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11 条记录 (耗时 0.013 秒)

    Acetic acid derivatives, process for the preparation thereof and composition containing the same
    3.
    发明公开
    Acetic acid derivatives, process for the preparation thereof and composition containing the same 失效
    乙酸衍生物，它们的制备方法以及含有它们的制剂。

    公开(公告)号：EP0037254A1

    公开(公告)日：1981-10-07

    申请号：EP81301302.6

    申请日：1981-03-26

    申请人： Dainippon Pharmaceutical Co., Ltd.

    发明人： Uno, Hitoshi ,  Kurokawa, Miko ,  Nakamura, Hideo

    IPC分类号： C07D313/12 ,  C07D337/12 ,  A61K31/335 ,  A61K31/38 ,  C07D405/06 ,  C07D409/06 ,  A61K31/44 ,  A61K31/535

    CPC分类号： C07C323/00 ,  C07D313/12 ,  C07D337/12 ,  Y10S514/825 ,  Y10S514/916

    摘要： Novel acetic acid derivatives of the formula:
    wherein X is oxygen or sulfur; R, is hydrogen or a lower alkyl; R 2 is hydroxy, an alkoxy, an alkenyloxy, a cycloalkyloxy, an aryloxy, a substituted aryloxy, an aryl-lower alkoxy, a substituted aryl-lower alkoxy, an aryl-lowrer alkenyloxy, a substituted aryl-lower alkenyloxy, an ω-di-substituted amino-lower alkoxy, a lower alkoxycarbonyl-lower alkoxy, a lower alkoxy-lower alkoxy, a hydroxy-lower alkoxy-lower alkoxy, an acyl-lower alkoxy, or a group
    wherein R 3 is hydrogen, hydroxy, a lower alkyl, an aryl-lower alkyl, a hydroxy-lower alkyl, or a carboxy-lower alkyl, R 4 is hydrogen, a lower alkyl or a hydroxy-lower alkyl, or the R 3 and R 4 may combine together with the nitrogen atom to which they are joined to form a heterocyclic group; and the group -CH(R 1 )COR 2 is joined to the carbon atom at 2- or 3-position, and pharmaceutically acceptable salts thereof have excellent anti-inflammatory, analgesic and antipyretic activities with weak ulcerogenicity in the gastrointestinal tract and toxicity. They can be prepared by cyclization reaction and made up into pharmaceutical compositions.

    4-(2'-Pyridylamino)-phenylacetic acid derivatives, process for their preparation, pharmaceuticals containing these compounds and their use
    4.
    发明公开
    4-(2'-Pyridylamino)-phenylacetic acid derivatives, process for their preparation, pharmaceuticals containing these compounds and their use 失效
    4-（2'-吡啶基氨基）苯基乙酸衍生物，它们的制备方法，含有这些化合物和它们的药物组合物。

    公开(公告)号：EP0011854A1

    公开(公告)日：1980-06-11

    申请号：EP79104726.9

    申请日：1979-11-27

    申请人： Dainippon Pharmaceutical Co., Ltd.

    发明人： Uno, Hitoshi ,  Nagai, Yasutaka ,  Hino, Katsuhiko ,  Nakamura, Hideo

    IPC分类号： C07D213/74 ,  A61K31/44

    CPC分类号： C07D213/74

    摘要： The invention relates to novel 4-(2'-pyridylamino) -phenylacetic acid derivatives of the formula I

    Wherein R 1 is hydrogen, a halogen, a lower alkyl having 1 to 3 carbon atoms, or nitro, R 2 is hydrogen, a halogen, or a lower alkyl having 1 to 3 carbon atoms, R 3 is hydrogen, a halogen, or a lower alkyl having 1 to 3 carbon atoms, R 4 is hydrogen or a lower alkyl having 1 to 3 carbon atoms, R s is hydrogen or-CH 2 CH 2 OR 6 wherein R 6 is lower alkyl having 2 or 3 carbon atoms and being substituted with 1 or 2 hydroxy groups, provided that R 1 or R 2 is not 4-halogen,
    or pharmaceutically acceptable salts thereof, a process fortheir preparation (e.g.2-[4-(2'-pyridylamino)pehnyl] propionic acid (compound A) is prepared by reacting methyl 2-(4-amino -phenyl)propionate with 2-chloropyridine, followed by hydrolysis), pharmaceutcial composition containing these compounds, and their use as anti-inflammatory and analgesic agents. They have excellent anti-inflammatory and analgesic activities with an extremely weak ulcerogenicity in the gastrointestinal tract. Some of the compounds have superior inhibitory activity against chronic inflammation mediated by cellular immunity.
    In the figure the prophylactic effect on adjuvant-induced arthritis in rats is shown (vehicle control (line 1), reference compound Ibuprofen (line 2), new compound A (line 3)].

    摘要翻译： 本发明涉及新的4-卤（2分钟-pyridylamino）下式的苯基乙酸衍生物：... ...... 其中R 1是氢，具有1至3个碳原子的低级烷基，或 硝基，R 2是氢，卤素，或具有1至3个碳原子的低级烷基，R3是氢，卤素，或具有1至3个碳原子的低级烷基，R 4是氢或具有1至3个碳的低级烷基 原子，R 5是氢或-CH2CH2OR6 worin R 6为具有2或3个碳原子和具有1个或2个羟基取代的被做R1或R2不是4-卤，或它们的药学上可接受的盐的低级烷基，条件...，用于处理 其制备方法，pharmaceutcial组合物（例如2- [4-（2分钟-pyridylamino）pehnyl]（丙酸（化合物A）是通过使2- 4-氨基 - 苯基） - 丙酸酯与2-氯吡啶，然后水解制备） 含有合成的化合物以及它们作为抗炎剂和止痛剂的用途。 它们具有优异的抗炎镇痛作用与胃肠道ulcerogenicity极其微弱。 一些化合物具有抵抗由细胞免疫介导的慢性炎症优异的抑制活性。 ... 在被示出对大鼠佐剂诱导的关节炎的预防作用图（溶媒对照（第1行），参考化合物布洛芬（线2），新的化合物A（第3行）。