Bracco Imaging S.p.a.

Nihon Medi-physics Company, Limited

De Filippis, Vincenzo

Palmieri, Angelo Michele

Refosco, Fiorenzo

Garaci, Enrico

Pazzagli, Mario

Ziche, Marina

Squeo, Maria

Montemurno, Concetta Antonia

Granito, Mario Leonardo

Stanisci, Francesco

Fiorenzo Refosco

Alessandro Maiocchi

Enrico Garaci

Cristina Bolzati

Francesco Tisato

Marina Porchia

Adriano Duatti

Licia Uccelli

Simona Ghiani

Shinji Tokunaga

Alessandra Boschi

Barbara Spolaore

Stefania Agostini

Nicola Salvarese

Mario Cavazza-Ceccato

Marina Ziche

Vincenzo De Filippis

Francesco Stanisci

Mario Leonardo Granito

Mario Pazzagli

Maria Squeo

Concetta Antonia Montemurno

Angelo Michele Palmieri

The present invention relates to a labeling procedure for the incorporation, in mild reaction conditions, of sensitive and thermosensitive targeting molecules into a [99m Tc(N)(PNP)]-based compound suitable for a kit formulation.

Method for labeling of sensitive and thermosensitive targeting biomolecules with technetium based compounds

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

A radiopharmaceutical for diagnostic imaging containing as an active ingredient a technetium-99m nitride heterocomplex comprising technetium-99m nitride and two different ligands coordinated therewith, i.e., a bisphosphinoamine compound as a &#x3c0; electron acceptor and a bidentate ligand as a &#x3c0; electron donor and represented by the following formula (I): [Tc(N)(PNP)(XY)](I)whereinTc(N) is technetium-99m nitride, PNP is a bisphosphinoamine compound and XY is a bidentate ligand, is markedly accumulated in heart and adrenal glands and hence is useful for radiodiagnostic imaging of heart and adrenal glands.

Radiopharmaceutical for diagnostic imaging containing a technetium-99m nitride heterocomplex

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.

Radioactive transition metal nitride heterocomplex

Growing community of inventors

Valdagno, Italy

Fiorenzo Refosco