IP Library › Granted Patent US 12697376
Granted Patent B2
US 12697376 · App. 18/681,557 · Granted Aug 4, 2026

Cationic lipid compounds

Inventors: Cai Gu Huang (Guangdong, CN); Tie Qiang Huang (Guangdong, CN); Jun Rong Tan (Guangdong, CN)
Assignee: Guangzhou Anobri Pharmaceutical Co. Ltd
A61K39/00A61K9/1272A61K31/7105C07C219/06
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Quick Facts
Patent No.
US 12697376
App. No.
18/681,557
Granted
Aug 4, 2026
Kind
B2
Abstract

The invention relates to lipid compounds that can be used alone or in combination with other lipid components, such as neutral lipids, charged lipids, steroids, and polymer conjugated lipids to form lipid nanoparticles for delivery of therapeutic and/or prophylactic agents; pharmaceutical compositions containing the lipid nanoparticles; and methods of using the lipid nanoparticles to treat or prevent diseases.

Claims (25)

1 . A compound of structure (I):

or a salt, isomer or an N-oxide thereof,

wherein R 1 , R 2 are independently C 1-3 alkyl or hydrogen, and

wherein R1 and R2 cannot simultaneously be hydrogen.

2 . The compound of claim 1 , wherein the C 1-3 alkyl group is a linear alkane.

3 . The compound of claim 2 , wherein the C 1-3 alkyl group is methyl, ethyl, n-propyl.

4 . A composition comprising the compound of claim 1 and a therapeutic and/or prophylactic agent.

5 . The composition of claim 4 , further comprising one or more excipients selected from the group consisting of neutral lipids, steroids, and polymer conjugated lipids.

6 . The composition of claim 4 , further comprising one or more excipients selected from the group consisting of:

(a) a neutral lipid is selected from the group consisting of 1,2-distearoyl-sn-glycero-3-phosphocholine (DSPC), 1,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC), 1,2-dimethoyl-sn-glycero-phosphocholine (DMPC), 1,2-dioleoyl-sn-glycero-3-phosphocholine (DOPC), 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine (POPC), 1,2-dioleoyl-sn-glycero-3-phosphoethanolamine (DOPE), sphingomyelin (SM), and combinations thereof;

(b) a steroid selected from the group consisting of cholesterol, fecal steroid, sitosterol, ergosterol, rapeseed sterol, soybean sterol, tomatidine, ursolic acid, alpha-tocopherol, and combinations thereof; and

(c) a polymer-conjugated lipid.

7 . The composition of claim 6 , wherein the neutral lipid is DSPC, the steroid is cholesterol, and the polymer-conjugated lipid is a pegylated lipid.

8 . The composition of claim 7 , wherein the pegylated lipid is 1,2-dimyristoyl-sn-glycerol methoxypolyethylene glycol (PEG-DMG).

9 . The composition of claim 6 , wherein the polymer-conjugated lipid is a pegylated lipid.

10 . The composition of claim 9 , wherein the pegylated lipid is 1,2-dimyristoyl-sn-glycerol methoxypolyethylene glycol (PEG-DMG).

11 . The composition of claim 6 , wherein the therapeutic agent is selected from the group consisting of siRNA, aiRNA, miRNA, dsRNA, shRNA, mRNA, and mixtures thereof.

12 . The composition of claim 11 , wherein the RNA is an mRNA.

13 . The composition of claim 4 , wherein the therapeutic agent is selected from the group consisting of siRNA, aiRNA, miRNA, dsRNA, shRNA, mRNA, and mixtures thereof.

14 . The composition of claim 13 , wherein the RNA is an mRNA.

15 . A method of treating a disorder in a mammal comprising administering to the mammal the composition of claim 6 .

16 . A method of treating a disorder in a mammal comprising administering to the mammal the composition of claim 4 .

17 . The method of claim 16 , wherein the mammal is a human.

18 . The compound of claim 1 selected from the group consisting of:

19 . The composition of claim 6 in the form of a lipid nanoparticle.