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    PROCESS FOR THE PREPARATION OF OXAZOLIDINONE DERIVATIVE
    2.
    发明公开
    PROCESS FOR THE PREPARATION OF OXAZOLIDINONE DERIVATIVE 审中-公开
    VERFAHREN ZUR HERSTELLUNG VON OXAZOLIDINON-DERIVATEN

    公开(公告)号：EP1118611A1

    公开(公告)日：2001-07-25

    申请号：EP99944807.9

    申请日：1999-09-24

    申请人： NIPPON CHEMIPHAR CO., LTD.

    发明人： YAMAMOTO, Masao ,  YOSHIDA, Shinichi

    IPC分类号： C07D263/22

    CPC分类号： C07D263/20 ,  C07D263/22

    摘要： The invention relates to a process for preparing (5RS)-5-benzyl-3-[(1SR)-3-morpholino-1-phenylpropyl]-1,3-oxazolidin-2-one or its pharmacologically acceptable salt which is of value as a remedy for treatment of incontinence of urine and thamuria and which is performed by the steps of:

    dissolving an acid and a mixture of (2RS)-1- [(1SR)-3-morpholino-1-phenylpropyl]amino-3-phenyl-2-propanol and (2RS) -1- ((lRS,) -3-morpholino-1-phenylpropyl] amino-3-phenyl-2-propanol in a solvent to obtain a salt of the former (1SR)-compound utilizing difference of solubility between the salt of (1SR)-compound and a salt of the latter (1RS)-compound;
    bringing a basic compound into contact with the salt of (1SR)-compound to produce a free (1SR)-compound;
    reacting thus produced (2RS)-1-[(1SR)-3-morpholino-1-phenylpropyl]amino-3-phenyl-2-propanol with a compound having the formula (I):

            R 2 C=O     (I)

    wherein R represents a chlorine atom, an alkoxy group, an aryloxy group or an amino group, or a chloroformic acid ester; and
    cyclizing the resulting product.

    摘要翻译： 本发明涉及制备（5RS）-5-苄基-3-Ä（1SR）-3-吗啉代-1-苯基丙基] -1,3-恶唑烷-2-酮或其药理学上可接受的盐的方法，其值为 用于治疗尿和性尿失禁的治疗方法，其通过以下步骤进行：将酸和（2RS）-1-Ä（1SR）-3-吗啉代-1-苯基丙基氨基-3-苯基-2 丙醇和（2RS）-1 - （（1R，3R）-3-吗啉代-1-苯基丙基）氨基-3-苯基-2-丙醇在溶剂中反应，得到前者（1SR） - 化合物的盐，利用溶解度差异 （1SR） - 化合物的盐和后者的盐（1RS） - 化合物之间;使碱性化合物与（1SR）化合物的盐接触以产生游离（1SR） - 化合物;如此制备的（1SR） 2RS）-1-Ä（1SR）-3-吗啉代-1-苯基丙基氨基-3-苯基-2-丙醇与具有式（I）的化合物反应：R2C = O其中R表示氯原子，烷氧基， 芳氧基或氨基，或氯仿a 碳酸酯 并使所得产品环化

    CONDENSED PYRIMIDINE DERIVATIVE AND XANTHINE OXIDASE INHIBITOR
    6.
    发明授权
    CONDENSED PYRIMIDINE DERIVATIVE AND XANTHINE OXIDASE INHIBITOR 有权
    稠合嘧啶衍生物和黄嘌呤氧化酶抑制剂

    公开(公告)号：EP1757610B1

    公开(公告)日：2011-06-08

    申请号：EP05751417.6

    申请日：2005-06-13

    申请人： Nippon Chemiphar Co., Ltd.

    发明人： YOSHIDA, Shinichi ,  KOBAYASHI, Kunio ,  MOCHIDUKI, Nobutaka ,  YAMAKAWA, Tomio ,  KOBAYASHI, Tadashi ,  SHINOHARA, Yoriko

    IPC分类号： C07D498/04 ,  A61K31/519 ,  A61P19/06 ,  A61P43/00 ,  C07D513/04

    CPC分类号： C07D513/04 ,  C07D498/04

    摘要： Disclosed is a compound represented by the following general formula (I) (wherein R1 represents an aryl group having 6-10 carbon atoms or a heteroaryl group which may have, as a substituent, a group selected from an alkyl group having 1-8 carbon atoms, an alkyl group having 1-8 carbon atoms which is substituted with a halogen atom, an alkoxy group having 1-8 carbon atoms, an alkoxy group having 1-8 carbon atoms which is substituted with an alkoxy group having 1-8 carbon atoms, an alkoxycarbonyl group having 2-8 carbon atoms, a formyl group, a carboxyl group, a halogen atom, a hydroxyl group, a nitro group, a cyano group, an amino group, an aryl group having 6-10 carbon atoms and an aryloxy group having 6-10 carbon atoms; R2 represents a cyano group, a nitro group or the like; R3 represents an hydroxyl group or the like; X represents an oxygen atom, a sulfur atom or the like; and Y represents an oxygen atom or a sulfur atom). Also disclosed is a xanthine oxidase inhibitor containing such a compound.

    CONDENSED PYRIMIDINE DERIVATIVE AND XANTHINE OXIDASE INHIBITOR
    8.
    发明公开
    CONDENSED PYRIMIDINE DERIVATIVE AND XANTHINE OXIDASE INHIBITOR 有权
    新戊酰氧化酶抑制剂的邻苯二酚

    公开(公告)号：EP1757610A1

    公开(公告)日：2007-02-28

    申请号：EP05751417.6

    申请日：2005-06-13

    申请人： Nippon Chemiphar Co., Ltd.

    发明人： YOSHIDA, Shinichi ,  KOBAYASHI, Kunio ,  MOCHIDUKI, Nobutaka ,  YAMAKAWA, Tomio ,  KOBAYASHI, Tadashi ,  SHINOHARA, Yoriko

    IPC分类号： C07D498/04 ,  A61K31/519 ,  A61P19/06 ,  A61P43/00 ,  C07D513/04

    CPC分类号： C07D513/04 ,  C07D498/04

    摘要： The invention relates to compounds of the following formula (I) or their salts:

    in which R 1 is a group of phenyl, naphthyl, pyridyl or the like which may have a substituent such as an alkyl group having 1-8 carbon atoms, an alkoxy group having 1-8 carbon atoms, an alkoxycarbonyl group having 2-8 carbon atoms, carboxyl, halogen, hydroxyl, nitro, or cyano; R 2 is cyano, nitro, or the like; R 3 is hydroxyl or the like; X is oxygen, sulfur, or the like; and Y is oxygen or sulfur, and a xanthine oxidase inhibitor containing the compound.

    摘要翻译： 本发明涉及下式（I）的化合物或其盐：其中R 1是可具有取代基的苯基，萘基，吡啶基等基团，例如具有1-8个碳原子的烷基， 具有1-8个碳原子的烷氧基，具有2-8个碳原子的烷氧基羰基，羧基，卤素，羟基，硝基或氰基; R 2是氰基，硝基等; R 3是羟基等; X是氧，硫等; Y为氧或硫，含有该化合物的黄嘌呤氧化酶抑制剂。