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    PHARMACEUTICAL COMPOSITION
    1.
    发明公开
    PHARMACEUTICAL COMPOSITION 有权
    药物组合物

    公开(公告)号：EP2156832A1

    公开(公告)日：2010-02-24

    申请号：EP08751561.5

    申请日：2008-04-16

    申请人： Pola Pharma Inc.

    发明人： MURAKAMI, Yasushi ,  KOBAYASHI, Naoko ,  NISHIO, Azuma ,  KUBOTA, Nobuo

    IPC分类号： A61K31/4168 ,  A61K47/22 ,  A61P35/00 ,  C07D233/91

    CPC分类号： A61K9/08 ,  A61K9/0019 ,  A61K31/4168 ,  A61K41/0038 ,  C07D233/91

    摘要： To provide a pharmaceutical composition containing a 2-nitroimidazole derivative, which has high solubility in an aqueous carrier and high stability.
    The pharmaceutical composition is characterized by containing 1-(1-hydroxymethyl-2,3-dihydroxypropyl)oxymethyl-2-nitroimidazole and creatinine, and containing creatinine of 0.001 to 1 part by mass with respect to 1 part by mass of 1-(1-hydroxymethyl-2,3-dihydroxypropyl)oxymethyl-2-nitroimidazole .

    摘要翻译： 提供含有2-硝基咪唑衍生物的药物组合物，其在水性载体中具有高溶解度和高稳定性。 该药物组合物的特征在于含有1-（1-羟基甲基-2,3-二羟基丙基）氧甲基-2-硝基咪唑和肌酸酐，并且相对于1质量份的1-（1）质量含有0.001-1质量份的肌酸酐 - 羟甲基-2,3-二羟丙基）氧甲基-2-硝基咪唑。

    METHOD FOR PRODUCING 2-NITROIMIDAZOLE DERIVATIVE
    2.
    发明授权
    METHOD FOR PRODUCING 2-NITROIMIDAZOLE DERIVATIVE 有权
    用于生产2-硝基咪唑衍生物

    公开(公告)号：EP2128140B1

    公开(公告)日：2012-03-14

    申请号：EP08702779.3

    申请日：2008-01-17

    申请人： Pola Pharma Inc.

    发明人： NISHIO, Azuma

    IPC分类号： C07D233/91 ,  A61K51/00

    CPC分类号： C07D233/91 ,  A61K51/0453

    摘要： Disclosed is a method for producing a 2-nitroimidazole derivative having an acyclic sugar chain in a side chain which is suitable for production of a derivative having a radioisotope. Specifically disclosed is a method for producing 1-(1- benzoyloxymethyl-2-hydroxyethyl)oxymethyl-2-nitroimidazole, which is characterized in that 1-O-benzoylglycerin is obtained by reacting glycerin with a benzoylating agent, then 4-benzoyloxymethyl-1,3-dioxolane is obtained by reacting 1-O-benzoylglycerin with dimethoxymethane in the presence of a dehydrating agent, and then 4-benzoyloxymethyl-1,3-dioxolane is reacted with 2-nitroimidazole or 2-nitro-1-trialkylsilylimidazole in the presence of a Lewis acid.

    METHOD FOR PRODUCING 2-NITROIMIDAZOLE DERIVATIVE
    6.
    发明公开
    METHOD FOR PRODUCING 2-NITROIMIDAZOLE DERIVATIVE 有权
    VERFAHREN ZUR HERSTELLUNG EINES 2-NITROIMIDAZOL-DERIVATS

    公开(公告)号：EP2128140A1

    公开(公告)日：2009-12-02

    申请号：EP08702779.3

    申请日：2008-01-17

    申请人： Pola Pharma Inc.

    发明人： NISHIO, Azuma

    IPC分类号： C07D233/91 ,  A61K51/00 ,  C07D317/24

    CPC分类号： C07D233/91 ,  A61K51/0453

    摘要： Disclosed is a method for producing a 2-nitroimidazole derivative having an acyclic sugar chain in a side chain which is suitable for production of a derivative having a radioisotope. Specifically disclosed is a method for producing 1-(1- benzoyloxymethyl-2-hydroxyethyl)oxymethyl-2-nitroimidazole, which is characterized in that 1-O-benzoylglycerin is obtained by reacting glycerin with a benzoylating agent, then 4-benzoyloxymethyl-1,3-dioxolane is obtained by reacting 1-O-benzoylglycerin with dimethoxymethane in the presence of a dehydrating agent, and then 4-benzoyloxymethyl-1,3-dioxolane is reacted with 2-nitroimidazole or 2-nitro-1-trialkylsilylimidazole in the presence of a Lewis acid.

    摘要翻译： 公开了一种制备具有侧链中具有无环糖链的2-硝基咪唑衍生物的方法，该方法适于制备具有放射性同位素的衍生物。 具体公开了1-（1-苯甲酰氧基甲基-2-羟乙基）氧基甲基-2-硝基咪唑的制造方法，其特征在于，通过使甘油与苯甲酰化试剂反应得到1-O-苯甲酰甘油，然后将4-苯甲酰氧基甲基-1 通过在脱水剂存在下使1-O-苯甲酰甘油与二甲氧基甲烷反应获得3-二氧戊环，然后使4-苯甲酰氧基甲基-1,3-二氧戊环与2-硝基咪唑或2-硝基-1-三烷基甲硅烷基咪唑在 存在路易斯酸。