Radioactive transition metal-imido hetero-diphosphine...

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

Reexamination Certificate

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Details

C424S001110, C424S001370, C424S001770

Reexamination Certificate

active

10533988

ABSTRACT:
The present invention provides radioactive metal heterocomplexes of formula (I): [(Me═N—R)L1L2]+Z (I), wherein Me, R, L1L2and Z−have the meanings indicated in the description. The complexes include a trivalent radioactive metal-imido group, typically a technetium- or rhenium-imido group, strongly stabilized by the presence of an ancillary tridentate hetero-diphosphine ligand L1, which allows the formation of substitution-inert [(Me═N—R)L1] moieties. Such moieties are fixed in an intermediate [(Me═N—R)Y2L1)]+compound which contains two labile, cispositioned, Y ligands, where Y is preferably an halide group. The latter are easily replaced by a bidentate ligand L2to give the final [(Me═N—R)L1L2]+Z−heterocomplexes. The complexes of the invention are useful for the preparation of radiopharmaceuticals: in fact, a bioactive fragment which confers biological target-seeking properties can be introduced either on the L2framework or the imido R group.

REFERENCES:
patent: 5589576 (1996-12-01), Archer et al.
patent: 6270745 (2001-08-01), Duatti et al.
patent: 0949265 (1999-10-01), None
patent: WO 91/03262 (1991-03-01), None
PCT International Search Report for PCT/EP03/12128 dated Apr. 15, 2004.
PCT International Preliminary Examination Report for PCT/EP03/12128 dated Jul. 6, 2004.
Arterburn et al. “Functionalized organomidorhenium(V) complexes as potential radiopharmaceuticals: syntheses of glycine derivatives and the structure determination of a rhenium analogue of chlorambucil”Angewandte Chemie. International Edition, vol. 35, No. 23/24, Jan. 3, 1997. (Abstract), incorrect year, no page numbers listed.
Arterburn et al. “Functionalized organomidorhenium(V) complexes as potential radiopharmaceuticals: syntheses of glycine derivatives and the structure determination of a rhenium analogue of chlorambucil” Angewandte Chemie. International Edition, vol. 35, No. 23/24, 1996, pp. 2877-2879.

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