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    Acetic acid derivatives and composition containing the same
    4.
    发明授权
    Acetic acid derivatives and composition containing the same 失效
    乙酸衍生物及含有其的组合物

    公开(公告)号：US4356186A

    公开(公告)日：1982-10-26

    申请号：US246114

    申请日：1981-03-20

    申请人： Hitoshi Uno ,  Mikio Kurokawa ,  Hideo Nakamura

    发明人： Hitoshi Uno ,  Mikio Kurokawa ,  Hideo Nakamura

    IPC分类号： A61K31/34 ,  A61K31/38 ,  A61P29/00 ,  C07D313/12 ,  C07D337/12 ,  C07D337/14 ,  C07D405/06 ,  C07D409/06 ,  A61K31/335

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

    摘要： Novel acetic acid derivatives of the formula: ##STR1## wherein X is oxygen or sulfur; R.sub.1 is hydrogen or a lower alkyl; R.sub.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-lower alkenyloxy, a substituted aryl-lower alkenyloxy, an .omega.-disubstituted amino-lower alkoxy, a lower alkoxycrbonyl-lower alkoxy, a lower alkoxy-lower alkoxy, a hydroxy-lower alkoxy-lower alkoxy, an acyl-lower alkoxy, or a group ##STR2## wherein R.sub.3 is hydrogen, hydroxy, a lower alkyl, an aryl-lower alkyl, a hydroxy-lower alkyl, or a carboxy-lower alkyl, R.sub.4 is hydrogen, a lower alkyl or a hydroxy-lower alkyl, or the R.sub.3 and R.sub.4 may combine together with the nitrogen atom to which they are joined to form a heterocyclic group; and the group --CH(R.sub.1)COR.sub.2 is joined to the carbon atom at 2- or 3-position, and pharmaceutically acceptable salts thereof, processes for their preparation, and pharmaceutical compositions containing these compounds. They have excellent anti-inflammatory, analgesic and antipyretic activities with weak ulcerogenicity in the gastrointestinal tract and toxicity.

    摘要翻译： 下式的新型乙酸衍生物：其中X是氧或硫; R1是氢或低级烷基; R2是羟基，烷氧基，烯氧基，环烷氧基，芳氧基，取代的芳氧基，芳基 - 低级烷氧基，取代的芳基 - 低级烷氧基，芳基 - 低级烯氧基，取代的芳基 - 低级烯氧基，ω-二取代 氨基 - 低级烷氧基，低级烷氧基羰基 - 低级烷氧基，低级烷氧基 - 低级烷氧基，羟基 - 低级烷氧基 - 低级烷氧基，酰基 - 低级烷氧基或基团，其中R3是氢，羟基，低级烷基 ，芳基 - 低级烷基，羟基 - 低级烷基或羧基 - 低级烷基，R 4是氢，低级烷基或羟基 - 低级烷基，或者R 3和R 4可以与它们所在的氮原子结合在一起 连接形成杂环基; 并且基团-CH（R 1）COR 2与2-或3-位的碳原子及其药学上可接受的盐连接，其制备方法和含有这些化合物的药物组合物。 它们具有优良的抗炎，止痛和解热活性，肠胃道溃疡性弱，毒性低。

    4-(2-Pyridylamino)phenylacetic acid derivatives
    8.
    发明授权
    4-(2-Pyridylamino)phenylacetic acid derivatives 失效
    4-（2-吡啶基氨基）苯乙酸衍生物

    公开(公告)号：US4256753A

    公开(公告)日：1981-03-17

    申请号：US95572

    申请日：1979-11-19

    申请人： Hitoshi Uno ,  Yasutaka Nagai ,  Katsuhiko Hino ,  Hideo Nakamura

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

    IPC分类号： A61K31/44 ,  A61K31/4402 ,  A61K31/4418 ,  A61P25/04 ,  A61P29/00 ,  C07D213/74

    CPC分类号： C07D213/74

    摘要： Novel 4-(2'-pyridylamino)phenylacetic acid derivatives of the formula: ##STR1## wherein R.sub.1 is hydrogen, a halogen, a lower alkyl having 1 to 3 carbon atoms, or nitro, R.sub.2 is hydrogen, a halogen, or a lower alkyl having 1 to 3 carbon atoms, R.sub.3 is hydrogen, a halogen, or a lower alkyl having 1 to 3 carbon atoms, R.sub.4 is hydrogen or a lower alkyl having 1 to 3 carbon atoms, R.sub.5 is hydrogen or --CH.sub.2 CH.sub.2 OR.sub.6 wherein R.sub.6 is a lower alkyl having 2 or 3 carbon atoms and being substituted with 1 or 2 hydroxy groups, provided that R.sub.1 or R.sub.2 is not 4-halogen, or pharmaceutically acceptable salts thereof, and a process for the preparation thereof, pharmaceutical composition of said compounds, and a method of using said compounds 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.

    摘要翻译： 下式的新型4-（2'-吡啶基氨基）苯乙酸衍生物：其中R 1是氢，卤素，具有1至3个碳原子的低级烷基或硝基，R 2是氢，卤素或低级 具有1至3个碳原子的烷基，R 3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个碳原子的低级烷基，R 5是氢或-CH 2 CH 2 OR 6，其中R 6是 具有2或3个碳原子并且被1或2个羟基取代的低级烷基，条件是R1或R2不是4-卤素，或其药学上可接受的盐，及其制备方法，所述化合物的药物组合物和 使用所述化合物作为抗炎和止痛剂的方法。 它们具有优异的抗炎和止痛活性，在胃肠道中具有非常弱的溃疡形成能力。 一些化合物对由细胞免疫介导的慢性炎症具有优异的抑制活性。

    1-Substituted-4-(1,2-diphenylethyl)piperazine derivatives and compositions containing the same
    10.
    发明授权
    1-Substituted-4-(1,2-diphenylethyl)piperazine derivatives and compositions containing the same 失效
    1-取代的4-（1,2-二苯基乙基）哌嗪衍生物和含有它们的组合物

    公开(公告)号：US4080453A

    公开(公告)日：1978-03-21

    申请号：US663158

    申请日：1976-03-02

    申请人： Haruki Nishimura ,  Hitoshi Uno ,  Kagayaki Natsuka ,  Noriaki Shimokawa ,  Masanao Shimizu ,  Hideo Nakamura

    发明人： Haruki Nishimura ,  Hitoshi Uno ,  Kagayaki Natsuka ,  Noriaki Shimokawa ,  Masanao Shimizu ,  Hideo Nakamura

    IPC分类号： C07D295/02 ,  C07D295/03 ,  C07D295/096 ,  C07D295/14 ,  A61K31/495

    CPC分类号： C07D295/03 ,  C07D295/096

    摘要： 1-Substituted-4-(1,2-diphenylethyl)piperazine derivatives of the formula: ##STR1## wherein X is 2- or 3-hydroxy, 2-methoxy, 3-methyl, 3-alkoxy having 1 to 4 carbon atoms, or 2- or 3-alkanoyloxy having 2 to 5 carbon atoms; R is allyl, 3-hydroxyisoamyl, 3-methyl-2-butenyl, 3-methyl-3-butenyl, propyl, an unsubstituted monocycloalkyl having 5 to 8 carbon atoms, 2-chlorophenyl, or a phenyl substituted by hydroxy or methoxy; with proviso that when X is a substituent at position 2, R is cyclohexyl and when X is 3-methyl, R is 2-methoxyphenyl or an unsubstituted monocycloalkyl having 6 to 8 carbon atoms, and their pharmaceutically acceptable salts, and the preparation thereof, and analgesic or antitussive compositions containing the same as the essentially active ingredient.

    摘要翻译： 1-取代的4-（1,2-二苯基乙基）哌嗪衍生物，其结构式如下：其中X是2-或3-羟基，2-甲氧基，3-甲基，具有1至4个碳原子的3-烷氧基， 或具有2至5个碳原子的2-或3-烷酰氧基; R是烯丙基，3-羟基异戊基，3-甲基-2-丁烯基，3-甲基-3-丁烯基，丙基，未取代的具有5-8个碳原子的单环烷基，2-氯苯基或被羟基或甲氧基取代的苯基; 条件是当X是位置2的取代基时，R是环己基，当X是3-甲基时，R是2-甲氧基苯基或未取代的具有6-8个碳原子的单环烷基及其药学上可接受的盐及其制备方法， 以及含有与基本上活性成分相同的镇痛或镇咳药物。