Polychelant compounds for targeted radiotherapy

The invention encompasses compounds of general formula (I), and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof: wherein C is a chelating agent and ngt; l is a polyfunctional linker moiety comprising a plurality of functional groups for covalently linki...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Hauptverfasser: BRUMBY THOMAS, CRUCIANI VALENTINA, CUTHBERTSON, ALAN, CHRISTIAN AMBROSE, RAFIQUE WILLIAM, INDREVOLL, BJU RN, KOLOGOSTY, VIATCHESLAV, R
Format: Patent
Sprache:chi ; eng
Schlagworte:
Online-Zugang:Volltext bestellen
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
Beschreibung
Zusammenfassung:The invention encompasses compounds of general formula (I), and stereoisomers, tautomers, N-oxides, hydrates, solvates and salts thereof, and mixtures thereof: wherein C is a chelating agent and ngt; l is a polyfunctional linker moiety comprising a plurality of functional groups for covalently linking a chelating agent, such as a main chain comprising a polyamine or a polyacid, or an amino acid-containing polymer comprising a side chain having an amino, thiol or carboxylic acid moiety, such as lysine, cysteine or glutamic acid, and V is a moiety targeting a tissue, where m = 1-5, and m = 1-5. It is preferably coupled to a polyfunctional linker moiety L via a coupling moiety or directly to a chelating moiety C. [(C) n-L]-(V) m (I). 本发明涵盖通式(I)的化合物、及其立体异构体、互变异构体、N-氧化物、水合物、溶剂化物和盐,以及它们的混合物:其中C为螯合剂且n>1,L为包含用于共价连接螯合剂的多个官能基的多官能连接基部分,例如含多元胺或多元酸的主链或包含具有氨基、硫醇或羧酸部分的侧链的含氨基酸的聚合物,所述氨基酸例如赖氨酸、半胱氨酸或谷氨酸,且V为靶向组织的部分,其中m=1-5,其优选通过偶联部分偶联至多官能连接基部分L或直接偶联至螯合剂部分C。[(C)n-L]-(V)m(I)。