N-[(Amino)Alkyl]-1-pyrrolidine, 1-piperidine and 1-homopiperidinecarboxamides (and thiocarboxamides) with sulphur linked substitution in the 2, 3 or 4-position
申请人:A.H. ROBINS COMPANY, INCORPORATED
公开号:EP0160436A2
公开(公告)日:1985-11-06
Pyrrolidine, piperidine and homopiperidine- carboxamide and thiocarboxamide compounds of the formula:
wherein X is -S-, -S(0)- or -S(0)2-; A is a loweralkalene chain and A1 and A2 are alkalene chains when p and d are one; R, R1 and R2 are hydrogen, loweralkyl, phenyl cycloalkyl or phenylalkyl and R1 and R2 may form a heterocyclic residue with the adjacent nitrogen atom; Q is a selected aromatic radical, and the pharmaceutically acceptable acid addition salts are useful as cardiac antiarrhythmia agents.
Chemical intermediates, unsubstituted on pyrrolidine, piperidine and homopiperidine nitrogen but with the -(A2)p-X-(A2)d-Q side chain are also disclosed.
式中的吡咯烷、哌啶和均哌啶-羧酰胺和硫代羧酰胺化合物:
其中,X 是-S-、-S(0)- 或-S(0)2-;A 是低级烯烃链,当 p 和 d 为 1 时,A1 和 A2 是烯烃链;R、R1 和 R2 是氢、低级烷基、苯基环烷基或苯基烷基,R1 和 R2 可与相邻的氮原子形成杂环残基;Q 是选定的芳香基,药学上可接受的酸加成盐可用作抗心律失常剂。
还公开了吡咯烷、哌啶和高哌啶氮上未取代但具有-(A2)p-X-(A2)d-Q 侧链的化学中间体。