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US 10,874,752 B2Granted
MIBG analogs and uses thereof
AssigneeBoard of Regents of the University of Nebraska
InventorsJanina Baranowska-Kortylewicz, Zbigniew P. Kortylewicz
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Abstract
Compounds and compositions for targeting cells expressing norepinephrine transporter, and methods of making and using the same. The compounds comprise MIBG analogs conjugated to active agents for treatment and/or diagnosis of various conditions, including neuroblastoma.
Claims21
A therapeutic and/or diagnostic compound for selective targeting of norepinephrine transporter in a cell, comprising an MIBG analog conjugated to an active agent, said MIBG analog being selected from the group consisting of:
- where n is 1-5, and the wavy line indicates the point of attachment to the active agent wherein said active agent is a radiolabeled thymidine analog of the formula:
- wherein:
- R represents an Auger electron-emitting radionuclide;
- Ra represents —OH, a natural or unnatural L- or D-amino acid residue, a peptide comprising natural or unnatural L- or D-amino acid residues, cycloSaligenyl phosphotriester moiety, or said MIBG analog, and
- Rb represents a substituted or unsubstituted C1-C6 alkoxy, C1-C8 alkanoate group, —OH, a natural or unnatural L- or D-amino acid residue, a peptide comprising natural or unnatural L- or D-amino acid residues, cycloSaligenyl phosphotriester moiety, or said MIBG analog,
- provided that at least one of the Ra and Rb substituents represents said MIBG analog.
3 more elements
Dependencies are inferred from the claim text.