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1954 条记录 (耗时 0.044 秒)

    5-Fluoruoracil Derivatives
    69.
    发明公开
    5-Fluoruoracil Derivatives 审中-公开
    5-氟尿嘧啶 - 衍生物

    公开(公告)号：EP2712868A1

    公开(公告)日：2014-04-02

    申请号：EP12186564.6

    申请日：2012-09-28

    申请人： B. Braun Melsungen AG

    发明人： Rosemeyer, Helmut ,  Malecki, Edith

    IPC分类号： C07H19/06 ,  A61K31/7072 ,  A61P35/00

    CPC分类号： C07H19/06

    摘要： The present invention relates to a compound represented by formula (I)

    wherein X is selected from the group of formulae (II) to (IV)



    wherein
    R 1 is H or C 1 -C 50 chain which may be branched or linear and which may be saturated or unsaturated and which may optionally be interrupted and/or substituted by one or more hetero atom(s) (Het1) and/or functional group(s)(G1); or
    R 1 is a C 3 -C 28 moiety which comprises at least one cyclic structure and which may be saturated or unsaturated and which may optionally be interrupted and/or substituted by one or more hetero atom(s) (Het1) and functional group(s)(G1);
    R 2 is H; or
    R 2 is a Mono-phosphate, Di-phosphate, Tri-phosphate or phosphoramidite moiety; or
    R 2 is -Y-X or -Y-L-Y 1 - X;
    Y and Y 1 are independently from each other a single bond or a functional connecting moiety,
    X is a colloid-active compound (CA) or a fluorescence marker (FA) or a polynucleotide moiety having up to 50 nucleotide residues, preferably 10 to 25 nucleotides, especially a polynucleotide having an antisense or antigen effect;
    L is a linker by means of which Y and X are covalently linked together;
    R 3 and R 4 represent independently from each other a C 1 -C 28 -alkyl moiety which may optionally be substituted or interrupted by one or more heteroatom(s) and/or functional group(s);or
    R 3 and R 4 form a ring having at least 5 members, preferably a ring having 5 to 8 carbon atoms and wherein the ring may be substituted or interrupted by one or more hetero atom(s) and/or functional group(s); or
    R 3 and R 4 represent independently from each other a C 1 -C 28 -alkyl moiety substituted with one or more moieties selected from the group -Y-X or -Y-L-Y 1 -X; or
    R 3 and R 4 represent independently from each other -Y-X or -Y-L-Y 1 - X;
    R 5 and R 6 represent independently from each other a C 1 -C 28 -alkyl moiety which may optionally be substituted or interrupted by one or more heteroatom(s) and/or functional group(s); or
    R 5 and R 6 represent independently from each other a C 1 -C 28 -alkyl moiety substituted with one or more moieties selected from the group -Y-X or -Y-L-Y 1 -X; or
    R 5 and R 6 form a ring having at least 5 members, preferably a ring having 5 to 18 carbon atoms and wherein the ring may be substituted or interrupted by one or more hetero atom(s) and/or functional group(s);
    and/or one or more moieties selected from the group -Y-X or -Y-L-Y 1 - X;
    R 5 and R 6 represent independently from each other -Y-X or -Y-L-Y 1 - X;
    R 7 is a hydrogen atom or -O-R 8 ;
    R 8 is H or C 1 -C 28 chain which may be branched or linear and which may be saturated or unsaturated and which may optionally be interrupted and/or substituted by one or more hetero atom(s) (Het1) and/or functional group(s)(G1); or
    R 8 is -Y-X or -Y-L-Y 1 - X,
    with the proviso that R 1 and R 2 are not both H and/or
    with the proviso that the compound comprises at least two chains each of which having 4 or more carbon atoms.

    摘要翻译： 本发明涉及由式（I）表示的化合物，其中X选自式（II）至（IV）的基团，其中R 1为H或可以是支链或直链的C 1 -C 50链， 是饱和或不饱和的，并且其可以任选被一个或多个杂原子（Het1）和/或官能团（G1）中断和/或取代; 或R 1是C 3 -C 28部分，其包含至少一个环状结构，并且其可以是饱和或不饱和的，并且其可任选地被一个或多个杂原子（Het1）和官能团中断和/或取代 （一个或多个）（G1）; R 2为H; 或R 2是单磷酸盐，二磷酸盐，三磷酸盐或亚磷酰胺部分; 或R 2为-Y-X或-Y-L-Y 1-X; Y和Y 1彼此独立地是单键或功能连接部分，X是胶体活性化合物（CA）或荧光标记（FA）或具有多达50个核苷酸残基，优选10至25个的多核苷酸部分 核苷酸，特别是具有反义或抗原作用的多核苷酸; L是通过Y和X共价连接在一起的接头; R 3和R 4彼此独立地表示可任选被一个或多个杂原子和/或官能团取代或中断的C 1 -C 28 - 烷基部分;或R 3和R 4形式 具有至少5个成员的环，优选具有5至8个碳原子的环，并且其中所述环可以被一个或多个杂原子和/或官能团取代或间隔; 或R 3和R 4彼此独立地表示被一个或多个选自-Y-X或-Y-L-Y 1 -X的部分取代的C 1 -C 28烷基部分; 或R 3和R 4彼此独立地表示-Y-X或-Y-L-Y 1-X; R 5和R 6彼此独立地表示可任选地被一个或多个杂原子和/或官能团取代或间隔的C 1 -C 28 - 烷基部分; 或R 5和R 6彼此独立地表示被一个或多个选自-Y-X或-Y-L-Y 1 -X的部分取代的C 1 -C 28烷基部分; 或R 5和R 6形成具有至少5个成员，优选具有5至18个碳原子的环的环，并且其中该环可以被一个或多个杂原子和/或官能团取代或中断， ; 和/或选自-Y-X或-Y-L-Y 1-X的一个或多个部分; R 5和R 6彼此独立地表示-Y-X或-Y-L-Y 1-X; R 7是氢原子或-O-R 8; R 8是H或C 1 -C 28链，其可以是支链或直链的，并且其可以是饱和或不饱和的，并且其可以任选地被一个或多个杂原子（Het1）和/或官能 组（一个或多个）（G1）; 或R 8为-Y-X或-Y-L-Y 1-X，条件是R 1和R 2不同时为H和/或条件是该化合物包含至少两个具有4个或更多个碳原子的链。