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US 12,723,016 B2Granted
Spleen-targeted ionizable lipid compound, composition comprising same and use thereof
AssigneeBeijing Carrius Bio Ltd.
InventorMing Wang
Life of this patent
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Abstract
The present invention provides an ionizable lipid compound, which can target spleen for delivery of biological macromolecules including nucleic acid drugs or nucleic acid vaccines with high efficiency. The present invention also relates to a lipid nanoparticle (LNP) comprising the ionizable lipid compound and an active molecule, and a pharmaceutical composition comprising the lipid nanoparticle.
Claims15
A lipid compound of formula (I),
- wherein
- R2a and R3a are each independently selected from the group consisting of hydrogen, a monovalent aliphatic group, a monovalent heteroaliphatic group, a monovalent aromatic group, a monovalent heteroaromatic group, and Ht;
- t and s are each independently 0 or 1, and when t or s is zero, it means that the part is directly a single bond, provided that t and s are not both 0;
- A1, A2, and A3 are each independently selected from the group consisting of a single bond, a divalent aliphatic group, a divalent heteroaliphatic group, a divalent aromatic group, and a divalent heteroaromatic group;
- each Ht is independently at each occurrence —R1—X—R2—Y—R3—Z—R4,
- wherein
- each R1 is independently at each occurrence selected from the group consisting of a divalent aliphatic group, a divalent heteroaliphatic group, a divalent aromatic group, and a divalent heteroaromatic group;
- each X is independently at each occurrence
- wherein
- m is 1-6;
- W is selected from the group consisting of O, S, and NRc;
- L1 is directly connected to R1 or R2 and is independently selected from the group consisting of a single bond, O, S, and NRd;
- L2 independently is selected from the group consisting of a bond, O, S, and NRe;
- wherein Rc, Rd, and Re, are each independently selected from the group consisting of hydrogen, hydroxy, an oxyaliphatic group, a monovalent aliphatic group, a monovalent heteroaliphatic group, a monovalent aromatic group, and a monovalent heteroaromatic group;
- Y and Z are each independently at each occurrence selected from the group consisting of S and O;
- each R2 is independently at each occurrence selected from the group consisting of a single bond, a divalent aliphatic group, a divalent heteroaliphatic group, a divalent aromatic group, and a divalent heteroaromatic group;
- R3 is independently at each occurrence
- each R4 is independently at each occurrence a hydrophobic group selected from the group consisting of —(CH2CH2O)y—C1-2 alkyl, —(CH2CH2O)y—C2 alkenyl and —(CH2CH2O)y—C2 alkynyl, wherein y is 0 or 1 or 2.
15 more elements
A lipid compound selected from the group consisting of
Dependencies are inferred from the claim text.