SMALL MOLECULE CONJUGATES FOR INTRACELLULAR DELIVERY OF NUCLEIC ACIDS

Abstract Compounds are provided for the delivery of nucleic acids as well as conjugates of these compounds with nucleic acids, in particular siRNAs. A conjugate is prepared by a process comprising conjugating an antisense oligonucleotide with a compound of formula (III): 41-0 6 "cr.? - j (; 0 _...

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Main Authors HADWIGER, PHILIPP, ROZEMA, DAVID B, OTT, GUENTHER, MOHR, PETER, HOFFMANN, TORSTEN, JAHN-HOFMANN, KERSTIN, KITAS, ERIC A, LEWIS, DAVID L, MUELLER, HANS MARTIN, ROEHL, INGO
Format Patent
LanguageEnglish
French
Published 09.11.2021
Subjects
BEER
BIOCHEMISTRY
CHEMISTRY
COMPOSITIONS THEREOF
CULTURE MEDIA
DERIVATIVES THEREOF
ENZYMOLOGY
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
MICROBIOLOGY
MICROORGANISMS OR ENZYMES
MUTATION OR GENETIC ENGINEERING
NUCLEIC ACIDS
NUCLEOSIDES
NUCLEOTIDES
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
PROPAGATING, PRESERVING OR MAINTAINING MICROORGANISMS
SPIRITS
SUGARS
VINEGAR
WINE
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Summary:Abstract Compounds are provided for the delivery of nucleic acids as well as conjugates of these compounds with nucleic acids, in particular siRNAs. A conjugate is prepared by a process comprising conjugating an antisense oligonucleotide with a compound of formula (III): 41-0 6 "cr.? - j (; 0 _10 0..40 0 0 (m) The oligonucleotide is a single-stranded non-naturally occurring nucleic acid comprising a non-naturally occurring nucleotide, which is a locked nucleic acid (LNA). A process for conjugation is also described, in which the conjugating is canied out using N-Hydroxy-succinimide (NHS) chemistry. Date Recue/Date Received 2021-03-23 Il est décrit des composés abstrait servant à livrer des acides nucléiques ainsi que des conjugués de ces composés et dacides nucléiques, particulièrement de petits ARNi. Un conjugué est préparé au moyen dun procédé qui comprend la conjugaison dun oligonucléotide antisens et dun composé de la formule (III) : 41- 0 6 cr.? - j (; 0 _10 0..40 0 0 (m). Loligonucléotide est un acide nucléique monocaténaire dorigine non naturelle qui comprend un nucléotide dorigine non naturelle, soit un acide nucléique bloqué. Il est également décrit un procédé de conjugaison dans lequel la conjugaison est effectuée au moyen de la chimie du N-hydroxysuccinimide (NHS). Date Recue/Date Received 2021-03-23
Bibliography:Application Number: CA20112976966