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US 2020/0345871 A1Published application
Radiolabelled oligonucleotides and process for their preparation
AssigneeHoffmann-La Roche Inc.
InventorMARTIN ROBERT EDELMANN
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Abstract
The invention comprises radiolabeled oligonucleotide of the formula I wherein n, X1, X2, the linker 1, the linker 2, Q and the receptor targeting moiety are as defined I the description. The radiolabeled oligonucleotides of the formula I can be used for the determination of the biodistribution and pharmacokinetics of the oligonucleotide in the tissue or body fluid.
Claims30
A radiolabeled oligonucleotide comprising formula I:
- wherein,
- n is 0 or 1;
- X and X2 independently of each other are S or O;
- linker 1 is a C2-12-alkylene bridge, an ethylene glycol bridge containing 1 to 10 ethylene glycol units, or a glycerol based bridge of the formula:
- wherein m is an integer of 1 to 6;
- linker 2 is an optionally amino group protected amino C2-12-alkylene bridge or an amino ethylene glycol bridge containing 1 to 10 ethylene glycol units;
- Q is a residue of the formula 2a or 2b
- wherein R1* and R2* are each independently radiolabeled C1-6-alkyl groups;
- and
- the receptor targeting moiety is a non-nucleotide moiety which adds additional functionality to the oligonucleotide.
7 more elements
(canceled)
An oligonucleotide comprising formula X:
- wherein,
- n is 0 or 1;
- X1 and X2 independently of each other are S or O;
- linker 1 is a C2-12-alkylene bridge, an ethylene glycol bridge containing 1 to 10 ethylene glycol units, or a glycerol based bridge of the formula:
- wherein m is an integer of 1 to 6;
- linker 2 is an optionally amino group protected amino C2-12-alkylene bridge or an amino ethylene glycol bridge containing 1 to 10 ethylene glycol units;
- Q is a residue of the formula 2a′ or 2b′
- wherein R1 and R2 are each independently C1-6-alkyl groups;
- and
- the receptor targeting moiety is a non-nucleotide moiety which adds additional functionality to the oligonucleotide.
7 more elements
Dependencies are inferred from the claim text.