申请人:A. H. Robins Company, Incorporated
公开号:US04547514A1
公开(公告)日:1985-10-15
Pharmaceutical compositions comprised of aryloxy-N-(aminoalkyl)-1-pyrrolidine and piperidine carboxamides and carbothioamides are provided of the formula: ##STR1## wherein Ar is selected from the group consisting of 1-naphthyl, 2-naphthyl, 2,3-dihydro-1H-inden-4-yl, 2,3-dihydro-1H-inden-5-yl, phenyl, substituted phenyl wherein the substituents are selected from lower alkyl of from 1 to 8 carbon atoms, lower alkyloxy of from 1 to 8 carbon atoms, halogen and trifluoromethyl; m and n are 1 or 2 but are never 2 at the same time; p is 1, 2, 3 or 4; R is selected from hydrogen or lower alkyl of from 1 to 3 carbon atoms; R.sup.1 and R.sup.2 are selected from hydrogen, lower alkyl of from 1 to 8 carbon atoms, phenyl, phenyl lower alkyl of from 7 to 9 carbon atoms, and cycloalkyl of from 3 to 8 carbon atoms, and R.sup.1 and R.sup.2 taken together with the adjacent atom may form a heterocyclic residue selected from 4-morpholino, 1-pyrrolidino, 1-piperidino, 1-piperazino and 4-lower alkyl piperazin-1-yl; X is oxygen or sulfur; and the pharmaceutically acceptable acid addition salts thereof having antiarrhythmic activity.
提供了包含芳氧基-N-(氨基烷基)-1-吡咯烷和哌啶羧酰胺和羧硫酰胺的制药组合物,其化学式为:##STR1## 其中Ar选自包括1-萘基,2-萘基,2,3-二氢-1H-茚-4-基,2,3-二氢-1H-茚-5-基,苯基,取代苯基,所述取代基选自1至8个碳原子的低烷基,1至8个碳原子的低烷氧基,卤素和三氟甲基;m和n为1或2,但同时永远不为2;p为1、2、3或4;R选自氢或1至3个碳原子的低烷基;R.sup.1和R.sup.2选自氢,1至8个碳原子的低烷基,苯基,7至9个碳原子的苯基低烷基和3至8个碳原子的环烷基,且R.sup.1和R.sup.2与相邻原子结合可形成4-吗啉基,1-吡咯烷基,1-哌啶基,1-哌嗪基和4-低烷基哌嗪-1-基的杂环残基;X为氧或硫;以及其药学上可接受的酸加成盐,具有抗心律失常活性。