TITLE
LIPIDIC COMPOUNDS COMPRISING AT LEAST ONE TERMINAL RADICAL OF
FORMULA -NH-CX- A OR -NH-CX-NH-A, COMPOSITIONS CONTAINING THEM
AND USES THEREOF
APPLICANT
SANOFI PASTEUR
NATIONALITY :FRANCE
Of, 14,ESPACE HENRY VALLEE,
69007LYON
FRANCE
The following specification particularly describes the nature of the invention and
the manner in which it is to be performed.
wo 2022/013443 PCTIEP2021/070026
213
25. A lipid nanoparticle comprising at least one lipidic compound according to any one of
claims I to 17 and at least one nucleic acid.
26. A lipid nanoparticle according to claim 25, further comprising at least one lipid as
defined in any one of claims 18 to 22.
5 27. A pharmaceutical composition comprising (i) at least one nucleic acid and at least one
lipidic compound according to any of claims 1 to 17, or (ii) at least one nucleic acid and at least one
composition according to any one of claims 18 to 22, or (iii) at least one lipid nanoparticle according
to claim 25 or 26.
28. An immunogenic composition comprising (i) at least one nucleic acid encoding for an
lO antigen and at least one lipidic compound according to any of claims 1 to 17, or (ii) at least one
nucleic acid encoding for an antigen and at least one composition according to any one of claims
18 to 22, or (iii) at least one lipid nanoparticle according to claim 25 or 26, wherein the nucleic acid
encodes for at least one antigen.
29. A composition comprising (i) at least one nucleic acid and at least one lipidic compound
15 according to any of claims 1 to 17, or (ii) at least one nucleic acid encoding for an antigen and at
least one composition according to any one of claims 18 to 22, or (iii) at least one lipid nanoparticle
according to claim 25 or 26, for use as a medicament.
30. A composition comprising (i) at least one nucleic acid and at least one lipidic compound
according to any of claims 1 to 17, or (ii) at least one nucleic acid encoding for an antigen and at
20 least one composition according to any one of claims 18 to 22, or (iii) at least one lipid nanoparticle
according to claim 25 or 26, for use in a therapeutic method for preventing and/or treating a disease
seleeted in a gtoup consisting of infectious diseases, allergies, autoimmune diseases, rare blood
disorders, rare metabolic diseases, rare neurologic diseases, and tumour or cancer diseases.
25
lJated this 7th February 2023.
~oS-
(SNIGDHARANI DAS)
OF D.P. AHUJA & CO.
APPLICANT'S AGENT
Regn. No. IN/PA-667
'
~~~~==~~======~====~~====~==~~~~====~~~~~~~ < (54) Title: LIPIDIC COMPOUNDS COMPRISING AT LEAST ONE 'IERMINAL RADICAL OF FORMULA -NH-CX-A OR-NHr'l
CX-NH-A, COMPOSffiONS CONTAINING THEM AND USES THEREOF
~ (57) Abstract The disclosure relates to novel lipidic compounds, lipid nanoparticles (LNPs) containing thereof, and the use of the
~ lipidic co;mpounds or the LNPs for the delivery of nucleic acid. The lipidic compounds as disclosed herein comprise at least one terminal
""""' radical of formula (I): ~~<-NH -CX -(N'H)n-A (I) wherein: - *-represents a single bond linking said radical of formula (I), directly or not.
~ to to one C10 to C5,:Iipophilic or hydrophobic till-group;- nis 0 or 1~ -Xis anoxygenor sulfur atom. and- A represents anoption,;llly
N substituted 5- or 6-membered unsaturated heterocyclic radical or 5- or 6-membered. heteroaromatic ring mdical, bothcont.ai!ring at least
Q one nitrogen atnm; or one of the phamtaceulically acceptable salts of said radical offonnula ([); and \\rith said compound that is in all
N the possible racemic, enantiomeric and diastereoisomeric isomer forms.
0
~
•