Ligands for improving metal chelate formation kinetics

C - Chemistry – Metallurgy – 07 – K

Patent

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C07K 5/00 (2006.01) A61K 51/04 (2006.01) A61K 51/08 (2006.01) C07B 59/00 (2006.01) C07D 213/40 (2006.01) C07D 213/64 (2006.01) C07D 213/68 (2006.01) C07F 13/00 (2006.01) C07K 14/655 (2006.01) C07K 14/815 (2006.01) A61K 43/00 (1990.01) A61K 49/02 (1990.01)

Patent

CA 2129036

2129036 9315771 PCTABS00024 Amide-thiolate ligands having improved metal chelate formation kinetics are disclosed. The ligands include an amine to facilitate rapid formation of an amine-amide-thiolate intermediate complex, followed by transfer of the metal to or conversion of the ligand to a thermodynamically stable amide-thiolate complex. In one embodiment of the invention, the amine is a tertiary amine, or its equivalent, strategically located to facilitate complex formation. In another embodiment of the invention, the amine is part of pyridine containing a lower alkoxy substituent in the 2 or 4 ring position. O-dealkylation occurs upon complexation causing the amine to become a vinylogous amide as part of a thermodynamically stable amide-thiolate complex. The amide-thiolate ligands of the present invention may be used for post formed labeling of biological substances for use in the fields of diagnosis and therapy.

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