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发明授权
CN1882587B 三环化合物作为甘氨酸转运抑制剂的用途 失效 - 权利终止

三环化合物作为甘氨酸转运抑制剂的用途
摘要：
本发明涉及具有通式(I)的化合物，其中：R代表氢原子或乙烯基基团；n代表0、1或2；X代表具有式CH的基团或氮原子；R1代表苯基或萘基基团，或环己基基团，或杂芳基基团；R2代表氢原子，或者一个或多个选自卤素原子及三氟甲基、烷基、烷氧基、噻吩基、苯氧基、羟基、巯基、硫烷基、氰基或通式-NR4R5、SO2NR4R5、-SO2烷基、-SO2-苯基、-CONR4R5、-COOR7、-CO-烷基、-CO-苯基、-NHCOR8、-NHSO2-烷基、-NHSO2-苯基及-NHSO2NR4R5或具有通式-OCF2O-的二价基团的取代基；R4和R5各自代表氢原子或烷基基团或R4和R5与氮原子一起形成吡咯烷环、哌啶环或吗琳环。式(I)的化合物具有作为glyt1和/或glyt2转运蛋白的特异抑制剂的特殊活性。
摘要（英）：

The invention relates to a compound having general formula (I), wherein: R represents a hydrogen atom or a vinyl group; n represents 0, 1 or 2; X represents a groups having formula CH or a nitrogen atom; R1 represents a phenyl or naphthyl group, or a cyclohexyl group, or a heteroaryl group; R2 represents a hydrogen atom, or one or more substituents selected from among the halogen atoms and the trifluoromethyl, alkyl, alkoxy, thienyl, phenyloxy, hydroxy, mercapto, thioalkyl, cyano groups or a group having general formula -NR4R5, SO2NR4R5, -SO2-alkyl, -SO2-phenyl, -CONR4R5, -COOR7, -CO-alkyl, -CO-phenyl, -NHCOR8, -NHSO2-alkyl, -NHSO2-phenyl and -NHSO2NR4R5 or a divalent group having formula -OCF2O-; and R4 and R5 each represent a hydrogen atom or an alkyl group or R4 and R5, together with the nitrogen atom bearing same, form a pyrrolidine, piperidine or morpholine ring. The compound of the formula (I) exhibits a particular activity as specific inhibitors of the glycine transporters glyt1 and/or glyt2.

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