FLUORESCENTLY LABELED IMMUNOGLOBULIN SINGLE VARIABLE DOMAI NS

    公开(公告)号:WO2023057508A1

    公开(公告)日:2023-04-13

    申请号:PCT/EP2022/077690

    申请日:2022-10-05

    Abstract: The current invention relates to a conjugate comprising an immunoglobulin single variable domain conjugated to one or more detectable labels, wherein at least one of said labels comprises a fluorescent moiety, said fluorescent moiety having a structure chosen from formula (I) or formula (II). The current invention also relates to a conjugate comprising an immunoglobulin single variable domain conjugated to one or more detectable labels, wherein said conjugate exhibits less than 10 percent serum protein binding as measured by HPLC. The invention further relates to a pharmaceutical composition comprising aforementioned conjugate and the use of aforementioned conjugate or composition.

    NEAR-INFRARED CYANINE DYES AND CONJUGATES THEREOF

    公开(公告)号:WO2021259899A1

    公开(公告)日:2021-12-30

    申请号:PCT/EP2021/066920

    申请日:2021-06-22

    Abstract: 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.

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