Aryloxy-N-(aminoalkyl)-1-pyrrolidine and piperidine carboxamides and carbothioamides having antiarrhythmic activity
申请人:A.H. ROBINS COMPANY, INCORPORATED
公开号:EP0147909A1
公开(公告)日:1985-07-10
Antiarrhythmic pharmaceutical compositions comprise . an aryloxy-N-(aminoalkyl)-1-pyrrolidine or piperidine carboxamide or carbothioamide of formula (I)
wherein Ar represents 1-naphthyl, 2-naphthyl, 2,3-dihydro-1H-inden-4-yl, 2,3-dihydro-lH-inden-5-yl, phenyl or substituted phenyl wherein the or each substituent independently is lower alkyl of from 1 to 8 carbon atoms, lower alkyloxy of from 1 to 8 carbon atoms, halogen or trifluoromethyl; m and n are 1 or 2 but are never 2 at the same time; p is 1, 2, 3 or 4; R represents hydrogen or lower alkyl of from 1 to 3 carbon atoms; each of R1 and R2 independently represents hydrogen, lower alkyl of from 1 to 8 carbon atoms, phenyl, phenyl lower alkyl of from 7 to 9 carbon atoms, or cycloalkyl of from 3 to 8 carbon atoms, or R1 and R2 taken together with the adjacent atom form a 4-morpholino, 1-pyrrolidino, 1-piperidino, 1-piperazino and 4-lower alkyl piperazin-1-yl heterocyclic residue; X represents oxygen or sulphur; or a pharmaceutically acceptable acid addition salts thereof. Novel compounds within formula (I) are also disclosed, as are processes for their preparation and intermediates useful in their preparation.
抗心律失常药物组合物包括.式 (I) 的芳氧基-N-(氨基烷基)-1-吡咯烷或哌啶甲酰胺或硫代甲酰胺
其中 Ar 代表 1-萘基、2-萘基、2,3-二氢-1H-茚-4-基、2,3-二氢-lH-茚-5-基、苯基或取代苯基,其中或每个取代基独立地为 1 至 8 个碳原子的低级烷基、1 至 8 个碳原子的低级烷氧基、卤素或三氟甲基;m 和 n 为 1 或 2,但绝不同时为 2;p 为 1、2、3 或 4;R 代表氢或 1 至 3 个碳原子的低级烷基;R1和R2各自独立地代表氢、1至8个碳原子的低级烷基、苯基、7至9个碳原子的苯基低级烷基或3至8个碳原子的环烷基,或R1和R2与相邻原子一起形成4-吗啉基、1-吡咯烷基、1-哌啶基、1-哌嗪基和4-低级烷基哌嗪-1-基杂环残基;X代表氧或硫;或其药学上可接受的酸加成盐。此外,还公开了式 (I) 中的新型化合物,以及它们的制备工艺和用于制备它们的中间体。