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    NOVEL PYRIDINE DERIVATIVE HAVING ANTI-HELICOBACTER PYLORI ACTIVITY
    2.
    发明公开
    NOVEL PYRIDINE DERIVATIVE HAVING ANTI-HELICOBACTER PYLORI ACTIVITY 有权
    消除PYRIDINDERIVAT MIT WIRKUNG GEGEN HELICOBACTER PYLORI

    公开(公告)号：EP2003130A2

    公开(公告)日：2008-12-17

    申请号：EP07715278.3

    申请日：2007-03-07

    申请人： aRigen Pharmaceuticals, Inc.

    发明人： ITO, Masaharu ,  YAMAMOTO, Masaichi

    IPC分类号： C07D401/12 ,  A61K31/4439 ,  A61K45/00 ,  A61K47/36 ,  A61P1/04 ,  A61P1/18 ,  A61P31/04 ,  A61P35/00 ,  A61P43/00

    CPC分类号： A61K31/4439 ,  A61K9/0019 ,  A61K9/0095 ,  A61K9/1623 ,  A61K9/2018 ,  A61K9/4858 ,  A61K45/06 ,  A61K47/36 ,  C07D401/12

    摘要： The obj ect is to provide an excellent pharmaceutical having an anti-Helicobacter pylori activity. Disclosed is a novel pyridine derivative represented by the following general formula (I):

    wherein R represents a linear or branched hydroxyalkyl group having 5 to 10 carbon atoms, or a pharmaceutically acceptable salt thereof, which has a potent antibacterial activity against H. pyroli ( Helicobacter pyroli ). Examples of the disease which can be prevented/treated by administration of a pharmaceutical agent comprising the compound include gastritis, gastric ulcer, duodenal ulcer, gastric MALT lymphoma, gastric hyperplastic polyp, development of gastric cancer after endoscopic resection of the early stage of gastric cancer and the like.

    摘要翻译： 本发明的目的是提供具有抗幽门螺杆菌活性的优良药物。 公开了由以下通式（I）表示的新型吡啶衍生物：其中R表示具有5-10个碳原子的直链或支链羟烷基或其药学上可接受的盐，其具有对吡嘧啶的有效抗菌活性（ 幽门螺杆菌）。 可以通过施用包含该化合物的药剂来预防/治疗的疾病的实例包括胃炎，胃溃疡，十二指肠溃疡，胃MALT淋巴瘤，胃增生性息肉，胃癌早期胃镜切除后胃癌的发展 等等。

    PYRIDINE THIO DERIVATIVE, AND PHARMACEUTICAL COMPOSITION WHICH CONTAINS SAME AND HAS ANTI-HELICOBACTER PYLORI ACTION
    4.
    发明公开
    PYRIDINE THIO DERIVATIVE, AND PHARMACEUTICAL COMPOSITION WHICH CONTAINS SAME AND HAS ANTI-HELICOBACTER PYLORI ACTION 审中-公开
    PYRIDINTHIODERIVAT SOWIE PHARMAZEUTISCHE ZUSAMMENSETZUNG DAMIT UND MIT ANTI-HELIDOBACTER-PYLORI-WIRKUNG

    公开(公告)号：EP2420500A1

    公开(公告)日：2012-02-22

    申请号：EP10761444.8

    申请日：2010-04-08

    申请人： aRigen Pharmaceuticals, Inc.

    发明人： YAMAMOTO, Masaichi ,  ITO, Masaharu ,  TSUJII, Masahiko ,  HAMAZAKI, Mitsunori

    IPC分类号： C07D401/12 ,  A61K31/4439 ,  A61P1/04 ,  A61P31/04 ,  A61P35/00

    CPC分类号： C07D401/12

    摘要： Disclosed are a novel pyridine thio derivative, and a pharmaceutical composition using the novel pyridine thio derivative, particularly a pharmaceutical composition having selective antibacterial activity against Helicobacter pylori. Specifically disclosed is a pyridine thio derivative represented by general formula (I) (wherein R 1 and R 2 each represents a hydrogen atom, a C 1-8 alkyl group or the like; R 3 and R 4 each represents a hydrogen atom, a C 1-8 alkyl group or the like; X represents -O-, -S- or the like; Y represents a C 1-12 alkyl group which may be substituted by a substituent or -(R S -O) n -R 6 (wherein R 5 represents a C 1-5 alkylene group; R 6 represents a C 1-8 alkyl group which may be substituted by a substituent, and n represents an integer of 1-10); and Z represents a hydrogen atom or the like), or a pharmacologically acceptable salt thereof. Also specifically disclosed is a pharmaceutical composition containing the pyridine thio derivative or a salt thereof.

    摘要翻译： 公开了一种新型吡啶硫代衍生物，以及使用新型吡啶硫代衍生物的药物组合物，特别是对幽门螺杆菌具有选择性抗菌活性的药物组合物。 具体公开的是由通式（I）表示的吡啶硫代衍生物（其中R 1和R 2各自表示氢原子，C 1-8烷基等; R 3和R 4各自表示氢原子， C 1-8烷基等; X表示-O-，-S-等; Y表示可被取代基取代的C 1-12烷基或 - （RS-O）n -R 6 （其中R 5表示C 1-5亚烷基; R 6表示可被取代基取代的C 1-8烷基，n表示1-10的整数）; Z表示氢原子或 类似物）或其药理学上可接受的盐。 还具体公开了含有吡啶硫代衍生物或其盐的药物组合物。

    HELICOBACTER PYLORI ERADICATING AGENT HAVING INHIBITORY ACTIVITY ON GASTRIC ACID SECRETION
    6.
    发明公开
    HELICOBACTER PYLORI ERADICATING AGENT HAVING INHIBITORY ACTIVITY ON GASTRIC ACID SECRETION 有权
    MITTEL ZUM AUSMERZEN VON HELICOBACTER PYLORI MIT HEMMENDER WIRKUNG AUF DIEMAGENSÄURESEKRETION

    公开(公告)号：EP2103608A1

    公开(公告)日：2009-09-23

    申请号：EP07849849.0

    申请日：2007-12-18

    申请人： Arigen, Pharmaceuticals, Inc.

    发明人： ITO, Masaharu ,  YAMAMOTO, Masaichi

    IPC分类号： C07D401/12 ,  A61K31/4439 ,  A61P1/00 ,  A61P1/04 ,  A61P1/18 ,  A61P31/04

    CPC分类号： C07D401/12

    摘要： Disclosed are: a compound which is stable in an acid, has an antibacterial effect against a bacterium Helicobacter pylori, can exert a satisfactory level of an antibacterial effect when used singly, does not affect an enteric bacterium, has an antibacterial effect against a bacterium resistant to an antibacterial agent, and has an inhibitory effect on gastric acid secretion; and a pharmaceutical composition comprising the compound. Specifically disclosed are: a compound represented by the general formula (I) or a salt thereof; and a pharmaceutical composition comprising the compound or the salt thereof:

    wherein R represents a linear alkyl group having 4 to 8 carbon atoms, preferably 5 to 7 carbon atoms.

    摘要翻译： 公开的是：在酸中稳定的化合物对幽门螺杆菌具有抗菌作用，当单独使用时可以发挥令人满意的抗菌作用，不影响肠道细菌，对抗细菌具有抗菌作用 对抗菌剂，对胃酸分泌具有抑制作用; 和包含该化合物的药物组合物。 具体公开的是：由通式（I）表示的化合物或其盐; 以及包含该化合物或其盐的药物组合物：其中R表示具有4至8个碳原子，优选5至7个碳原子的直链烷基。