申请人:KYOWA HAKKO KOGYO KABUSHIKI KAISHA
公开号:EP0273401A1
公开(公告)日:1988-07-06
Isoindolin-1-one compounds represented by the following formula (I);
wherein n represents an integer of 1 to 6; m represents 0 or 1; R1, R2 and R3 are each independently hydrogen or lower alkyl, and when m is 1, R, and one of R2 and R3 may form a five-membered or six-membered ring over N atom; X represents hydrogen or hydroxy; Ar represents naphthyl, pyridyl or substituted phenyl represented by the formula (II); Ar and X may form a lactone ring;
[wherein Y represents carboxyl, lower alkoxycarbonyl, carbamoyl, N,N-lower alkyl-substituted carbamoyl or amino represented by the formula (III):
(wherein Rs and R7 are each independently hydrogen, lower alkyl or lower alkanoyl); R4 and R5 are each independently hydrogen, lower alkyl, cyano or halogen]} or a phrarmaceutically acceptable acid addition salt or metal salt thereof have an excellent antiarrhythmic activity.
由下式(I)代表的异吲哚啉-1-酮化合物;
其中 n 代表 1 至 6 的整数;m 代表 0 或 1;R1、R2 和 R3 各自独立地为氢或低级烷基,当 m 为 1 时,R 以及 R2 和 R3 中的一个可在 N 原子上形成五元环或六元环;X 代表氢或羟基;Ar 代表萘基、吡啶基或由式(II)代表的取代苯基;Ar 和 X 可形成内酯环;
[其中 Y 代表羧基、低级烷氧基羰基、氨基甲酰基、N,N-低级烷基取代的氨基甲酰基或由式(III)代表的氨基:
(其中 Rs 和 R7 各自独立地为氢、低级烷基或低级烷酰基);R4 和 R5 各自独立地为氢、低级烷基、氰基或卤素]}或其短链可接受的酸加成盐或金属盐具有极佳的抗心律失常活性。