Drug – bio-affecting and body treating compositions – Radionuclide or intended radionuclide containing; adjuvant... – In an organic compound
Patent
1998-01-16
2000-06-06
Dees, Jose' G.
Drug, bio-affecting and body treating compositions
Radionuclide or intended radionuclide containing; adjuvant...
In an organic compound
534 10, 534 14, A61K 5108, C07F 500
Patent
active
060714921
DESCRIPTION:
BRIEF SUMMARY
BACKGROUND OF THE INVENTION
The present invention relates to a cardiac tropism radiopharmaceutical product incorporating a nitride complex of a transition metal M having a central part M.tbd.N usable for myocardial scintigraphy.
According to the invention, the term transition metal is understood to mean a metal, whose layer d is partly filled in the usual degree of oxidation of said metal. It applies to elements of periods III to XII of the periodic table of elements having 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 WO-85/03063, J. Chem. Soc. Dalton Trans., 1981, pp 1796-1801 and the book "Technetium in Chemistry and Nuclear Medicine", Ed. M. Nicolini, G. Bandoli, U. Mazzi, Cortine Int. Verone, 1986, pp 103 to 108.
DESCRIPTION OF THE BACKGROUND
Technetium nitride complexes having a cardiac tropism have been described in WO-A-90/06137. These complexes have a central portion M.tbd.N and ligands of the dithiocarbamate type having side groups of the alkyl type, optionally substituted by alkoxy, alkylcarboxy, carbamoyl or amino groups.
These complexes have good biological properties with respect to their cardiac retention, but can have a disturbing, early pulmonary fixation for myocardial examinations and they are relatively slowly eliminated from the organism, particularly the heart.
This is a disadvantage for the scintigraphic examination of the myocardiuim. Thus, a complete examination of the myocardium generally requires two injections of the radiopharmaceutical product, one at rest and the other after an effort test. With radiopharmaceutical products having a stable fixation in the myocardium, these four injections must be spaced by a minimum of 4 hours in order to eliminate the residual cardiac activity due to the first injection. It would therefore be of significant interest to have more rapidly eliminated, cardiac tropism radiopharmaceutical products.
Another problem encountered with radiopharmaceutical products of this type is their hepatic fixation, which can be prejudicial if it is of a persistent nature. Thus, such a fixation does not make it possible to carry out a satisfactory scintigraphic examination of the myocardium, when the second injection is too close to the first. It would therefore be of interest to have cardiac tropism radiopharmaceutical products which are rapidly eliminated from the liver and heart.
SUMMARY OF THE INVENTION
The present invention relates to radiopharmaceutical products incorporating a transition metal nitride complex, which are more rapidly eliminated from the heart and which do not have disturbing pulmonary and hepatic fixations. These complexes also comprise ligands of the dithiocarbamate type, but the alkyl groups of these ligands are either a branched chain having at least one ether function, or a branched chain, whereof a carbon atom is substituted by two alkoxy groups, which corresponds to an acetyl function.
According to the invention, the radiopharmaceutial product comprises a complex of a transition metal complying with the formula: same or different, comply with the formula: ##STR2## in which R and R', which are the same or different, represent: an alkyl group, ##STR3## in which:
R.sup.1 is an alkyl group, R.sup.2 is an alkyl group or an alkoxy group, or R.sup.1 and R.sup.2 form together the group --CH.sub.2 CH.sub.2 O--,
R.sup.1 is an alkyl group, R.sup.2 is an alkyl group or an alkoxy group, or R.sup.1 and R.sup.2 form together the group --CH.sub.2 CH.sub.2 O--,
R.sup.3 is a hydrogen atom or an alkyl group and n is equal to 0, 1, 2 or 3, ##STR4## in which R.sup.1 and R.sup.3 are as defined hereinbefore and R.sup.4 is an alkyl group, ##STR5## a group of formula: which R and R' together with the nitrogen atom to which they are linked, form the group of formula: ##STR6## in which R.sup.1 and R.sup.5 are identical or different alkyl groups, or in which R.
REFERENCES:
patent: 5288476 (1994-02-01), Pasqualini et al.
patent: 5399339 (1995-03-01), Pasqualini et al.
Bellande Emmanuel
Comazzi Veronique
Laine Jacques
Pasqualini Roberto
Cis Bio International
Dees Jos,e G.
Hartley Michael G.
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