Metal chelates as pharmaceutical imaging agents, processes of ma

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

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556 1, 556 42, 556 45, 556 57, 556 63, 556107, 556130, 556137, 514492, 514494, 514495, 514497, 514498, 514502, 514505, 562556, 562561, 562565, 544225, 534 14, A61K 5100, C07F 1900, C07F 1300

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059550538

ABSTRACT:
The present invention relates to novel metal chelates, exemplified as technetium-99m or rhenium chelates, and to the process of preparing such metal chelates from corresponding ligands. These ligands and their corresponding metal chelates are synthesized to have a cysteinylethylene (EC) structure, a thioacetamidethiourea (TATU) structure, or a dithiourea (DTU) structure. The present invention further relates to a pharmaceutical composition comprising a metal chelate, for example, a .sup.99m Tc-chelate, to the use of the composition for renal imaging and examination of renal function, and to a kit for preparing such a composition prior to use.

REFERENCES:
patent: 4849511 (1989-07-01), Verbruggen
patent: 4925650 (1990-05-01), Nosco et al.
Verbruggen, A.M. et al., "Technetium-99m-L,L-Ethylenedicysteine: A Renal Imaging Agent. I. Labeling and Evaluation in Animals," J. Nuclear Medicine (Apr. 1992) 33(4):551-557.
Taylor, A., Jr. et al., "Technetium-99m MAG.sub.3 Kit Formulation: Preliminary Results in Normal Volunteers and Patients with Renal Failure," J. Nuclear Medicine (May 1988) 29(5):616-622.
Shattuck, L.A. et al., "Evaluation of the Hepatobiliary Excretion of Technetium-99m-MAG3 and Reconstitution Factors Affecting Radiochemical Purity," J. Nuclear Medicine (Feb. 1994) 35(2):349-355.
Verbruggen, A. et al., "Evaluation of the Diastereomers of Tc-99m-Mercaptoace-Tylglycyl-D-Alanylglycine (Tc-99m-D-MAGAG) in Primates," Proceedings of 35th Annual Meeting, J. Nuclear Medicine (May 1988) 29(5):909-910.
Eshima, D. et al., "Animal Evaluation of Technetium-99m Triamide Mercaptide Complexes as Potential Renal Imaging Agents," J. Nuclear Medicine (Jul. 1987) 28(7):1180-1186.
VanNerom, C. et al., "Comparison of Renal Excretion Characteristics of Isomers L,L and D,D of Tc-99m Ethylenedicysteine," J. Nuclear Medicine, Proceedings of 37th Annual Meeting, p. 806 (1990).
Bubeck, B. et al., "Pharmacokinetics of Technetium-99m-MAG.sub.3 is Humans," J. Nuclear Medicine (Aug. 1990) 31(8):1285-1293.

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