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US 12,728,174 B2Granted
Radiolabeled MOEM type oligonucleotides and process for their preparation
AssigneeHoffmann-La Roche Inc.
InventorsMartin Robert Edelmann, Thorsten Muser
Life of this patent
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Abstract
The invention comprises radiolabeled MOEM type oligonucleotide of the formula (I), (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.
Claims17
Radiolabeled oligonucleotide of the formula I
- 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 II
- 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* stands for a residue of the formula III
- wherein,
- n is an integer of 1 to 4,
- R1 and R2 independently of each other are hydrogen, CF3, C1-6-alkyl or R1 and R2 together with the carbon atom they are attached to form a C3-5-cycloalkane ring;
- Z* is a radiolabeled C1-C6 alkyl group;
- and
- the receptor targeting moiety is a moiety which adds additional functionality to the oligonucleotide.
10 more elements
Dependencies are inferred from the claim text.