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CYCLIC AMINOPHENYLACETIC ACID DERIVATIVES WITH IMMUNOMODULATING ACTION, PROCESSES FOR PREPARATION AND SYNTHESIS INTERMEDIATES THEREOF

机译:具有免疫调节作用的环氨基苯甲酸衍生物,其制备和合成过程在其中起作用

摘要

The invention relates to novel cyclic aminophenylacetic acid derivatives which have modulatory action on the immune reaction, to processes of preparation and intermediates in their synthesis, to therapeutic agents for autoimmune diseases, which contain these derivatives as effective ingredients, said derivatives being the general formula (I): wherein R and R are each independently a hydrogen atom or a lower alkyl group of 1 to 3 carbon atoms, R is a phenyl group which may be substituted with 1 to 3 halogen atoms, a methoxy or their combinations or a trifluoromethyl group and X indicates a hydrogen atom, a lower alkyl group, a lower alkoxy group, cyano, thiocyano, trimethylsilylethynyl group, a substituted or unsubstituted phenyl group, carbamoyl, carboxyl, lower alkoxycarbonyl, acetyl, nitro, amino, lower alkanoylamino, optionally substituted benzoylamino, optionally substituted phenylsulfonylamino, alkylthio lower alkyl, lower alkylsulfinyl, lower alkylsulfonyl or a halogen atom.
机译:本发明涉及对免疫反应具有调节作用的新型环状氨基苯基乙酸衍生物,其合成方法和中间体,涉及自身免疫性疾病的治疗剂,其中含有这些衍生物作为有效成分,所述衍生物为通式( I):其中R 1和R 2各自独立地为氢原子或1-3个碳原子的低级烷基,R为可被1-3个卤素原子,甲氧基或其组合或三氟甲基取代的苯基。 X表示氢原子,低级烷基,低级烷氧基,氰基,硫氰基,三甲基甲硅烷基乙炔基,取代或未取代的苯基,氨基甲酰基,羧基,低级烷氧羰基,乙酰基,硝基,氨基,低级烷酰基氨基,任选取代的苯甲酰基氨基,任选取代的苯基磺酰基氨基,烷硫基低级烷基,低级烷基亚磺酰基,低级烷基磺酰基或卤素原子。

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