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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:
 [1];  [2];  [3]
  1. Edmonds, WA
  2. Kirkland, WA
  3. Las Cruces, NM
Issue Date:
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
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
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/

Citation Formats

Fritzberg, Alan, Kasina, Sudhaker, and Johnson, Dennis L. Radiolabeled technetium chelates for use in renal function determinations. United States: N. p., 1994. Web.
Fritzberg, Alan, Kasina, Sudhaker, & Johnson, Dennis L. Radiolabeled technetium chelates for use in renal function determinations. United States.
Fritzberg, Alan, Kasina, Sudhaker, and Johnson, Dennis L. Sat . "Radiolabeled technetium chelates for use in renal function determinations". United States. https://www.osti.gov/servlets/purl/869364.
@article{osti_869364,
title = {Radiolabeled technetium chelates for use in renal function determinations},
author = {Fritzberg, Alan and Kasina, Sudhaker and Johnson, Dennis L},
abstractNote = {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.},
doi = {},
journal = {},
number = ,
volume = ,
place = {United States},
year = {1994},
month = {1}
}

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Works referenced in this record:

The reaction of trans-cinnamoyl-papain with a series of polyglycinamides of varying chain length
journal, April 1967


Tissue distribution properties of technetium-99m-diamide-dimercaptide complexes and potential use as renal radiopharmaceuticals
journal, October 1986


Evaluation of the renal excretion characteristics of technetium-99m mercaptoacetylglycyl-D-alanylglycine in healthy volunteers
journal, April 1992


Solution equilibria of copper(II) and nickel(II) complexes of glycyl peptide amides
journal, June 1975


Reductive Deamination of Oligopeptides by Solvated Electrons in Aqueous Solution
journal, November 1971