Modified cyanine dyes and conjugates thereof
AssigneeBracco Imaging S.P.A.
InventorsFrancesco BLASI, Chiara BRIOSCHI, Federica BUONSANTI, Luigi MIRAGOLI, Roberta NAPOLITANO, Laura ORIO, Lorena PIZZUTO, Giovanni VALBUSA
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Abstract
The present invention relates to the field of optical imaging. More particularly, it relates to compounds of the cyanine family characterized by improved physico-chemical and biological properties and to their 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.
Claims15
A compound of formula (I)
- wherein
- R1 and R2 are independently a —CO—NH—Y group, wherein Y is selected from a linear or branched alkyl, cycloalkyl and heterocyclyl, substituted by at least two hydroxyl groups;
- R3 is linear or branched alkyl substituted by a group selected from —NH2, —SO3H, —COOH and —CONH2;
- R4 is linear or branched bivalent alkyl;
- R5 is selected from —COO— and —CONH—;
- S is a spacer;
- T is a targeting moiety;
- n is an integer equal to 1, 2 or 3;
- and
- m is an integer equal to 0 or 1,
- or a pharmaceutically acceptable salt thereof.
The compound of formula (I) according to any of the preceding claims, wherein T is targeting moiety selected from the group consisting of a small molecule, a protein, a peptide, a peptidomimetic, an enzyme substrate, an antibody or fragment thereof and an aptamer.
The compound of formula (I) according to any of the preceding claims, wherein T is a moiety interacting with an integrin receptor.
The compound of formula (I) according to any of the preceding claims for use as fluorescence contrast agent for the detection and demarcation of a tumor margin in guided surgery of an individual patient.
Dependencies are inferred from the claim text.