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    Galactopyranosyl derivatives useful as medicaments
    75.
    发明授权
    Galactopyranosyl derivatives useful as medicaments 有权
    用作药物的吡喃半乳糖衍生物

    公开(公告)号：US09321796B2

    公开(公告)日：2016-04-26

    申请号：US14411413

    申请日：2013-06-20

    Applicant: Universiteit Gent

    Inventor： Dirk Elewaut ,  Nora Pauwels ,  Sandrine Aspeslagh ,  Serge Van Calenbergh

    IPC: C07H15/26 ,  C07H15/04 ,  C07H15/18

    CPC classification number: C07H15/26 ,  C07H15/04 ,  C07H15/18

    Abstract: This invention relates to carbamate-containing or thiocarbamate-containing galacto-pyranosyl compounds useful as therapeutic agents and being represented by the structural formula (II), wherein: X is O or S, R is selected from the group consisting of C1-8 alkyl, C3-10 cycloalkyl, aryl-C1-4 alkyl, heterocyclyl-C1-4 alkyl, cycloalkyl-C1-4 alkyl, aryl and heterocyclyl, wherein R is optionally substituted with one or more R9; R2, R3, R4, R6 and R7 are independently selected from the group consisting of hydroxyl and protected hydroxyl groups; R5 is selected from the group consisting C6-30 alkyl and arylalkyl; R8 is C6-30 alkyl; and each R9 is independently selected from the group consisting of halogen, hydroxy, trifluoromethyl, trifluoromethoxy, C1-8alkoxy, C1-6 alkyl, cyano, methylthio, phenyl, phenoxy, chloromethyl, dichloromethyl, chloro-difluoromethyl, acetyl, nitro, benzyl, heterocyclyl and di-C1-4 alkyl-amino, or a pharmaceutically acceptable salt thereof.

    Abstract translation: 本发明涉及可用作治疗剂并由结构式（II）表示的含氨基甲酸酯或含硫代氨基甲酸酯的半乳糖吡喃糖基化合物，其中：X为O或S，R选自C 1-8烷基 ，C 3-10环烷基，芳基-C 1-4烷基，杂环基-C 1-4烷基，环烷基-C 1-4烷基，芳基和杂环基，其中R任选被一个或多个R 9取代; R2，R3，R4，R6和R7独立地选自羟基和保护的羟基; R5选自C6-30烷基和芳基烷基; R8为C6-30烷基; 苯基，苯氧基，氯甲基，二氯甲基，氯代 - 二氟甲基，乙酰基，硝基，苄基，环己基，环己基， 杂环基和二-C 1-4烷基 - 氨基，或其药学上可接受的盐。

    GLYCOSIDE DERIVATIVES, PREPARATION THEREOF AND USE THEREOF AS PROSTHETIC GROUPS
    77.
    发明申请
    GLYCOSIDE DERIVATIVES, PREPARATION THEREOF AND USE THEREOF AS PROSTHETIC GROUPS 审中-公开
    甘氨酸衍生物，其制备及其作为前体组合使用

    公开(公告)号：US20160031923A1

    公开(公告)日：2016-02-04

    申请号：US14412161

    申请日：2013-07-02

    Applicant: UNIVERSITÉ DE LORRAINE ,  CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE - CNRS

    Inventor： YVES CHAPLEUR ,  Sandrine LAMANDE ,  Charlotte COLLET ,  Françoise CHRETIEN

    IPC: C07H15/04

    CPC classification number: C07H15/04 ,  C07B59/005 ,  C07H15/26

    Abstract: The present invention relates to glycoside-derived compounds, to the processes for preparing same and to the use thereof as prosthetic groups for radiolabelling biomolecules. These compounds are co-azido-alkyl 6-deoxy-6-[18F]-fluoroglycosides of formula (I), in which: k is equal to 2 or 3; n is an integer between 1 and 5; R is independently H or a C1-C5 alkyl group, m being an integer between 0 and 2 if k=2 and m between 0 and 3 if k=3; and X is chosen from the group comprising O, S, CH2 and NR′, in which R′ is independently a C1-C5 alkyl group or an aryl group, including all the stereoisomers thereof.

    Abstract translation: 本发明涉及糖苷衍生的化合物，其制备方法及其作为放射性标记生物分子的假基团的用途。 这些化合物是式（I）的叠氮基 - 烷基6-脱氧-6- [18 F] - 氟代糖苷，其中：k等于2或3; n是1和5之间的整数; R独立地为H或C1-C5烷基，如果k = 2，则m为0至2之间的整数，如果k = 3，则m为0至3之间的m; X选自O，S，CH 2和NR'的基团，其中R'独立地是C 1 -C 5烷基或芳基，包括其所有的立体异构体。

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