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    Oligonucleotide labeling reactants and their use
    2.
    发明公开
    Oligonucleotide labeling reactants and their use 有权
    寡核苷酸标记反应物及其用途

    公开(公告)号：EP1152010A2

    公开(公告)日：2001-11-07

    申请号：EP01660078.5

    申请日：2001-04-27

    申请人： WALLAC OY

    发明人： Hovinen, Jari ,  Takalo, Harri

    IPC分类号： C07H19/10 ,  C07H19/20 ,  C07H21/00 ,  C07F9/6558

    CPC分类号： C07H19/10 ,  C07F9/582 ,  C07F9/65033 ,  C07F9/65583 ,  C07H19/20 ,  C07H21/00 ,  Y02P20/55

    摘要： The invention relates to a novel labeling reactant of formula (I) suitable for labeling an oligonucleotide
    wherein:

    R is a temporary protecting group. A is either a phosphorylating moiety or a solid support tethered to a bridge point Z via a linker arm E. E' is a linker arm between
    G and Z. G is a bivalent aromatic structure, tethered to two iminodiacetic acid ester groups N(COOR'") 2 or G is a structure selected from a group consisting of

    or
    G is a protected functional group. The invention further concerns a method for direct attachment of a conjugate group to an oligonucleotide structure enabling the attachment of a desired number of these groups during chain assembly. The method comprises a Mitsonobu alkylation.

    摘要翻译： 本发明涉及适于标记寡核苷酸的式（I）的新标记反应物，其中：R是临时保护基。 A是通过连接臂E连接到桥点Z的磷酸化部分或固体支持物.E'是G和Z之间的连接臂.G是连接两个亚氨基二乙酸酯基团N的二价芳族结构（COOR ''）2或G是选自由G组成的组或G是被保护的官能团的结构本发明还涉及用于将缀合物基团直接连接至寡核苷酸结构的方法，使得能够连接所需数量的这些基团 在链组装期间，该方法包括Mitsonobu烷基化。

    Labeling reactants and their use
    3.
    发明公开
    Labeling reactants and their use 有权
    Markierungsreagenzien und deren Verwendung

    公开(公告)号：EP0967205A1

    公开(公告)日：1999-12-29

    申请号：EP99660100.1

    申请日：1999-06-03

    申请人： WALLAC OY

    发明人： Takalo, Harri ,  Hovinen, Jari ,  Mukkala, Veli-Matti ,  Liitti, Päivi ,  Mikola, Heikki

    IPC分类号： C07D213/38 ,  C07D401/14 ,  G01N33/48

    CPC分类号： C07D401/14 ,  C07D213/38 ,  G01N33/533 ,  Y02P20/55

    摘要： The invention relates to a novel labeling reactant, suitable for labeling of a biospecific binding reactant using solid-phase synthesis. The invention further concerns new labeling methods. The novel labeling reactant has the formula (I)
    wherein

    A is a bivalent aromatic structure capable of absorbing light or energy and transferring the excitation energy to a lanthanide ion after the product made by the said solid-phase synthesis has been released from the used solid support, deprotected and converted to a lanthanide chelate;
    R is - Z(G' - NH - X) G" - E, where
    X is a transient protecting group;
    E is a carboxylic acid, its salt, active ester or halide;
    Z is the bridge point;
    G is a bridge between A and Z, G' is a bridge between NH and Z and G" is a bridge between E and Z.
    R' is -COOR''' where R''' is an alkyl of 1 to 4 carbon atoms, phenyl or benzyl.

    摘要翻译： 本发明涉及适用于使用固相合成标记生物特异性结合反应物的新型标记反应物。 本发明还涉及新的标记方法。 新型标记反应物具有式（I）其中A是能够吸收光或能量的二价芳族结构，并且在通过所述固相合成制成的产物已被释放后，将激发能转移到镧系元素离子 使用的固体支持物，去保护并转化成镧系螯合物; R是-Z（G'-NH-X）G“-E，其中X是瞬时保护基; E是羧酸，其盐，活性酯或卤化物; Z是桥点; G是 A和Z，G'是NH和Z之间的桥，G“是E和Z之间的桥.R'是-COOR”，其中R“是1至4个碳原子的烷基，苯基或苄基 。

    Oligonucleotide labeling reactants based on acyclonucleosides and conjugates derived thereof
    5.
    发明公开
    Oligonucleotide labeling reactants based on acyclonucleosides and conjugates derived thereof 有权
    Oligonukleotidmarkierungsreagenzien基于无环核苷，及其衍生的共轭

    公开(公告)号：EP1308452A3

    公开(公告)日：2004-10-27

    申请号：EP02396153.5

    申请日：2002-10-10

    申请人： WALLAC OY

    发明人： Hovinen, Jari

    IPC分类号： C07F9/6512 ,  C07H21/00

    CPC分类号： C07H21/00 ,  C07B2200/11 ,  C07F9/65121 ,  C07F9/65583 ,  Y02P20/55

    摘要： The invention relates to a labeling reactant of formula (I) useful for labeling an oligonucleotide wherein: R is a temporary protecting group. A is either a phosphorylating moiety or a solid support tethered to Z via a linker arm E" . Z is a bridge point and is formed from E is a linker arm between R and Z . E' is a linker arm between Z and Z'. E" is a linker arm between Z and A. E''' is a linker arm between Z' and G. Z' is a purine or pyrimidine base. G is a protected bivalent aromatic structure, tethered to two iminodiacetic acid ester groups N(CH 2 COOR") 2 , or G is a structure selected from the group consisting of or G is a protected functional group, or G is a protected or unprotected organic dye, hapten or a spin label. The invention also relates to a labeling reactant analogous to the one defined above useful for labeling an oligo- or polynucletide using polymerases. The invention further relates to an oligonucleotide or polynucleotide conjugate that can be synthesized using said reactants.

    Oligonucleotide labeling reactants based on acyclonucleosides and conjugates derived thereof
    7.
    发明公开
    Oligonucleotide labeling reactants based on acyclonucleosides and conjugates derived thereof 有权
    Oligonukleotidmarkierungsreagenzien auf der Basis von azyklischen Nukleosiden，und deren derivatisierte Konjugate

    公开(公告)号：EP1308452A2

    公开(公告)日：2003-05-07

    申请号：EP02396153.5

    申请日：2002-10-10

    申请人： WALLAC OY

    发明人： Hovinen, Jari

    IPC分类号： C07F9/6512 ,  C07H21/00

    CPC分类号： C07H21/00 ,  C07B2200/11 ,  C07F9/65121 ,  C07F9/65583 ,  Y02P20/55

    摘要： The invention relates to a labeling reactant of formula (I) useful for labeling an oligonucleotide
    wherein: R is a temporary protecting group. A is either a phosphorylating moiety or a solid support tethered to Z via a linker arm E" . Z is a bridge point and is formed from
    E is a linker arm between R and Z . E' is a linker arm between Z and Z'. E" is a linker arm between Z and A. E''' is a linker arm between Z' and G. Z' is a purine or pyrimidine base. G is a protected bivalent aromatic structure, tethered to two iminodiacetic acid ester groups N(CH 2 COOR") 2 , or G is a structure selected from the group consisting of

    or G is a protected functional group, or G is a protected or unprotected organic dye, hapten or a spin label.
    The invention also relates to a labeling reactant analogous to the one defined above useful for labeling an oligo- or polynucletide using polymerases.
    The invention further relates to an oligonucleotide or polynucleotide conjugate that can be synthesized using said reactants.

    摘要翻译： 本发明涉及可用于标记寡核苷酸的式（I）标记反应物，其中：R为临时保护基。 A是磷酸化部分或通过连接臂E“固定在Z上的固体支持物”Z是桥接点，由形成，E是R和Z之间的连接基团，E'是Z Z'.E“是Z和A之间的连接臂.E”'是Z'和G之间的连接基团.Z'是嘌呤或嘧啶碱基。 G是被保护的二价芳族结构，连接到两个亚氨基二乙酸酯基团N（CH 2 COOR“）2，或G是选自 CHEM>或G是被保护的官能团的结构，或G是 本发明还涉及类似于上述定义的标记反应物，其可用于使用聚合酶标记寡核苷酸或多核苷酸。本发明还涉及可以使用寡核苷酸或多核苷酸缀合物，其可以 使用所述反应物合成。

    Oligonucleotide labeling reactants and their use
    8.
    发明公开
    Oligonucleotide labeling reactants and their use 有权
    Oligonukleotidmarkierungsstoffe及其使用

    公开(公告)号：EP1152010A3

    公开(公告)日：2002-01-02

    申请号：EP01660078.5

    申请日：2001-04-27

    申请人： WALLAC OY

    发明人： Hovinen, Jari ,  Takalo, Harri

    IPC分类号： C07H19/10 ,  C07H19/20 ,  C07H21/00 ,  C07F9/6558 ,  G01N33/53

    CPC分类号： C07H19/10 ,  C07F9/582 ,  C07F9/65033 ,  C07F9/65583 ,  C07H19/20 ,  C07H21/00 ,  Y02P20/55

    摘要： The invention relates to a novel labeling reactant of formula (I) suitable for labeling an oligonucleotide wherein: R is a temporary protecting group. A is either a phosphorylating moiety or a solid support tethered to a bridge point Z via a linker arm E. E' is a linker arm between G and Z. G is a bivalent aromatic structure, tethered to two iminodiacetic acid ester groups N(COOR'")2 or G is a structure selected from a group consisting of or G is a protected functional group. The invention further concerns a method for direct attachment of a conjugate group to an oligonucleotide structure enabling the attachment of a desired number of these groups during chain assembly. The method comprises a Mitsonobu alkylation.