Bracco Imaging S.p.a.

Spiderbiotech S.r.l.

Lorena Pizzuto

Federica Buonsanti

Federico Crivellin

Laura Orio

Roberta Napolitano

Giovanni Valbusa

Andrea Ferraris

Francesco Blasi

Luciano Lattuada

Federico Maisano

Santo Landolfo

Luigi Miragoli

David Lembo

Giorgio Gribaudo

Chiara Brioschi

Andrea Giuliani

Giovanna Pirri

Fulvio Ferretti

Davide Gibellini

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

The present invention relates to monomeric and multimeric peptidic compounds which have antipathogenic, in particular antiviral or/and antibacterial activity. In a preferred aspect, the peptide compounds of the invention have an activity in respect of a broad spectrum of viruses, both DNA and RNA viruses, irrespective of whether they possess virus envelope or not. Further, the present invention refers to compositions comprising said peptidic compounds for medical use, i.e. for the treatment or prevention of pathogenic, in particular viral or/and bacterial infections.

Antipathogenic peptides

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San Francesco al Campo, Italy

Lorena Pizzuto