AMINOOXYLIPIDS FOR THE CONSTRUCTION OF SELF-ASSEMBLING LIPOSOMAL SYSTEMS ENABLING THEIR SUBSEQUENT MODIFICATION BY BIOLOGICALLY FUNCTIONAL MOLECULES

Result code in IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00027162%3A_____%2F21%3AN0000084" target="_blank" >RIV/00027162:_____/21:N0000084 - isvavai.cz</a>

Result on the web

<a href="https://isdv.upv.cz/webapp/resdb.print_detail.det?pspis=EP/3535238&plang=CS" target="_blank" >https://isdv.upv.cz/webapp/resdb.print_detail.det?pspis=EP/3535238&plang=CS</a>

DOI - Digital Object Identifier

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Result language

angličtina

Original language name

AMINOOXYLIPIDS FOR THE CONSTRUCTION OF SELF-ASSEMBLING LIPOSOMAL SYSTEMS ENABLING THEIR SUBSEQUENT MODIFICATION BY BIOLOGICALLY FUNCTIONAL MOLECULES

Original language description

New aminooxylipids of general formula (I), wherein n1 = 5-30 and X is polymethylene linker of the general formula (II) where n2 = 2 -10, or X is polyethylene glycol linker of the general formula (III), wherein n3 = 1-14, are provided. A method of preparation of the aminooxylipids of general formula (I) characterized in that the acylation of N-tert-butoxycarbonyl-polymethylenediamine {(CH3)3C-0-(C=0)-HN-(CH2)n-N H2, n = 2 -13}, or N-tert- butoxycarbonyl-polyethyleglycoldiamine {(CH3)3C-0-(C=0)-HN-(CH2)2-[0-(CH2)]n-0-(CH2)2NH2, n = 1-14} with in position C(2) symmetrically branched fatty acids of general formula (IV), wherein n1 = 5-30, in the presence of condensation reagent, or from acid of general formula (IV) derived acylchloride of general formula (V) wherein n1 = 5-30, produces N-Boc-aminolipids of general formula (VI), wherein n1 = 5-30 a X is polymethylene linker of the general formula (II) or X is polyethylene glycol linker of the general formula (III). These are converted by debocylation to aminolipids of general formula (VII), wherein n1 = 5-30 and X is polymethylene linker of the general formula (II) or X is polyethylene glycol linker of the general formula (III). By their condensation with N-terf-butoxycarbonyl-aminooxyacetic acid in the presence of condensation reagent, N-Boc-aminooxylipids of general formula (VIII), where in n1 = 5- 30 and X is polymethylene linker of the general formula (II) or X is polyethylene glycol linker of the general formula (III), are obtained, which by debocylation afford aminooxylipids of general formula (I). Acylchlorides of general formula (V) are prepared by reaction of acid of general formula (IV) with oxalylchloride in the presence of catalytic amount of N, N-dimethylformamide in organic aprotic solvent. The use of nontoxic aminooxylipids of the general formula I for construction of nontoxic self-assembly liposomal carriers of therapeutics presenting aminooxy groups and so-called "post-liposomal" modification of these carriers with biologically functional molecules using oxime ligation technique (binding counterparts: aminooxy group and aldehyde or ketone group).

Czech name

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Czech description

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Type

P - Patent

CEP classification

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OECD FORD branch

10401 - Organic chemistry

Project

Result was created during the realization of more than one project. More information in the Projects tab.

Continuities

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)<br>I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Publication year

2021

Confidentiality

U - Předmět řešení projektu je utajovanou skutečností podle zvláštních právních předpisů nebo je skutečností, jejíž zveřejnění by mohlo ohrozit činnost zpravodajské služby. Údaje o projektu jsou upraveny tak, aby byly zveřejnitelné

Patent/design ID

CZ/EP 3535238

Publisher

EPO_1 -

Publisher name

European Patent Office

Place of publication

Munich, The Hague, Berlin, Vienna, Brussels

Publication country

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Date of acceptance

Apr 21, 2021

Owner name

Vysoká škola chemicko-technologická v Praze, Technická 5, 16628 Praha 6, Česká republika; Výzkumný ústav veterinárního lékařství, v.v.i., Hudcova 296/70, 621 00 Brno, Česká republika; Apigenex s.r.o., Poděbradská 56/186, 18066 Praha 9, Česká republika

Method of use

A - Výsledek využívá pouze poskytovatel

Usage type

A - K využití výsledku jiným subjektem je vždy nutné nabytí licence