Small molecule conjugates for intracellular delivery of biologically active compounds
US-9301990-B2 · Apr 5, 2016 · US
US9968647B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9968647-B2 |
| Application number | US-201615090147-A |
| Country | US |
| Kind code | B2 |
| Filing date | Apr 4, 2016 |
| Priority date | Dec 29, 2010 |
| Publication date | May 15, 2018 |
| Grant date | May 15, 2018 |
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The invention provides novel compounds and conjugates of these compounds useful for the delivery of biologically active substances. Further novel design criteria for chemically stabilized siRNA particular useful when covalently attached to a delivery polymer to achieve in vivo mRNA knock down are disclosed therein.
Opening claim text (preview).
What is claimed is: 1. A conjugate prepared by a process comprising conjugating an oligonucleotide with a compound of formula (III): wherein the oligonucleotide is a single-stranded antisense oligonucleotide with at least one-naturally occurring nucleic acid nucleotide; and where the non-naturally occurring nucleotide is locked nucleic acid (LNA). 2. The conjugate of claim 1 wherein the oligonucleotide comprises a C-6 aminolinker. 3. A pharmaceutical composition comprising a conjugate according to claim 1 .
2'-R Modification · CPC title
Acyclic or carbocyclic radicals, substituted by hetero rings · CPC title
Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids · CPC title
interfering nucleic acids [NA] · CPC title
Linear peptides containing at least one abnormal peptide link · CPC title
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