CLEAVABLE LIPIDIC COMPOUNDS, COMPOSITIONS CONTAINING THEREOF, AND USES THEREOF

• Main Authors: HAENSLER, Jean, EVEN, Luc, RIPOLL, Manon
• Format: Patent
• Language: English; French; German
• Published: 24.05.2023
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; CHEMISTRY; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

The disclosure relates to novel lipidic compounds, method of manufacturing lipid nanoparticles (LNPs) containing thereof, lipid nanoparticles (LNPs) containing thereof, and the use of the LNPs for the delivery of nucleic acid. The lipidic compounds as disclosed herein is a cleavable lipidic compound comprising at least one terminal radical of formula (I): Y-(CHR)n-Z-(CHR′)p-Q*(I) wherein: -* is the end linked, directly or not, to one C10 to C55 lipophilic or hydrophobic tail-group; -Y is a radical selected in the group consisting of methyl, methoxy, trifluoromethyl, imidazolyl, or is one hydrogen; -Z is a radical -NH-CH2-CO-O-**or a radical -CR″(NH2)-CO-O-** with ** that is the end closest to Q and R″ that is selected in the group consisting of hydrogen, methyl radical and trifluoromethyl radical; -Q is a radical -NH-CH2-CO-O-*** or a radical -CR″(NH2)-CO-O-*** with R″ selected in the group consisting of hydrogen, methyl radical and trifluoromethyl radical and *** that is the end linked, directly or not, to said lipophilic or hydrophobic tail-group; -R et R′ are, independently one from the other, one hydrogen, one methyl radical or one trifluoromethyl CA radical; -n et p are independently one from the other 0, 1 or 2; or one of its pharmaceutically acceptable salts and with said compound being in all the possible racemic, enantiomeric and diastereoisomeric isomer forms.