1-Phenoxy-2-hydroxy-3-substd. aminopropane derivs. - useful as beta and alpha adrenergic blockers

摘要

(A)Aminopropoxybenzene derivs. of formula (I) are new. where R is phenyl opt. substd. by 1-3 fluoro, chloro, bromo, or 1-4C alkyl or alkoxy. R1 is H, fluoro-chloro, bromo, 1-4C alkyl, alkoxy, or alkylthio, 3-7C cycloalkyl, 1-5C alkanoyl, trifluoro-methyl, 1-pyrrolyl, cyano, carbamoyl, 2-5C alkenyl or 3-5C alkenyloxy (the double bond is not alpha to the oxygen). R2 is 1-4C alkyl, 3-7C cycloalkyl, 3-7C cycloalkyl (1-4C) alkyl, phenyl or 7-10C phenalkyl; the phenyl ring is opt. substd. as for R. A is 2-5C alkylene. X is a bond O or S, Y is O or S. Z is O (and n is then 2 or 3) or a bond (and n is then 1-3). (B) Phenols of formula (IVa) including their hydroxy-protected derivs. are new. where (R" is as R2 except for cycloalkylalkyl.S (I) are beta-adrenergic blockers and some also alpha-adrenergic blockers, with better cardioselectivity then known cpds. They are useful for treating e.g. angina pectons; myocardial infarct; hypertension,; migraine; glaucoma, thyreotoxicosis or arrythmia. The usual oral dose is 10-500 mg per day.