Radiolabeled technetium chelates for use in renal function deter

Drug – bio-affecting and body treating compositions – Radionuclide or intended radionuclide containing; adjuvant...

Patent

Rate now

  [ 0.00 ] – not rated yet Voters 0   Comments 0

Details

534 14, 424 9, A61K 4902, C07F 1300

Patent

active

049801473

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.

REFERENCES:
patent: 3830746 (1974-08-01), Brown
patent: 3833509 (1974-09-01), Brown et al.
patent: 3912935 (1975-10-01), Harris
patent: 4048296 (1977-09-01), Wolfangel
patent: 4296785 (1981-10-01), Vittello et al.
patent: 4444690 (1984-04-01), Fritzberg
patent: 4615876 (1986-10-01), Troutner et al.
A. R. Fritzberg et al., "Synthesis and Evaluation of N.sub.2 S.sub.2 Complexes of Tc-99m as Renal Function Agents," The Journal of Nuclear Medicine, vol. 25, p. 16 (May 1984).
Alan R. Fritzberg, "Current Status of Renal Radiopharmaceuticals," Journal of Nuclear Medicine Technology, vol. 12, No. 4, pp. 177-188 (Dec. 1984).
Sugiura, Yokio; "Newly Synthesized Sulfhydryl-and Imidazole-Containing Tripeptides with a Specific Copper-Binding Site"; Faculty of Pharmaceutic, Kyoto University, Kyoto; Received Dec. 15, 1977.
W. C. Klingensmith, III, et al., "Clinical Comparison of Tc-99m N,N'-Bis (Mercaptoacetamido)Ethylenediamine and (.sup.131)Ortho-iodihippurate for Evaluation of Renal Tubular Function: Concise Communication" The Journal of Nuclear Medicines, May 1982, vol. 23, No. 5, pp. 377-380.
Alan R. Fritzberg et al., "Synthesis and Biological Evaluation of Tc-99m N,N'-Bis(Mercaptoacetyl)-2,3-Diaminopropanoate: A Potential Replacement for (.sup.131)0-Iodohippurate" The Journal of Nuclear Medicine, Jul. 1982, vol. 23, No. 7.
Mallinckrodt, Inc., Technical Product Data, "Hippuran .sup.R I 131 Injection Iodohippurate Sodium I 131 Injection Diagnostic-For Intravenous Use", R1/83 MK-20348 (Mallinckrodt Inc., Diagnostic Products Division, St. Louis, Mo. (63134).
W. C. Klingensmith, III et al., "Clinical Evaluation of Tc-99m N,N'-Bis(mercaptoacetyl)-2,3-Diaminopropanoate as a Replacement for I-131 Hippurate: Concise Communication", The Journal of Nuclear Medicine, vol. 25, No. 1.
R. F. Schneider et al., "N,N'-bis(S-Benzoylmercaptoacetamido) Ethylenediamine and Propylenediamine Ligands as Renal Function Imaging Agents, 1, Alternate Synthetic Methods" The Journal of Nuclear Medicine, vol. 25, No. 2.
Richard F. Schneider, "Alternate Synthesis and Evaluation of a Series of N,N-Bis (Mercaptoacetamido) Ethylenediamine and Propylenediamine Ligands as Renal Imaging Agents," Division of Nuclear Medicine, The Upstate Medical Center, 750 E. Adams St. Syracuse, New York 13210.
Fritzberg, Alan et al., "Synthesis and Biological Evaluation of Technetium-99m MAG.sub.3 as a Hippuran Replacement," Journal of Nuclear Medicine, 27:1, pp. 111-116 (Jan. 1986).
Kasina, Sudhakar et al., "Tissue Distribution Properties of Technetium-99m-Diamide-Dimercaptide Complexes and Potential Use of Renal Radiopharmaceuticals," Journal of Medicinal Chemistry, 29, pp. 1933-1940 (1986).
A. Fritzberg et al., "A Potential Tc-99m Renal Tubular Function Agent: Tc-99m-BIX-N,N'-(Mercaptoacetamido)-2,3-Diaminoproponoate".

LandOfFree

Say what you really think

Search LandOfFree.com for the USA inventors and patents. Rate them and share your experience with other people.

Rating

Radiolabeled technetium chelates for use in renal function deter does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Radiolabeled technetium chelates for use in renal function deter, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Radiolabeled technetium chelates for use in renal function deter will most certainly appreciate the feedback.

Rate now

     

Profile ID: LFUS-PAI-O-1161526

  Search
All data on this website is collected from public sources. Our data reflects the most accurate information available at the time of publication.