Organic compounds -- part of the class 532-570 series – Organic compounds – Radioactive metal containing
Patent
1990-05-01
1992-01-07
Maples, John S.
Organic compounds -- part of the class 532-570 series
Organic compounds
Radioactive metal containing
424 11, C07F 500, A61K 4902
Patent
active
050793462
ABSTRACT:
Complexes having the formula: ##STR1## where each of R.sub.1 -R.sub.14 is independently selected from the group consisting of hydrogen, alkyl groups in which one or more carbon atoms is optionally substituted by a heteroatom such as N, O or S, and phenyl optionally mono- or di-substituted with a substituent selected from the group consisting of --SR.sub.15,-- OR.sub.15, and --NR.sub.15 R.sub.16, where R.sub.15 and R.sub.16 are independently selected from H and alkyl groups; or each grouping of R.sub.1 and R.sub.2, R.sub.3 and R.sub.4, R.sub.5 and R.sub.6, R.sub.7 and R.sub.8, R.sub.11 and R.sub.12, and R.sub.13 and R.sub.14 may independently be taken together to form a cyclic alkyl in which one or more carbon atoms is optionally substituted by a heteroatom, and Ga is a radioactive gallium isotope, and pharmaceutically acceptable salts thereof prepared from gallium radioiosotopes and ligands such as tetraethylcyclohexyl-bis-aminoethanethiol (BAT-TECH) are disclosed which, because of their high uptake in the heart and lipid-solubility, should be useful for myocardial perfusion imaging.
REFERENCES:
patent: 4885363 (1989-12-01), Tweedle et al.
Green, Mark A. and Welch, Michael J. "Review--Gallium Radiopharmaceutical Chemistry", Nucl. Med. Biol., vol. 16, No. 5, pp. 435-448 (1989).
Kung, H. F., et al., "Synthesis of New Bis(aminoethanethiol) (BAT) Derivatives: Possible Ligands for .sup.99m Tc Brain Imaging Agents", J. Med. Chem., 1985, 28, 1280.
Liu, B. L., Kung, H. F., Jin, Y. T., Zhu, L., and Meng, M.: A new myocardial imaging agent: synthesis, characterization and biodistribution of [.sup.113m In]TE-BAT.
J. Nucl. Med. 30:367-373, 1989.
Green, M. A., Welch, M. J., Mathias, C. J., et al.: Gallium-68 1,1,1-tris (5-methoxysalicylaldiminomethyl) ethane: A potential tracer for evaluation of myocardial blood flow, J. Nucl. Med. 26:170-180, 1985.
Green, M. A., Klippenstein, D. L., Tennison, J. R.: Copper (II) bis(triosemicarbazone) complexes as potential tracers for evaluation of cerebral and myocardial blood flow with PET, J. Nucl. Med. 29: 1549-1557, 1989.
Maples John S.
Trustees of the University of Pennsylvania
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