申请人:A. H. Robins Company, Incorporated
公开号:US04835164A1
公开(公告)日:1989-05-30
Novel heterocyclicmethanols are disclosed having the formula: ##STR1## wherein Z is pyrrolidinyl, piperidinyl, homopiperidinyl or pyridinyl; R.sup.1 is hydrogen, loweralkyl or carbethoxymethyl; R.sup.2 is hydrogen, loweralkyl, cycloalkyl, phenyl or phenyl-loweralkyl; R.sup.3 is 1 or 2-naphthalenyl, 2,3-dihydroinden-4 or 5-yl, phenyl or phenyl substituted by loweralkyl, loweralkoxy, halogen, trifluoromethyl, phenyl, methylenedioxy, nitro, amino, loweralkylamino, diloweralkylamino, loweracylamino; the 1-position of 2-pyrrolidinyl, 2-piperidinyl or 2-homopiperidinyl may be substituted by an R.sup.4 loweralkyl group, or R.sup.1 may form methylene or --CH.sub.2 -C(O)-bridges with R.sup.4 ; the pharmaceutically acceptable salts and diastereomers thereof, which compounds have antiarrhythmic and/or hypotensive activity in animals.
公开了具有以下式子的新型杂环甲醇:##STR1## 其中Z为吡咯烷基,哌啶基,同哌啶基或吡啶基; R.sup.1为氢,低碳基或羰乙氧甲基; R.sup.2为氢,低碳基,环烷基,苯基或苯基-低碳基; R.sup.3为1或2-萘基,2,3-二氢吲哚-4或5-基,苯基或被低碳基,低碳氧基,卤素,三氟甲基,苯基,亚甲二氧基,硝基,氨基,低碳基氨基,二低碳基氨基,低酰胺基取代的苯基; 2-吡咯烷基,2-哌啶基或2-同哌啶基的1-位置可以被R.sup.4的低碳基取代,或者R.sup.1可以与R.sup.4形成亚甲基或--CH.sub.2-C(O)-桥。这些化合物及其药学上可接受的盐和对映异构体在动物中具有抗心律失常和/或降压活性。