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    Method for preparing oligonucleotides
    42.
    发明申请
    Method for preparing oligonucleotides 审中-公开
    寡核苷酸的制备方法

    公开(公告)号：US20100069623A1

    公开(公告)日：2010-03-18

    申请号：US12417750

    申请日：2009-04-03

    申请人： Ilaria Adamo ,  Cècile Dueymes ,  Andreas Schönberger ,  Jean-Louis Imbach ,  Albert Meyer ,  Francois Morvan ,  Francoise Debart ,  Jean-Jacques Vasseur ,  Meinolf Lange ,  Fritz Link

    发明人： Ilaria Adamo ,  Cècile Dueymes ,  Andreas Schönberger ,  Jean-Louis Imbach ,  Albert Meyer ,  Francois Morvan ,  Francoise Debart ,  Jean-Jacques Vasseur ,  Meinolf Lange ,  Fritz Link

    IPC分类号： C07H21/04

    CPC分类号： C07H21/00 ,  C07H21/02 ,  C07H21/04 ,  Y02P20/55 ,  Y02P20/582

    摘要： A solution phase synthesis method for preparing an oligonucleotide, wherein at least some of the reagents are solid supported. The method suitable for large-scale synthesis comprises coupling a protected compound with a nucleotide derivative having a protection group in the presence of a solid supported activator to give an elongated oligonucleotide with a P(III)-internucleotide bond; optionally processing the elongated oligonucleotide by capping by reaction with a solid supported capping agent and/or by oxidizing or sulfurizing by reaction of the oligonucleotide with a solid supported oxidizing or sulfurization reagent; and removing the protection group. The coupling may include reacting a 3′-protected compound of formula: with a nucleotide derivative having a 5′-protection group, or reacting a 5′-protected compound of formula with a nucleotide derivative having a 3′-protection group.

    摘要翻译： 一种制备寡核苷酸的溶液相合成方法，其中至少一些试剂是固体负载的。 适用于大规模合成的方法包括在保持固体的活化剂存在下将受保护的化合物与具有保护基团的核苷酸衍生物偶联，得到具有P（III） - 核苷酸键的细长寡核苷酸; 任选地通过与固体支持的封端剂反应进行加帽和/或通过寡核苷酸与固体支持的氧化或硫化试剂的反应进行氧化或硫化来加工细长的寡核苷酸; 并移除保护组。 偶联可以包括使下式的3'-保护的化合物与具有5'-保护基团的核苷酸衍生物反应，或使5受保护的式的化合物与具有3'-保护基团的核苷酸衍生物反应。

    Nitrosoureas compounds preparation thereof and utilization thereof in anticancerous
    44.
    发明授权
    Nitrosoureas compounds preparation thereof and utilization thereof in anticancerous 失效
    硝基脲类化合物的制备及其在抗癌中的应用

    公开(公告)号：US5001158A

    公开(公告)日：1991-03-19

    申请号：US462335

    申请日：1990-01-02

    申请人： Jean-Claude Madelmont ,  Denise Godeneche ,  Marie-France Moreau ,  Daniel Parry ,  Gustin Meyniel ,  Joel Oiry ,  Jean-Louis Imbach

    发明人： Jean-Claude Madelmont ,  Denise Godeneche ,  Marie-France Moreau ,  Daniel Parry ,  Gustin Meyniel ,  Joel Oiry ,  Jean-Louis Imbach

    IPC分类号： A61K31/17

    CPC分类号： A61K31/17

    摘要： Compounds having the general formula (I), ##STR1## wherein X and Y represent individually H or --NO, at least one of them being a group-NO, n is 0, 1 or 2, R represents hydrogen, an aliphatic, cycloaliphatic, cycloaliphatic-alkyl, aryl or aralkyl radical, or a group of formula, ##STR2## wherein R.sub.1 is a lower alkyl radical or an aryl, all these radicals being optionally substituted. The present invention also relates to the compounds hereabove defined in the form of mixtures of their position isomers. Furthermore, the present invention discloses processes for preparing such compounds, as well as compositions, useful particularly in anticancerous chemotherapy, containing at least one of said compounds as an active principle.

    摘要翻译： 具有通式（I）的化合物，其中X和Y独立地表示H或-NO，它们中的至少一个为基团，n为0,1或2，R为氢，脂族，脂环族 ，脂环族 - 烷基，芳基或芳烷基，或下式的基团，其中R 1是低级烷基或芳基，所有这些基团都是任选取代的。 本发明还涉及以其位置异构体的混合物形式定义的上述化合物。 此外，本发明公开了制备这样的化合物的方法，以及特别用于抗癌化疗的组合物，其含有至少一种所述化合物作为活性成分。

    Method for preparing oligonucleotides
    46.
    发明授权
    Method for preparing oligonucleotides 失效
    寡核苷酸的制备方法

    公开(公告)号：US08304532B2

    公开(公告)日：2012-11-06

    申请号：US13115845

    申请日：2011-05-25

    申请人： Ilaria Adamo ,  Cecile Dueymes ,  Andreas Schonberger ,  Jean-Louis Imbach ,  Albert Meyer ,  Francois Morvan ,  Francoise Debart ,  Jean-Jacques Vasseur ,  Meinolf Lange ,  Fritz Link

    发明人： Ilaria Adamo ,  Cecile Dueymes ,  Andreas Schonberger ,  Jean-Louis Imbach ,  Albert Meyer ,  Francois Morvan ,  Francoise Debart ,  Jean-Jacques Vasseur ,  Meinolf Lange ,  Fritz Link

    IPC分类号： C07H21/00

    CPC分类号： C07H21/00 ,  C07H21/02 ,  C07H21/04 ,  Y02P20/55 ,  Y02P20/582

    摘要： A solution phase synthesis method for preparing an oligonucleotide, wherein at least some of the reagents are solid supported. The method suitable for large-scale synthesis comprises coupling a protected compound with a nucleotide derivative having a protection group in the presence of a solid supported activator to give an elongated oligonucleotide with a P(III)-internucleotide bond; optionally processing the elongated oligonucleotide by capping by reaction with a solid supported capping agent and/or by oxidizing or sulfurizing by reaction of the oligonucleotide with a solid supported oxidizing or sulfurization reagent; and removing the protection group. The coupling may include reacting a 3′-protected compound of formula: with a nucleotide derivative having a 5′-protection group, or reacting a 5′-protected compound of formula with a nucleotide derivative having a 3′-protection group.

    摘要翻译： 一种制备寡核苷酸的溶液相合成方法，其中至少一些试剂是固体负载的。 适用于大规模合成的方法包括在保持固体的活化剂存在下将受保护的化合物与具有保护基团的核苷酸衍生物偶联，得到具有P（III） - 核苷酸键的细长寡核苷酸; 任选地通过与固体支持的封端剂反应进行加帽和/或通过寡核苷酸与固体支持的氧化或硫化试剂的反应进行氧化或硫化来加工细长的寡核苷酸; 并移除保护组。 偶联可以包括使下式的3'-保护的化合物与具有5'-保护基团的核苷酸衍生物反应，或使5受保护的式的化合物与具有3'-保护基团的核苷酸衍生物反应。

    Method for preparing oligonucleotides
    50.
    发明申请
    Method for preparing oligonucleotides 审中-公开
    寡核苷酸的制备方法

    公开(公告)号：US20060089494A1

    公开(公告)日：2006-04-27

    申请号：US10522854

    申请日：2003-07-30

    申请人： Ilaria Adamo ,  Cecile Dueymes ,  Andreas Schonberger ,  Jean-Louis Imbach ,  Albert Meyer ,  Francois Morvan ,  Francoise Debart ,  Jean-Jacques Vasseur ,  Meinolf Lange ,  Fritz Link

    发明人： Ilaria Adamo ,  Cecile Dueymes ,  Andreas Schonberger ,  Jean-Louis Imbach ,  Albert Meyer ,  Francois Morvan ,  Francoise Debart ,  Jean-Jacques Vasseur ,  Meinolf Lange ,  Fritz Link

    IPC分类号： C07H21/02 ,  C07H21/04

    CPC分类号： C07H21/00 ,  C07H21/02 ,  C07H21/04 ,  Y02P20/55 ,  Y02P20/582

    摘要： A method for preparing an oligonucleotide comprising the steps of a) providing a 3-protected compound having the formula: wherein B is a heterocyclic base R2 is H, a protected 2-hydroxyl group, F, a protected amino group, an O-alkyl group, an O-substituted alkyl, a substituted alkylamino or a C4′-O2′methylen linkage R3 is OR′3, NHR″3, NR″3R′″3, a 3′-protected nucleotide or a 3′-protected oligonucleotide, R′3 is a hydroxyl protecting group, R″3, R′″3 are independently an amine protecting group, b) reacting said compound with a nucleotide derivative having a 5-proctection group in the presence of a solid supported activator to give an elongated oligonucleotide with a P(III)-internucleotide bond c) optionally processing the elongated oligonucleotide with a P(III)-internucleotide bond by either or both of steps c1) and c2) in any sequence c1) capping preferably by reacting with a solid supported capping agent c2) oxidizing preferably by reacting the oligonucleotide with a solid supported oxidizing reagent d) removing the 5′-protection group.

    摘要翻译： 一种制备寡核苷酸的方法，包括以下步骤：a）提供具有下式的3-保护的化合物：其中B是杂环基R2是H，被保护的2-羟基，F，保护的氨基，O-烷基 基团，O-取代的烷基，取代的烷基氨基或C4'-O2'亚甲基键R3是OR'3，NHR'3，NR'3R“'，3'-保护的核苷酸或3' R'3是羟基保护基，R“3”，“3”独立地是胺保护基，b）使所述化合物与具有5-取代基的核苷酸衍生物在 c）通过任何序列c1）和c2）中任一或两个步骤c1）和c2）任选地用P（III） - 核苷酸键处理细长寡核苷酸 优选通过与固体支持的封端剂c2反应，优选通过使寡核苷酸与固体支持物反应来进行氧化 d）除去5'-保护基。