Bracco Imaging S.p.a.

Valeria Boi

Luciano Lattuada

Roberta Napolitano

Giovanni Battista Giovenzana

Sonia Gazzetto

Silvio Aime

Massimo Visigalli

Alberto Fringuello Mingo

Pier Lucio Anelli

Maria Argese

Laura Galimberti

Livio Cavalieri

Fulvia Vella

Andrea Banin

Andrea Barale

Federico Maisano

Federica Buonsanti

Laura Orio

Giovanni Rivolta

Aurelia Ferrigato

Armando Mortillaro

Livio Cavaliere

Daniela Giardina-Papa

The invention relates to a process for the preparation of the gadolinium dimeric contrast agent [p-[1-[bis[2-(hydroxy-KO)-3-[4,7,10-tris[(carboxy-KO)methyl]-1,4,7,10-tetraazacyclododec-1-yl-K/V1,K/V4,K/V7,K/V10]propyl]amino]-1-deoxy-D-glucitolato(6-)]]di-gadolinium complex. Such process includes preparation steps carried out one-pot and without isolation of the obtained intermediates. The gadolinium dimeric contrast agent can be for use in diagnostic imaging, in particular in Magnetic resonance Imaging (MRI).

Manufacturing of dimeric contrast agent

The invention relates to a process for the preparation of dimeric contrast agents for use in Magnetic resonance Imaging (MRI), in particular [μ-[1-[bis[2-(hydroxy-κO)-3-[4,7,10-tris[(carboxy-κO)methyl]-1,4,7,10-tetraazacyclododec-1-yl-κN,κN,κN,κN]propyl]amino]-1-deoxy-D-glucitolate(6-)]]di-gadolinium complex, which includes preparation steps carried out one-pot (without isolation of the obtained intermediate) and precipitation of at least part of free gadolinium metal ions in excess.

Manufacturing of dimeric contrast agents

The present invention relates to new class of dimeric macrocycles capable of chelating paramagnetic metal ions, their chelated complexes with metal ions and the use thereof as contrast agents, particularly suitable for Magnetic Resonance Imaging (MRI) analysis.

Dimeric contrast agents

The present invention relates to new class of functionalized macrocycles capable of chelating paramagnetic metal ions, their chelated complexes with metal ions and the use thereof as contrast agents, particularly suitable for Magnetic Resonance Imaging (MRI) analysis.

Contrast agents

The present invention relates to new class of functionalized polyazamacrocycles including at least one phosphonic or phosphinic group linked to a nitrogen atom of the macrocyclic cage, and capable of chelating paramagnetic metal ions, their chelated complexes with metal ions and the use thereof as contrast agents, particularly suitable for Magnetic Resonance Imaging (MRI) analysis.

The present invention relates to new class of dimeric macrocycles capable of chelating paramagnetic metal ions, their chelated complexes with the paramagnetic metal ions and the use thereof as contrast agents, particularly suitable for Magnetic Resonance Imaging (MRI) analysis.

The present invention relates to a process for the preparation of the mono sodium salt of the derivative 3,5-diiodo-O-[3-iodo-4-(sulphooxy)phenyl]-L-tyrosine (T3S) by starting from the corresponding phenolic compound, in the presence of chlorosulfonic acid and dimethylacetamide as a solvent. The so obtained T3S compound may conveniently be isolated in a pure form as a solid in good yields. The present invention further relates to the process for T3S preparation, wherein the starting reagent is T2 and further comprising the formulation of such compound in tablets. Furthermore, the invention discloses non-radioactive immunoassays based on T3S derivatives.

Process for the preparation of a sulfated derivative of 3,5-diiodo-o-[3-iodophenyl]-l-tyrosine

The present invention relates to a process for the preparation of the mono sodium salt of the derivative 3,5-diiodo-O-[3-iodo-4-(sulphooxy)phenyl]-L-tyrosine (T3S) by starting from the corresponding phenolic compound, in the presence of chloro-sulfonic acid and dimethylacetamide as a solvent. The so obtained T3S compound may conveniently be isolated in a pure form as a solid in good yields. The present invention further relates to the process for T3S preparation, wherein the starting reagent is T2 and further comprising the formulation of such compound in tablets. Furthermore, the invention discloses non-radioactive immunoassays based on T3S derivatives.

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Strambino, Italy

Valeria Boi