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    • 3. 发明授权
    • Acetic acid derivatives and composition containing the same
    • 乙酸衍生物及含有其的组合物
    • US4356186A
    • 1982-10-26
    • US246114
    • 1981-03-20
    • Hitoshi UnoMikio KurokawaHideo Nakamura
    • Hitoshi UnoMikio KurokawaHideo Nakamura
    • A61K31/34A61K31/38A61P29/00C07D313/12C07D337/12C07D337/14C07D405/06C07D409/06A61K31/335
    • C07C323/00C07D313/12C07D337/12Y10S514/825Y10S514/916
    • 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.
    • 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. 发明授权
    • 4-(2-Pyridylamino)phenylacetic acid derivatives
    • 4-(2-吡啶基氨基)苯乙酸衍生物
    • US4256753A
    • 1981-03-17
    • US95572
    • 1979-11-19
    • Hitoshi UnoYasutaka NagaiKatsuhiko HinoHideo Nakamura
    • Hitoshi UnoYasutaka NagaiKatsuhiko HinoHideo Nakamura
    • A61K31/44A61K31/4402A61K31/4418A61P25/04A61P29/00C07D213/74
    • C07D213/74
    • 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.
    • 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。