Cleavable bifunctional coupling agents

Details Cleavable bifunctional coupling agents Cleavable bifunctional coupling agents

1988-08-24

1992-09-01

Springer, David B.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

C07D207448

Patent

active

051440431

ABSTRACT:
A bifunctional coupling agent for joining a sulfhydryl containing protein or peptide and a metallic radionuclide comprising a sulfhydryl selective electrophile, a chelator containing at least one protected thiol and a organic linking radical containing at least one cleavable site which serves to join said electrophile and said chelator is disclosed. A radiodiagnostic or radiotherapeutic precursor comprising an antibody or antibody fragment and the specified bifunctional coupling agent bound to a sulfhydryl group on the antibody or antibody fragment and a radiodiagnostic or radiotherapeutic agent comprising such precursor having a metallic radionuclide bound thereto are also disclosed.

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Childs, et al., J. Nucl. Med., 26, 293 (1985).
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Paik, et al., J. Nucl. Med., 28, 602 (1988).
Deshpande, et al., J. Nucl. Med., 29, 922-923 (1988).
Optimum Conditions for Labeling of DTPA-Coupled Antibodies with Technetium-99m by R. L. Childs and D. J. Hnatowich pp. 293-299 (1985).

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