Alkanolamine derivatives of the formula
wherein Ar is phenyl or naphthyl which is unsubstituted or which bears one or two defined substituents, or Ar is certain defined heterocyclic or bicyclic aromatic systems;
wherein R1 is halogen, cyano, trifluoromethyl ortrifluo- romethylthio;
wherein either R2 and R3 each is hydrogen or alkyl, or R2 is hydrogen and R3 is cycloalkyl or cycloakyl-alkyl, or R2 and R3 are joiend to form, together with the adjacent nitrogen atom, a heterocyclic group;
wherein either R4 is hydrogen and R5 is hydrogen or alkyl, or R4 is hydrogen and R5 and R6 are joined together to form alkylene, or R4, R5 and R6 are joined together to form alk-1-yl-ω-ylidene;
wherein either R6 and R7 each is hydrogen or alkyl, or R6 is joined to R4 or to R4 and R5 as defined above and R7 is hydrogen or alkyl, or R6 and R7 are joined together to form alkylene, or one of R6 and R7 is hydrogen or alkyl and the other of R6 and R7 is joined to A as defined below;
and wherein either A is alkylene, cycloakylene or cycloakylene-alkylene, or wherein A together with either R6 and its accompanying nitrogen atom, or R7 and its accompanying nitrogen atom, form pyrrolidine-diyl or piperidine-diyl;
and acid-addition salts thereof; processes for their manufacture and pharmaceutical compositions containing them. The compounds possess β-adrenergic blocking and/ or diuretic activity.
式中的烷醇胺衍
生物
其中 Ar 是未取代的苯基或
萘基,或带有一个或两个确定的取代基,或 Ar 是某些确定的杂环或双环芳香系统;
其中 R1 为卤素、
氰基、三
氟甲基或三
氟甲基
硫代;
其中 R2 和 R3 各为氢或烷基,或 R2 为氢,R3 为环烷基或环烷基-烷基,或 R2 和 R3 与邻近的氮原子共同形成杂环基团;
其中 R4 为氢,R5 为氢或烷基,或 R4 为氢,R5 和 R6 连接形成亚烷基,或 R4、R5 和 R6 连接形成烷-1-基-ω-亚烷基;
其中 R6 和 R7 各自为氢或烷基,或 R6 与 R4 或如上定义的 R4 和 R5 连接,而 R7 为氢或烷基,或 R6 和 R7 连接在一起形成亚烷基,或 R6 和 R7 中的一个为氢或烷基,而 R6 和 R7 中的另一个与如下定义的 A 连接;
其中 A 为亚烷基、环亚烷基或环亚烷基-亚烷基,或其中 A 与 R6 及其伴随的氮原子或 R7 及其伴随的氮原子一起形成
吡咯烷二基或
哌啶二基;
及其酸加成盐;它们的制造工艺和含有它们的药物组合物。这些化合物具有β-
肾上腺素能阻断和/或利尿活性。