Aryloxymethyl derivatives of nitrogenous heterocyclic methanols and ethers thereof having cardiovascular activity
申请人:A.H. ROBINS COMPANY, INCORPORATED
公开号:EP0279707A2
公开(公告)日:1988-08-24
Novel heterocyclicmethanols are disclosed having the formula:
wherein Z is pyrrolidinyl, piperidinyl, homopiperidinyl or pyridinyl;
R¹ is hydrogen, loweralkyl or carbethoxymethyl;
R² is hydrogen, loweralkyl or cycloalkyl, phenyl or phenyl-loweralkyl;
R³ 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 R⁴ loweralkyl group, or R¹ may form methylene or -CH₂-C(O)- bridges with R⁴;
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:
其中 Z 是吡咯烷基、哌啶基、均哌啶基或吡啶基;
R¹ 是氢、低级烷基或碳氧甲基;
R² 是氢、低级烷基或环烷基、苯基或苯基-低级烷基;
R³ 是 1 或 2-萘基、2,3-二氢茚-4 或 5-基、苯基或被低级烷基、低级烷氧基、卤素、三氟甲基、苯基、亚甲基二氧基、硝基、氨基、低级烷基氨基、稀释低级烷基氨基、低级酰基氨基取代的苯基;
2-吡咯烷基、2-哌啶基或 2-高哌啶基的 1-位可被 R⁴ 低烷基取代,或 R¹ 可与 R⁴ 形成亚甲基或-CH₂-C(O)-桥;
其药学上可接受的盐和非对映异构体,这些化合物在动物体内具有抗心律失常和/或降血压活性。