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    NEAR-INFRARED CYANINE DYES AND CONJUGATES THEREOF
    4.
    发明公开
    NEAR-INFRARED CYANINE DYES AND CONJUGATES THEREOF 审中-公开

    公开(公告)号：US20230312523A1

    公开(公告)日：2023-10-05

    申请号：US18010905

    申请日：2021-06-22

    Applicant: BRACCO IMAGING S.P.A.

    Inventor： Francesco BLASI ,  Federica BUONSANTI ,  Federico CRIVELLIN ,  Andrea FERRARIS ,  Laura ORIO ,  Lorena PIZZUTO ,  Roberta NAPOLITANO ,  Giovanni VALBUSA

    IPC: C07D403/10 ,  C07D403/14 ,  C09B23/01

    CPC classification number: C07D403/10 ,  C07D403/14 ,  C09B23/0066

    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.

    PROCESS FOR THE PREPARATION OF IOPAMIDOL
    10.
    发明申请
    PROCESS FOR THE PREPARATION OF IOPAMIDOL 审中-公开

    公开(公告)号：US20190077745A1

    公开(公告)日：2019-03-14

    申请号：US16052695

    申请日：2018-08-02

    Applicant: BRACCO IMAGING S.P.A.

    Inventor： Elisa BATTISTINI ,  Federica BUONSANTI ,  Daniela IMPERIO ,  Luciano LATTUADA ,  Roberta NAPOLITANO

    IPC: C07C231/14 ,  C07C231/02 ,  C07F5/04 ,  C07F5/05 ,  C07F5/02 ,  C07C201/12 ,  C07C227/04 ,  C07C231/12 ,  C07C237/46

    Abstract: The present invention discloses a process for the preparation of Iopamidol of formula (II) and comprising the following steps: a) reacting the Compound (I) wherein X is OR2 or R3, and wherein R2 and R3 are a C1-C6 linear or branched alkyl, C3-C6 cycloalkyl, C6 aryl, optionally substituted with a group selected from the group consisting of methyl, ethyl, n-propyl, i-propyl, n-butyl, sec-butyl, t-butyl and phenyl, with the acylating agent (S)-2-(acetyloxy)propanoyl chloride in a reaction medium to provide the acetyloxy derivative of Compound (I); b) hydrolyzing the intermediate from step a) with an aqueous solution at a pH comprised from 0 to 7, by adding water or a diluted alkaline solution such as sodium hydroxide or potassium hydroxide, freeing the hydroxyls from the boron-containing protective groups, obtaining the N-(S)-2-(acetyloxy)propanoyl derivative of Compound (II); c) alkaline hydrolysis to restore the (S)-2-(hydroxy)propanoyl group and to obtain Iopamidol (II) and optional recovery of the boron derivative from the solution obtained in step b). The boron-containing protective group is versatile, efficient and recyclable. A one-pot synthesis, without intermediate isolation is provided, leading to a decreasing of recovered and recycled solvents and a significant increasing in the yield, representing a significant advantage in terms of cost-effectiveness of the entire process and environmental awareness.

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