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    • 3. 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。