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1. WO2011144892 - CATIONIC LIPIDS

Publication Number WO/2011/144892
Publication Date 24.11.2011
International Application No. PCT/GB2011/000749
International Filing Date 17.05.2011
IPC
A61K 47/48 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
48the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
C12N 15/88 2006.1
CCHEMISTRY; METALLURGY
12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
15Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
09Recombinant DNA-technology
87Introduction of foreign genetic material using processes not otherwise provided for, e.g. co-transformation
88using microencapsulation, e.g. using liposome vesicle
C07C 233/18 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
233Carboxylic acid amides
01having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
16having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
17with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
18having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
C07K 5/068 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
5Peptides having up to four amino acids in a fully defined sequence; Derivatives thereof
04containing only normal peptide links
06Dipeptides
068the side chain of the first amino acid containing more amino groups than carboxyl groups, or derivatives thereof, e.g. Lys, Arg
C07K 5/09 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
5Peptides having up to four amino acids in a fully defined sequence; Derivatives thereof
04containing only normal peptide links
08Tripeptides
09the side chain of the first amino acid containing more amino groups than carboxyl groups, or derivatives thereof, e.g. Lys, Arg
CPC
A61K 31/713
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
70Carbohydrates; Sugars; Derivatives thereof
7088Compounds having three or more nucleosides or nucleotides
713Double-stranded nucleic acids or oligonucleotides
A61K 47/543
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51the non-active ingredient being a modifying agent
54the modifying agent being an organic compound
543Lipids, e.g. triglycerides; Polyamines, e.g. spermine or spermidine
A61K 47/6455
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51the non-active ingredient being a modifying agent
62the modifying agent being a protein, peptide or polyamino acid
64Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
645Polycationic or polyanionic oligopeptides, polypeptides or polyamino acids, e.g. polylysine, polyarginine, polyglutamic acid or peptide TAT
6455Polycationic oligopeptides, polypeptides or polyamino acids, e.g. for complexing nucleic acids
C07C 251/02
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
251Compounds containing nitrogen atoms doubly-bound to a carbon skeleton
02containing imino groups
C07K 5/0819
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
5Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
04containing only normal peptide links
08Tripeptides
0819with the first amino acid being acidic
C12N 15/88
CCHEMISTRY; METALLURGY
12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
15Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
09Recombinant DNA-technology
87Introduction of foreign genetic material using processes not otherwise provided for, e.g. co-transformation
88using microencapsulation, e.g. using ; amphiphile; liposome vesicle
Applicants
  • THE UNIVERSITY COURT OF THE UNIVERSITY OF EDINBURGH [GB]/[GB] (AllExceptUS)
  • UNCITI-BROCETA, Asier [ES]/[GB] (UsOnly)
  • LIBERSKA, Aleksandra [PL]/[PL] (UsOnly)
  • BRADLEY, Mark [GB]/[GB] (UsOnly)
Inventors
  • UNCITI-BROCETA, Asier
  • LIBERSKA, Aleksandra
  • BRADLEY, Mark
Agents
  • NAISMITH, Robert, Stewart
Priority Data
1008267.518.05.2010GB
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) CATIONIC LIPIDS
(FR) LIPIDES CATIONIQUES
Abstract
(EN) The invention provides a cationic lipid comprising: (i) one head group, comprising one or more amino acids, in which at least one amino acid has a side chain that comprises a cationic moiety or a cationic precursor; a linking moiety of formula (5): -(HNR5)2NC(0)R3C(0)- (5), wherein: each R5 is independently an optionally substituted alkylene moiety; and R3 is an optionally substituted alkylene or alkenylene moiety; and (iii) two lipophilic moieties, wherein the head group and each of the lipophilic moieties are connected to the linking moiety through amide linkages.
(FR) La présente invention concerne un lipide cationique comprenant : (i) un groupe de tête comportant un ou plusieurs acides aminés, dans lequel au moins un acide aminé comprend une chaîne latérale comportant un groupe fonctionnel cationique ou un précurseur cationique; (ii) un groupe fonctionnel de liaison de formule (5) : -(HNR5)2NC(0)R3C(0)- (5), dans laquelle chaque R5 représente indépendamment du reste un groupe alkylène éventuellement substitué et R3 représente un groupe alcénylène ou alkylène éventuellement substitué; et (iii) deux groupes fonctionnels lipophiles. Le groupe de tête et chacun des groupes fonctionnels lipophiles sont reliés au groupe fonctionnel de liaison par des liaisons amides.
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