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 suitablemore » 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. « less

Inventors:

Fritzberg, Alan ^[1]; Kasina, Sudhaker ^[2]; Johnson, Dennis L ^[3]

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1. Edmonds, WA
2. Kirkland, WA
3. Las Cruces, NM

Issue Date:

1994-01-01

Research Org.:

Univ. of Utah, Salt Lake City, UT (United States)

OSTI Identifier:

869364

Patent Number(s):

5322929

Assignee:

University of Utah Research Foundation (Salt Lake City, UT)

Patent Classifications (CPCs):

A - HUMAN NECESSITIES A61 - MEDICAL OR VETERINARY SCIENCE A61K - PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES

C - CHEMISTRY C07 - ORGANIC CHEMISTRY C07C - ACYCLIC OR CARBOCYCLIC COMPOUNDS

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A - HUMAN NECESSITIES A61 - MEDICAL OR VETERINARY SCIENCE A61K - PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES

A61K2123/00 - Preparations for testing in vivo
A61K51/0478 - {complexes from non-cyclic ligands, e.g. EDTA, MAG3}
A61K51/08 - Peptides, e.g. proteins {, carriers being peptides, polyamino acids, proteins}

C - CHEMISTRY C07 - ORGANIC CHEMISTRY C07C - ACYCLIC OR CARBOCYCLIC COMPOUNDS

C07C233/56 - having carbon atoms of carboxamide groups bound to carbon atoms of carboxyl groups, e.g. oxamides

C - CHEMISTRY C07 - ORGANIC CHEMISTRY C07F - ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM

C07F13/005 - {Compounds without a metal-carbon linkage}

C - CHEMISTRY C07 - ORGANIC CHEMISTRY C07K - PEPTIDES

C07K5/0202 - {containing the structure -NH-X-X-C

Y - NEW / CROSS SECTIONAL TECHNOLOGIES Y02 - TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE Y02P - CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS

Y02P20/55 - Synthetic design, e.g. reducing the use of auxiliary or protecting groups

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DOE Contract Number:  

AC02-83ER60140

Resource Type:

Patent

Country of Publication:

United States

Language:

English

Subject:

radiolabeled; technetium; chelates; renal; function; determinations; directed; novel; radiopharmaceutical; imaging; agents; incorporating; tc-99m; radiolabel; particular; disclosed; relatively; extraction; efficiencies; hence; useful; conducting; procedures; compounds; following; formula; str1; -h; str2; -ch; conh; oh; z; -co; -conh; -so; nh; -conhch; tc; water-soluble; salts; foregoing; presently; preferred; compound; tc-99m-mercaptoacetylglycylglycylglycine; tc-99m-maggg; chelating; reacted; form; str3; definitions; suitable; protective; -coch; -coc; nhcoch; -cocf; provides; methods; preparing; soluble salts; provides methods; imaging agents; chelating agents; chelating agent; soluble salt; radiopharmaceutical imaging; renal function; extraction efficiencies; imaging agent; agents disclosed; radiolabeled technetium; novel radiopharmaceutical; novel imaging; technetium chelates; function determinations; incorporating tc-99m; agents incorporating; /530/