IP Library › Granted Patent US 12,678,515
Granted Patent B2
US 12,678,515 · App. 16/067,538 · Granted Jul 14, 2026

Lipids and lipid nanoparticle formulations for delivery of nucleic acids

Inventors: Steven M. Ansell (Vancouver, CA); Xinyao Du (Richmond, CA)
Assignee: Acuitas Therapeutics, Inc.
A61K47/6929A61K31/7105A61K47/543C07C229/12
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Quick Facts
Patent No.
US 12,678,515
App. No.
16/067,538
Filed
Jun 29, 2018
Granted
Jul 14, 2026
Kind
B2
Examiner
POPA, ILEANA
Art Unit
1633
USPC
514/44R
Abstract

Compounds are provided having the following structure (I) or (II): or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R, R 1 , R 2 , L, X, L, G 1 , G 2 , Z, a 1 , a 2 and n are independently as defined herein for each of structures (I) and (II). Use of the compounds as a component of lipid nanoparticle formulations for delivery of a therapeutic agent, compositions comprising the compounds and methods for their use and preparation are also provided.

Claims (19)

1 . A compound having the following structure (I):

or a pharmaceutically acceptable salt or stereoisomer thereof, wherein:

L is, at each occurrence, ~O(C═O)—, wherein ~ represents a covalent bond to X;

X is CH;

Z is C 1 -C 6 alkyl wherein the C 1 -C 6 alkyl is substituted with C 1 -C 6 alkylaminyl;

R is, at each occurrence, H;

R 1 and R 2 independently have one of the following structures:

 and

a 1 and a 2 are, at each occurrence, independently an integer from 4 to 9.

2 . The compound of claim 1 , wherein the compound has the structures:

3 . The compound of claim 1 , wherein Z, has the structures:

4 . The compound of claim 1 , wherein Z-L has the structures:

5 . The compound of claim 1 , having the structures:

6 . A composition comprising the compound of claim 1 and a therapeutic agent.

7 . A method for administering a therapeutic agent to a patient in need thereof, the method comprising administering the composition of claim 6 to the patient.

8 . The composition of claim 6 , wherein the therapeutic agent is messenger RNA (mRNA).

9 . A lipid nanoparticle comprising the compound of claim 1 and a therapeutic agent.

10 . The lipid nanoparticle of claim 9 , wherein the therapeutic agent is messenger RNA (mRNA).

11 . The compound of claim 1 , wherein Z, has the structures:

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 13, 2018
From: ANSELL, STEVEN M.; DU, XINYAO
To: ACUITAS THERAPEUTICS, INC.
Reel/Frame 047772/0321 →
Continuity (3)
Provisional Application 62302348 · Mar 2, 2016
Provisional Application 62273018 · Dec 30, 2015
Related Publication 20190022247A1 · Jan 24, 2019
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