Drug – bio-affecting and body treating compositions – Radionuclide or intended radionuclide containing; adjuvant... – In an organic compound
Patent
1991-05-10
1994-02-22
Geist, Gary
Drug, bio-affecting and body treating compositions
Radionuclide or intended radionuclide containing; adjuvant...
In an organic compound
534 10, 534 14, A61K 4902, A61K 4300
Patent
active
052884767
DESCRIPTION:
BRIEF SUMMARY
The present invention relates to a radiopharmaceutical product or radioactive drug in particular having a cardiac tropism, which comprises a nitride complex of a transition metal having a part M.ident.N, in which M represents the transition metal. It more particularly applies to radiopharmaceutical products having a cardiac tropism.
It is pointed out that the term transition metal means a metal whose coating d is partly filled in the standard oxidation degree of said metal. They are elements in periods III to XII of the periodic table of elements consisting of eighteen columns Examples of such metals are Tc, Ru, Co, Pt, Fe, Os, Ir, W, Re, Cr, Mo, Mn, Ni, Rh, Pd, Nb and Ta.
Technetium nitride complexes have been described by J. Baldas et al in the following documents: International Patent Application WO85/03063, J. Chem. Soc. Dalton Trans., 1981, pp. 1798-1801 and in the book "Technetium in Chemistry and Nuclear Medicine", M. Nicolini, G. Bandoli and U. Mazzi, Cortine Int. Verona, 1986, pp. 103 to 108.
These documents describe the preparation of technetium nitride complexes by a substitution reaction on .sup.99m TcNCl.sub.4 and it is stated that these complexes can be used as radiopharmaceutical products. However, these documents fail to provide any results giving evidence regarding the fixing of the complexes in the body and consequently give no indication of their tropisms with respect to certain organs and in particular the heart.
Among the radiopharmaceutical products having a cardiac tropism, technetium complexes are known, which contain as the ligand isonitriles substituted by an ether, in the manner described in European patent application EP-A-0 233 368 and dioxime-based technetium complexes as described in European patent EP-A-0 268 801. These complexes are formed from ligands which are difficult to synthesize.
Thus, research has been carried out to find other radio-pharmaceutical products having satisfactory properties for use as diagnosis or therapy products and more particularly radiopharmaceutical products with a cardiac tropism, e.g. for myocardial scintigraphy.
The present invention specifically relates to a radiopharmaceutical product, which comprises a complex of a transition metal complying with the formula: same or different, comply with the formula: ##STR2## in which V and W, which can be the same or different, represent O, S or Se, n and m, which can be the same or different, are equal to 0 or to 1, Y represents N, P or As, and R.sup.1 and R.sup.2, which can be the same or different, represent a straight or branched alkyl radical with 1 to 10 carbon atoms, which is either not substituted or substituted by --O--R.sup.3, OOC--R.sup.3, OCNR.sup.4 R.sup.5 or --NR.sup.4 R.sup.5 groups, in which R.sup.3 is a straight or branched alkyl radical with 1 to 5 carbon atoms and R.sup.4 and R.sup.5, which can be the same or different, are hydrogen atoms or straight or branched alkyl radicals with 1 to 5 carbon atoms, or in which R.sup.1 and R.sup.2 together form a hydrocarbon cycle optionally containing one or more heteroatoms.
The radiopharmaceutical products incorporating transition metal complexes in accordance with the above formula in particular have a cardiac tropism, which makes them interesting as heart therapy or diagnosis products.
In the radiopharmaceutical products according to the invention, the transition metal nitride complex can be of different types.
Thus, according to a first embodiment of the invention, in the aforementioned formula, Y represents N, m and n are equal to O, L.sup.1 and L.sup.2 are identical and R.sup.1 and R.sup.2 are unsubstituted alkyl radicals.
In this first embodiment according to the invention, R.sup.1 and R.sup.2 are preferably also identical.
For example, L.sup.1 and L.sup.2 can be in accordance with the following formulas: ##STR3##
According to a second embodiment of the invention, Y represents N, m and n are equal to 0, L.sup.1 and L.sup.2 are identical and at least one of the R.sup.1 and R.sup.2 represents an alkoxy alkyl radical.
For example, L.sup.1 and
REFERENCES:
patent: 4923969 (1990-05-01), Bonnyman et al.
patent: 4925925 (1990-05-01), Deutsch
L. Kaden, et al.; "Nitrido complexes of technetium (V)", & Isotopenprasix 1981, 17(4), 174-5 Chemical Abstracts, vol. 95, No. 2, Jul. 13, 1981, p. 716, resume No. 17322r, Columbus, Ohio.
J. Baldas, et al.:; "The preparation, characterization and reactions of chlorotetrakis(thiourea)-nitridotechnetium(V) chloride", & Inorg. Chim. Acta 1988, 141(2), 153-4, Chemical Abstracts, vol. 108, No. 22, May 30, 1988, p. 712, resume No. 197162g, Columbus. Ohio.
International Journal of Radiation/Applications & Instrumentation Paret A. vol. 38, No. 8, 1987, GB pp. 665-668; Ballinger, J. R.: "Technetium-99m Diethyldithiocarbamate (DDC): Comparison with Thallium-201DDC as an Agent for Brain Imaging".
International Journal of Applied Radiation and Isotopes, vol. 36, No. 2, Feb. 1985, Oxford, GB, pp. 133-139, Baldas J. et al.: "Substitution reactions of 99m TcNC14-A. Route to a new class of 99m Tc-Radiopharmaceuticals".
Bardy Andre
Duatti Adriano
Magon Luciano
Marchi Andrea
Pasqualini Roberto
Cis Bio International
Geist Gary
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