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    NOVEL BENZAMIDINE DERIVATIVES HAVING ANTI-INFLAMMATORY AND IMMUNOSUPPRESSIVE ACTIVITY
    22.
    发明公开
    NOVEL BENZAMIDINE DERIVATIVES HAVING ANTI-INFLAMMATORY AND IMMUNOSUPPRESSIVE ACTIVITY 有权
    BENZAMIDINDERIVATE MITENTZÜNDUNGSHEMMENDERUND IMMUNSUPPRESSIVER WIRKUNG

    公开(公告)号：EP1363875A2

    公开(公告)日：2003-11-26

    申请号：EP02718096.7

    申请日：2002-02-06

    申请人： ROTTA RESEARCH LABORATORIUM S.P.A.

    发明人： MAKOVEC, Francesco ,  ZANZOLA, Simona ,  ARTUSI, Roberto ,  ROVATI, Lucio, Claudio

    IPC分类号： C07C279/36 ,  A61K31/155 ,  A61P35/00 ,  C07D213/40 ,  C07C335/20 ,  C07C257/14 ,  C07C279/18 ,  C07D209/42 ,  C07D209/18

    CPC分类号： C07D213/40 ,  C07C257/14 ,  C07C279/18 ,  C07C279/36 ,  C07C335/20 ,  C07C2601/14 ,  C07C2603/74 ,  C07D209/14 ,  C07D209/40 ,  C07D277/48

    摘要： Compounds which can be represented by the general formula (I) and in which A is selected independently from the carboxamide group, the thiocarboxamide group, and the carbonyl group, -R1 is selected from an alkyl group having from 1 to 3 carbon atoms and the amino group, unsubstituted or substituted with the nitro group or the methyl group, -R2 is selected independently from hydrogen, an alkyl group having from 1 to 4 carbon atoms, the methoxy, ethoxy, propoxy group, a mono-, bi- or tricyclic cycloalkane residue having from 5 to 12 carbon atoms, the adamantyl group, an aryl, naphthyl or heterocyclic group, unsubstituted or substituted with methyl, methoxy, hydroxy, amino or halogen groups, -R3 and R4 are selected independently from hydrogen and an alkyl group having from 1 to 3 carbon atoms, -R5 represents one or two substituents independently selected from hydrogen and the methyl, methoxyl, and hydroxyl groups, -n is a whole number from 0 to 6, and the amidine groups is in the para or meta position relative to the '-A-NH-' group.

    摘要翻译： 可以由以下通式（I）表示的化合物：其中：A独立地选自甲酰胺基，硫代羧酰胺基和羰基，R 1选自具有1至3个碳的烷基 原子和氨基，未取代或被硝基或甲基取代，R 2独立地选自氢，具有1至4个碳原子的烷基，甲氧基，乙氧基，丙氧基，单 - ，双 - 或具有5至12个碳原子的三环环烷烃残基，未被取代或被甲基，甲氧基，羟基，氨基或卤素基团取代的金刚烷基，芳基，萘基或杂环基，R3和R4独立地选自氢和烷基 具有1至3个碳原子的基团，R 5表示独立地选自氢和甲基，甲氧基和羟基的一个或两个取代基，n是0至6的整数，并且脒基团在t 他相对于“-A-NH-”组的对位或间位。

    VERFAHREN ZUR HERSTELLUNG VON 1-METHYL-3-NITROGUANIDIN
    25.
    发明公开
    VERFAHREN ZUR HERSTELLUNG VON 1-METHYL-3-NITROGUANIDIN 有权
    用于生产1-甲基-3-硝基胍

    公开(公告)号：EP1261581A1

    公开(公告)日：2002-12-04

    申请号：EP01901150.1

    申请日：2001-01-12

    申请人： NIGU CHEMIE GMBH

    发明人： KERN, Norbert

    IPC分类号： C07C279/36

    CPC分类号： C07C277/08 ,  C07C279/36

    摘要： The invention relates to a method for producing 1-methyl-3-nitroguanidine. According to said method, nitroguanidine is reacted with methylamine and/or a methylammonium salt in an aqueous solution, at temperatures of 30 to 60 °C and at a pH value of 9.5 to 12.3. In this way, yields of 1-methyl-3-nitroguanidine of at least 80 % and degrees of purity > 99 % can be obtained in a particularly environmentally friendly and technically simple way.