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2. 发明授权

US5359076A Cyclic aminophenylacetic acid derivatives, process for preparing the same and immune response modulator having the same as an effective ingredient 失效
标题翻译：环状氨基苯乙酸衍生物，其制备方法和具有与有效成分相同的免疫应答调节剂
公开(公告)号：US5359076A
公开(公告)日：1994-10-25
申请号：US956012
申请日：1992-12-09
申请人： Yasushi Kohno , Katsuya Awano , Takayoshi Ishizaki , Eisuke Kojima , Shinji Kudoh , Yasuhiko Sakoe , Koji Saito
发明人： Yasushi Kohno , Katsuya Awano , Takayoshi Ishizaki , Eisuke Kojima , Shinji Kudoh , Yasuhiko Sakoe , Koji Saito
IPC分类号： A61K31/47 , A61P29/00 , A61P37/00 , A61P37/02 , C07C311/21 , C07C317/48 , C07C323/63 , C07C331/14 , C07D215/12 , C07D215/14 , C07D215/18 , C07D215/22 , C07D215/26 , C07D215/36 , C07D215/40 , C07D215/48 , C07D498/04 , C07D498/06 , C07F7/08 , C07D215/24 , C07D215/06 , C07D215/16
CPC分类号： C07D215/14 , C07C311/21 , C07C317/48 , C07C323/63 , C07C331/14 , C07D215/12 , C07D215/18 , C07D215/36 , C07D215/40 , C07D215/48 , C07F7/0812
摘要： The present invention provides novel cyclic aminophenylacetic acid derivatives having modulating action on immune response, their optical isomers, their salts and their preparative processes, and therapeutic agents for autoimmune diseases containing them as effective ingredients, the cyclic aminophenylacetic acid derivatives being represented by a general formula (1) ##STR1## wherein R and R.sup.1 each independently denotes hydrogen atom or lower alkyl group having 1 to 3 carbon atoms, R.sup.2 denotes a phenyl group (which may be substituted with 1 to 3 groups of halogen atom, methoxy group or their combinations) or trifluoromethyl group, and X denotes a hydrogen atom, lower alkyl group having 1 to 3 carbon atoms, lower alkoxy group having 1 to 3 carbon atoms, cyano group, thiocyano group, trimethylsilylethinyl group, phenyl group (which may be substituted with halogen atom, methoxy group, methyl group or their combinations), carbamoyl group, carboxyl group, lower alkoxycarbonyl group having 1 to 3 carbon atoms, acetyl group, benzoyl group, nitro group, amino group, lower alkanoylamino group having 1 to 3 carbon atoms, benzoylamino group which may be substituted, phenylsulfonylamino group which may be substituted, lower alkylthio group having 1 to 3 carbon atoms, lower alkylsulfinyl group having 1 to 3 carbon atoms, lower alkylsulfonyl group having 1 to 3 carbon atoms or halogen atom.
摘要翻译： PCT No.PCT / JP92 / 00476 Sec。 371日期：1992年12月9日 102（e）日期1992年12月9日PCT提交1992年4月15日PCT公布。公开号WO92 / 18482 本发明提供了具有对免疫应答的调节作用的新型环状氨基苯乙酸衍生物，其旋光异构体，其盐及其制备方法，以及含有它们作为有效成分的自身免疫性疾病的治疗剂，环状氨基苯乙酸衍生物由通式（1）表示，其中R和R 1各自独立地表示氢原子或具有1至3个碳原子的低级烷基，R 2表示苯基（可被1至3个取代基取代）卤素原子，甲氧基或它们的组合基团）或三氟甲基，X表示氢原子，碳原子数1〜3的低级烷基，碳原子数1〜3的低级烷氧基，氰基，硫氰基，三甲基甲硅烷基乙炔基，苯基（其可以被卤素原子，甲氧基，甲基或它们的组合取代），氨基甲酰基，羧基，低级烷氧基具有1至3个碳原子的酰基，乙酰基，苯甲酰基，硝基，氨基，具有1至3个碳原子的低级烷酰基氨基，可被取代的苯甲酰基氨基，可被取代的苯基磺酰基氨基，具有1个 3个碳原子，具有1至3个碳原子的低级烷基亚磺酰基，具有1至3个碳原子的低级烷基磺酰基或卤素原子。

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