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Details for Patent: 4,980,147

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Details for Patent: 4,980,147

Title: Radiolabeled technetium chelates for use in renal function determinations
Abstract:The present invention is directed to novel radiopharmaceutical imaging agents incorporating Tc-99m as a radiolabel. In particular, the novel imaging agents disclosed herein have relatively high renal extraction efficiencies, and hence are useful for conducting renal function imaging procedures. The novel Tc-99m compounds of a present invention have the following general formula: ##STR1## wherein X is S or N; and wherein Y is--H or wherein Y is ##STR2## and where R.sub.1 is --H, --CH.sub.3, or --CH.sub.2 CH.sub.3 ; R.sub.2 is --H, --CH.sub.2 CO.sub.2 H, --CH.sub.2 CONH.sub.2, --CH.sub.2 CH.sub.2 CO.sub.2 H, --CH.sub.2 CH.sub.2 CONH.sub.2, --CH.sub.3, --CH.sub.2 CH.sub.3, CH.sub.2 C.sub.6 H.sub.5, or --CH.sub.2 OH; and Z is --H, --CO.sub.2 H, --CONH.sub.2, --SO.sub.3 H, --SO.sub.2 NH.sub.2, or --CONHCH.sub.2 CO.sub.2 H; and the Tc is Tc-99m; and water-soluble salts thereof. Of the foregoing, the presently preferred Tc-99m compound of the present invention is Tc-99m-mercaptoacetylglycylglycylglycine (Tc-99m-MAGGG). The present invention is also directed to novel chelating agents that may be reacted with Tc-99m to form the foregoing compounds. Such novel chelating agents have the following general formula. ##STR3## where X and Y have the same definitions as above, and wherein Y' is --H.sub.2 when X is N, or wherein Y' is --H, or a suitable protective group such as --COCH.sub.3, --COC.sub.6 H.sub.5, --CH.sub.2 NHCOCH.sub.3, --COCF.sub.3, or --COCH.sub.2 OH when X is S. The present invention also provides methods for preparing and using the novel Tc-99m compounds.
Inventor(s): Fritzberg; Alan (Edmonds, WA), Kasina; Sudhakar (Kirkland, WA), Johnson; Dennis L. (Las Cruces, NM)
Assignee: University of Utah Research Foundation (Salt Lake City, UT)
Filing Date:May 14, 1985
Application Number:06/733,481
Claims:1. A method of evaluating renal function by scintigraphic urography, wherein the improvement comprises the steps of:

injecting a suitable Tc-99m-MAGG-amino acid into a patient;

waiting a suitable period of time while a suitable portion of the Tc-99m-MAGG-amino acid is removed from the patient's blood by the patient's kidneys; and

obtaining a scintigraphic image of the kidneys.

2. A method of evaluating renal function as defined in claim 1, wherein the Tc-99m-MAGG-amino acid is Tc-99M-MAGGG; Tc-99m-MAGG-Alanine; Tc-99m-MAGG-Asparagine; or Tc99m-MAGG-Glutamine.

3. A compound of the formula ##STR18## wherein X is S or N; and wherein Y is --H or wherein Y is ##STR19## and wherein R.sub.1 is --H, --CH.sub.3, or --CH.sub.2 CH.sub.3 ; R.sub.2 is --H, --CH.sub.2 CO.sub.2 H, --CH.sub.2 CONH.sub.2, --CH.sub.2 CH.sub.2 CO.sub.2 H, --CH.sub.2 CH.sub.2 CONH.sub.2, --CH.sub.3, --CH.sub.2 CH.sub.3, --CH.sub.2 OH; and Z is --H, --CO.sub.2 H, --CONH.sub.2, --SO.sub.3 H, --SO.sub.2 NH.sub.2, or --CONCH.sub.2 CO.sub.2 H; and the Tc is Tc-99m; and water-soluble salts thereof.

4. A compound as defined in claim 1, wherein X is S.

5. A compound as defined in claim 4, wherein Y is --CH.sub.2 CO.sub.2 H.

6. A compound as defined in claim 4, wherein Y is --CHCH.sub.3 CO.sub.CO.sub.2 H; --CH(CH.sub.2 CONH.sub.2)CO.sub.2 H; or --CH(CH.sub.2 CH.sub.2 CONH.sub.2)COOH.

7. A compound of the formula ##STR20## wherein X is S or N; and wherein Y is --H or wherein Y is ##STR21## and where R.sub.1 is --H, --CH.sub.3, or --CH.sub.2 CH.sub.3 ; R.sub.2 is --H, --CH.sub.2 CO.sub.2 H, --CH.sub.2 CONH.sub.2, --CH.sub.2 CH.sub.2 CO.sub.2 H, --CH.sub.2 CH.sub.2 CONH.sub.2, --CH.sub.3, --CH.sub.2 CH.sub.3, or --CH.sub.2 OH; and Z is --H, --CO.sub.2 H, --CONH.sub.2, --SO.sub.3 H, --SO.sub.2 NH.sub.2, or --CONHCH.sub.2 CO.sub.2 H; wherein when X is S then element a comprises two hydrogens and at least two of elements b-f are double-bonded oxygens, and other of elements b-f each comprise two hydrogens; wherein when X is N then at least two of elements a-f are double-bonded oxygens, and the other elements a-f each comprise two hydrogens; and the Tc is Tc-99m; and water-soluble salts thereof.

8. A chelate comprising Tc-99m and a ligand having the formula comprising: ##STR22## wherein X is S or N; Y' is --H or a group which protects the sulfur from oxidation where X is S, or where Y' is --H.sub.2 where X is N; and Y is --H.sub.2 or where Y is ##STR23## and where R.sub.1 is --H, --CH.sub.3, or --CH.sub.2 CH.sub.3 ; R.sub.2 is --H, --CH.sub.2 CO.sub.2 H, --CH.sub.2 CONH.sub.2, --CH.sub.2 CH.sub.2 CO.sub.2 H, --CH.sub.2 CH.sub.2 CONH.sub.2, --CH.sub.3, --CH.sub.2 CH.sub.3, or --CH.sub.2 OH; and Z is --H, --CO.sub.2 H, --CONH.sub.2, --SO.sub.3 H, --SO.sub.2 NH.sub.2, or --CONHCH.sub.2 CO.sub.2 H; and the water-soluble salts thereof.

9. A ligand as defined in claim 8, wherein the suitable protective group comprising Y' is --COCH, --COC.sub.6 H.sub.5, --CH.sub.2 NHCOCH.sub.3, --COCF.sub.3, or --COCH.sub.2 OH.
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