US 2004/0167330 A1 · Novel chelating agents and conjugates thereof, their synthesis and use as diagnois and therapeutic agents

Abstract

The present invention relates to novel bifunctional chelates that are based on asymmetrical cyclen derivatives. The chelates contain either three acetates and one methylphosphonic arm or three acetates and one methylphosphonic arm enabling to link the chelate through P-alkyl within phosphoric acid derivative or through P—O-alkyl within phosphonic derivative to any organic back-bone suited for targeting. Suitable targeting moieties are monoclonal antibodies, their fragments and recombinant derivatives such as single chain antibodies, diabodies, triabodies, humanized, human or chimeric variants but also peptides, aptamers, spiegelmers, nucleotides, anti sense oligomers and conventional small molecules. These novel bifunctional chelates are suited for the production of kits for the routine labelling of targeting moieties to be used in radiotherapy with radiometals such as Yttrium-90, or for Magnetic Resonance Imagining (MRI) using Gadolinium.

Claims20

Dependent claims

A compound of formula 1,

20
wherein
each X is independently selected from C(R1)21 CH2, CHR1, CHR2 or CR1R2,
each Z is independently R1, R2, —OR1 or OR2,
Y is independently OH, OM, OR1, OR2, NH2, NHR1, NHR2, NR1R2, N(R1)2 or N(R2)2 and M is a cation,
each R1 is independently selected from an organic radical having from 1-20 carbon atoms, and
each R2 is independently selected from a functional group or an organic radical having from 1-20 carbon atoms carrying at least one functional group,
or an optical isomer, a coordination compound or a salt thereof.

5 more elements

Dependencies are inferred from the claim text.

Novel chelating agents and conjugates thereof, their synthesis and use as diagnois and therapeutic agents

Life of this patent

Novel chelating agents and conjugates thereof, their synthesis and use as diagnois and therapeutic agents

Life of this patent

Abstract

Claims20