Tetraaza- or N2S2- complexants, and their use in radiodiagnostics or radiotherapy

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The present invention provides for substituted metal chelating compounds of the formula : in which at least two of the chelating atoms are nitrogen which are directly attached to aromatic rings and one or more of those nitrogen atoms has attached thereto a substituent other than hydrogen, and methods for making and using these compounds. Another aspect of the invention provides for the use of the chelation compounds described above in methods for diagnostic and therapeutic purposes. A diagnostic method is described for detecting the presence or absence of a target site within a mammalian host. This method comprises providing to cells a diagnostically effective dose of a compound of the present invention which contains a metal radionuclide, such as 99mTc and/or 111In, and detecting the biodistribution of the radionuclide. A therapeutic method is described for delivering a radionuclide, such as 186Re/188Re, 90Y, and 153Sm, to a target site within a mammalian host. This method comprises providing to cells a therapeutically effective dose of a chelate compound of the present invention.