Bracco Imaging S.p.a.

Nihon Medi-physics Company, Limited

Universitá Degli Studi Di Padova

Università Degli Studi Di Camerino

Marina Porchia

Francesco Tisato

Cristina Bolzati

Fiorenzo Refosco

Valentina Gandin

Cristina Marzano

Shinji Tokunaga

Carlo Santini

Maura Pellei

Giancarlo Gioia Lobbia

Grazia Papini

Stefania Agostini

Mario Cavazza-Ceccato

Cu(I) complexes of the type [Cu(thp)4][X], wherein thp is a tris(hydroxymethyl)phosphine, X is a counteranion, n=1-4, for the use as antineoplistic agents against solid tumors in humans.

[CU(thp)4]n[X]-n compounds for the treatment of a broad range of human solid tumors, including refractory tumors

A bisphosphonoamine compound represented by the following formula (I): wherein R1, R2, R3, R4 and R5 are independently an alkyl group having 1 to 6 carbon atoms, and n is an integer of 1 to 6, is extremely useful as an intermediate for preparing a technetium nitride complex for radiodiagnostic imaging. 

Intermediate compound of technetium nitride complex for radiodiagnostic imaging

The present invention provides radioactive metal heterocomplexes of formula (I): [(Me=N&#x2014;R)LL]+Zwherein Me, R, LLand Zhave 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 L, which allows the formation of substitution-inert [(Me=N&#x2014;R)L] moieties. Such moieties are fixed in an intermediate [(Me=N&#x2014;R)YL)]+ compound which contains two labile, cispositioned, Y ligands, where Y is preferably an halide group. The latter are easily replaced by a bidentate ligand Lto give the final [(Me=N&#x2014;R)LL]+ Zheterocomplexes. 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 Lframework or the imido R group.

Radioactive transition metal-imido hetero-diphosphine complexes, their preparation and radiopharmaceutical compositions thereof

The present invention provides radioactive metal heterocomplexes of formula (I): [(Me&#x2550;N&#x2014;R)LL]+Z (I), wherein Me, R, LLand Zhave 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 L, which allows the formation of substitution-inert [(Me&#x2550;N&#x2014;R)L] moieties. Such moieties are fixed in an intermediate [(Me&#x2550;N&#x2014;R)YL)]compound which contains two labile, cispositioned, Y ligands, where Y is preferably an halide group. The latter are easily replaced by a bidentate ligand Lto give the final [(Me&#x2550;N&#x2014;R)LL]Zheterocomplexes. 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 Lframework or the imido R group.

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Padua, Italy

Marina Porchia