申请人:NISSHIN FLOUR MILLING CO., LTD.
公开号:EP0499995A2
公开(公告)日:1992-08-26
Disclosed are compounds of formula (I)
in which A represents a group selected from the following formulas (a) to (f)
or
wherein R1 and R2 may be the same or different and each represents a hydrogen atom, a C1-C6 alkyl group, a phenyl group or an aryl(C1-C4)alkyl group, R3 represents a C1-C6alkyl group, R4 represents a hydrogen atom, a C1-C6 alkyl group, a phenyl group or an aryl(C1-C4)alkyl group, Rs, R6 and R7 may be the same or different and each represents a hydrogen atom, an amino group, a halogen atom, a C1-C4 alkoxy group or a phthalimide group and X represents O or NH, physiologically acceptable salts and quaternary ammonium salts thereof. The compounds are selective antagonists of 5HT at 5-HT3 receptors and useful in the treatment of psychotic disorders, neurotic diseases, gastric stasis symptoms, gastrointestinal disorders, nausea and vomiting.
公开了式 (I) 的化合物
其中 A 代表选自下式(a)至(f)的基团
或
其中 R1 和 R2 可以相同或不同,各自代表氢原子、C1-C6 烷基、苯基或芳基(C1-C4)烷基,R3 代表 C1-C6 烷基,R4 代表氢原子、C1-C6 烷基、苯基或芳基(C1-C4)烷基、Rs、R6 和 R7 可以相同或不同,各自代表氢原子、氨基、卤素原子、C1-C4 烷氧基或邻苯二甲酰亚胺基团,X 代表 O 或 NH、生理上可接受的盐及其季铵盐。这些化合物是 5-HT3 受体上 5HT 的选择性拮抗剂,可用于治疗精神障碍、神经性疾病、胃淤血症状、胃肠功能紊乱、恶心和呕吐。