-((2-hydroxy-6-(1H-pyrrole-3-carboxamido)hexyl)(6-((10-methylundecyl)oxy)-6-oxohexyl)amino)octanoate;
- (171) Heptadecan-9-yl 8-((2-hydroxy-6-(1H-pyrrole-3-carboxamido)hexyl)(6-((11-methyldodecyl)oxy)-6-oxohexyl)amino)octanoate;
- (172) Heptadecan-9-yl 8-((2-hydroxy-6-(1H-pyrrole-3-carboxamido)hexyl)(6-((12-methyltridecyl)oxy)-6-oxohexyl)amino)octanoate;
- (173) Heptadecan-9-yl 8-((2-hydroxy-6-(1H-pyrrole-3-carboxamido)hexyl)(6-((5-methylheptan-2-yl)oxy)-6-oxohexyl)amino)octanoate;
- (174) Heptadecan-9-yl 8-((2-hydroxy-6-(1H-pyrrole-3-carboxamido)hexyl)(6-((5-methyloctan-2-yl)oxy)-6-oxohexyl)amino)octanoate;
- (175) Heptadecan-9-yl 8-((2-hydroxy-6-(1H-pyrrole-3-carboxamido)hexyl)(6-((6-methylheptan-2-yl)oxy)-6-oxohexyl)amino)octanoate;
- (176) Heptadecan-9-yl 8-((2-hydroxy-6-(1H-pyrrole-3-carboxamido)hexyl)(6-((2-methyloctan-3-yl)oxy)-6-oxohexyl)amino)octanoate;
- (177) Heptadecan-9-yl 8-((6-((2,6-dimethylheptan-4-yl)oxy)-6-oxohexyl)(2-hydroxy-6-(1H-pyrrole-3-carboxamido)hexyl)amino)octanoate;
- and
- (178) Heptadecan-9-yl 8-((6-((7-ethyl-2-methylundecan-4-yl)oxy)-6-oxohexyl) (2-hydroxy-6-(1H-pyrrole-3-carboxamido)hexyl)amino)octanoate.
178 more elements
5:
- A lipid nanoparticle composition, comprising:
- the lipid compound, an isomer thereof, or a salt thereof of one claim 1;
- active substances;
- phospholipids;
- structural lipids;
- and
- PEGylated lipids (PEG-lipid).
4 more elements
6:
- The lipid nanoparticle composition of claim 5, wherein
- the active substances are one or more types selected from the group consisting of chemical therapeutics, small-molecule drugs, proteins, and nucleic acids.
7:
- The lipid nanoparticle composition of claim 5, wherein
- the active substances are nucleic acids.
8:
- The lipid nanoparticle composition of claim 5, wherein
- the phospholipids are selected from the group consisting of 1,2-distearoyl-sn-glycero-3-phosphocholine (DSPC), 1,2-dioleoyl-sn-glycero-3-phosphoethanolamine (DOPE), 1,2-dilinoleoyl-sn-glycero-3-phosphocholine (DLPC), 1,2-dimyristoyl-sn-glycero-3-phosphocholine (DMPC), 1,2-dioleoyl-sn-glycero-3-phosphocholine (DOPC), 1,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC), 1,2-diundecanoyl-sn-glycero-3-phosphocholine (DUPC), 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine (POPC), 1,2-di-O-octadecenyl-sn-glycero-3-phosphocholine (18:0 diether PC), 1-oleoyl-2-cholesterylhemisuccinoyl-sn-glycero-3-phosphocholine (OChemsPC), 1-hexadecyl-sn-glycero-3-phosphocholine (C16 Lyso PC), 1,2-dilinolenoyl-sn-glycero-3-phosphocholine, 1,2-diarachidonoyl-sn-glycero-3-phosphocholine, 1,2-didocosahexaenoyl-sn-glycero-3-phosphocholine, 1,2-diphytanoyl-sn-glycero-3-phosphoethanolamine (ME 16.0 PE), 1,2-distearoyl-sn-glycero-3-phosphoethanolamine, 1,2-dilinoleoyl-sn-glycero-3-phosphoethanolamine, 1,2-dilinolenoyl-sn-glycero-3-phosphoethanolamine, 1,2-diarachidonoyl-sn-glycero-3-phosphoethanolamine, 1,2-didocosahexaenoyl-sn-glycero-3-phosphoethanolamine, 1,2-dioleoyl-sn-glycero-3-phospho-rac-(1-glycerol) sodium salt (DOPG), dipalmitoylphosphatidylglycerol (DPPG), palmitoyloleoylphosphatidylethanolamine (POPE), distearoyl-phosphatidyl-ethanolamine (DSPE), dipalmitoyl phosphatidyl ethanolamine (DPPE), dimyristoylphosphoethanolamine (DMPE), 1-stearoyl-2-oleoyl-phosphatidylethanolamine (SOPE), 1-stearoyl-2-oleoyl-phosphatidylcholine (SOPC), sphingomyelin, phosphatidylcholine, phosphatidylethanolamine, phosphatidylserine, phosphatidylinositol, phosphatidic acid, palmitoyloleoyl phosphatidylcholine, lysophosphatidylcholine, lysophosphatidylethanolamine (LPE), and a mixture thereof.
9:
- The lipid nanoparticle composition of one claim 5, wherein
- the structural lipids are selected from the group consisting of cholesterol, pecosterol, cytosterol, ergosterol, stigmasterol, bracicasterol, tomatidine, ursolic acid, alpha-tocopherol, and a mixture thereof.
10:
- The lipid nanoparticle composition of claim 5, wherein
- the PEGylated lipids are selected from the group consisting of PEGylated phosphatidylethanolamine, PEGylated phosphatidic acid, PEGylated ceramide (PEG-CER), PEGylated dialkylamine, PEGylated diacylglycerol (PEG-DEG), PEGylated dialkyl glycerol, and a mixture thereof, and for example, PEG-lipids are selected from the group consisting of PEG-c-DOMG, PEG-DMG, PEG-DLPE, PEG-DMPE, PEG-DPPC, PEG-DSPE, and a mixture thereof.
11:
- A method for preparing an active substance-lipid nanoparticle, the method comprising:
- mixing an organic phase with an aqueous phase, the organic phase in which the lipid compound, an isomer thereof, or a salt thereof according to claim 1, phospholipids, structural lipids, and PEGylated lipids are mixed at a molar ratio of (20-60):(0-25):(30-60):(0-5);
- and the aqueous phase in which the active substance is dissolved, wherein the ratio (N/P ratio) of the number of ionizable nitrogen atoms of the lipid compound, an isomer thereof, or a salt thereof to the number of phosphorus atoms from the anionic phosphodiester group in the active substance is in the range of 1.5-15, and the mass ratio of the lipid compound, an isomer thereof, or a salt thereof to the active substance is (4-30):1.
12:
- A pharmaceutical composition comprising:
- the lipid nanoparticle composition of claim 5;
- and a pharmaceutically acceptable carrier.
13:
- A method for preventing or treating a disease, comprising a step of administering the lipid nanoparticle composition of claim 5 to a subject in need of the prevention or treatment of the disease.