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US 9,428,538 B2Granted
Optimized in vivo delivery system with endosomolytic agents for nucleic acid conjugates
AssigneesDna Therapeutics, Institut Curie, Centre National De La Recherche Scientifique
InventorsJian-Sheng Sun, Marie Dutreix, Maria Quanz
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Abstract
The present invention relates to an optimized in vivo delivery system with endosomolytic agents for nucleic acid of therapeutic interest conjugated to molecules facilitating endocytosis, in particular for use in the treatment of cancer.
Claims18
A conjugated nucleic acid molecule which has one of the following formulae:
- wherein the underlined nucleotide refers to a nucleotide having or not having a phosphorothioate or methylphosphonate backbone, the linked L′ is selected from the group consisting of hexaethyleneglycol, teradeoxythymidylate (T4) and 2,19-bis(phosphor)-8-hydraza-1-hydroxy-4-oxa-9-oxo-nonadecane;
- m is 1, L is a carboxamido oligoethylene glycol and C is selected from the group consisting of dioleoyl, octadecyl, folic acid, tocopherol and cholesterol.
A conjugated nucleic acid molecule of the following formula:
Dependencies are inferred from the claim text.