Metal radionuclide chelating compounds for improved chelation ki

Details Metal radionuclide chelating compounds for improved chelation ki Metal radionuclide chelating compounds for improved chelation ki

1991-12-06

1995-07-25

Geist, Gary

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

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

549415, 549419, 549472, 549479, 564154, 558232, 558251, 558256, C07D20746, C07D31500, C07C23301, C07C 6700

Patent

active

054363527

ABSTRACT:
The present invention provides metal chelating compounds, to chelates and chelate-targeting agent conjugates formed from the chelating compounds, and to methods for making and using these compositions. The chelating compounds incorporate two nitrogen atoms and three sulfur atoms ("N.sub.2 S.sub.3 "), two nitrogen atoms and four sulfur atoms ("N.sub.2 S.sub.4 "), or three nitrogen atoms and three sulfur atoms ("N.sub.3 S.sub.3 "). Metals, and metal oxides, capable of being chelated by the compounds include those that are radionuclides, such as .sup.99m Tc and .sup.186/188 Re.
The targeting agent portion of the chelate-targeting agent conjugates provided includes antibodies, peptides, hormones, enzymes and biological response modifiers. Methods for making the conjugates are provided and encompass the addition of a metal, or metal oxide, to a chelating compound prior to attachment to a targeting agent as well as subsequent to the attachment.
Another aspect of the invention provides kits for producing chelate-targeting agent conjugates for radiopharmaceutical use.
An additional aspect of the invention provides methods for using the chelate-targeting agent conjugates for diagnostic and therapeutic purposes, such as detection of a target site and delivery of a radionuclide to the site, respectively.

REFERENCES:
patent: 4914241 (1990-04-01), Hesse et al.
patent: 4987130 (1991-01-01), Tsushima et al.
patent: 5196550 (1993-03-01), Long, III et al.
Greene, Protective Groups in Organic Synthesis, Chapter 6, pp. 914-196, 1981.
Yano et al., "4-Substituted 1,2-dithiolane derivatives," Jap. Pat. No. 61,103,880 (May 22, 1986) as abstracted in CA105:208855.
Bal et al., Rocz. Chem. 50(5):961-6 as abstracted in CA86:29452, 1976.

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