Bracco Imaging S.p.a.

Laura Orio

Federico Crivellin

Federica Buonsanti

Lorena Pizzuto

Roberta Napolitano

Giovanni Valbusa

Andrea Ferraris

Francesco Blasi

Luciano Lattuada

Federico Maisano

Valeria Boi

Sonia Gazzetto

Luigi Miragoli

Aurelia Ferrigato

Chiara Brioschi

Armando Mortillaro

Andrea Barale

Fulvio Ferretti

Daniela Giardina-Papa

The present invention relates to the field of optical imaging. More particularly, it relates to compounds of the cyanine family with near-infrared emission characterized by improved physico-chemical and biological properties and to conjugates with biological ligands thereof. The invention also relates to the use of these compounds as optical diagnostic agents in imaging or therapy of solid tumors, to the methods for their preparation and to the compositions comprising them.

Near-infrared cyanine dyes and conjugates thereof

The present invention relates to the field of optical imaging. More particularly, it relates to compounds of the cyanine family with near-infrared emission characterized by improved physico-chemical and biological properties and to conjugates with biological ligands thereof. The invention also relates to the use of these compounds as optical diagnostic agents in imaging or therapy of solid tumors, to the methods for their preparation and to the compositions comprising them. The compounds have formula (I), formula (I), wherein X is direct bond or —O—; Y is a group selected from linear or branched C1-C6 alkyl, C3-C7 cycloalkyl and heterocyclyl, substituted by at least two hydroxyl groups; R1 and R2 are each independently a linear or branched C1-C6 alkyl substituted by a group selected from —SO3H, —COOH, —CONH2 and —COO—C1-C6 alkyl; and R3 is hydrogen, —SO3H or a linear or branched C1-C6 alkyl substituted by —COOH or —CONH—Y, wherein Y is a group selected from linear or branched C1-C6 alkyl, C3-C7 cycloalkyl and heterocyclyl, substituted by at least two hydroxyl groups.

The application relates to a process for the synthesis of a Near Infra-Red (NIR) fluorescent probe which is a cRGD-Cy5.5 conjugate of formula (I) known as DA364 comprising an aza-bicycloalkane based cyclic peptide labelled with a Cy5.5 dye moiety and used in the guided surgery of tumors and pathologic regions. 

Synthesis of NIR fluorescent probe

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Turin, Italy

Laura Orio