3-AMINOPROPYLOXYPHENYL DERIVATIVES, THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

摘要

PCT No. PCT/AU85/00063 Sec. 371 Date Nov. 21, 1985 Sec. 102(e) Date Nov. 21, 1985 PCT Filed Mar. 28, 1985 PCT Pub. No. WO85/04403 PCT Pub. Date Oct. 10, 1985. I wherein (A) R is O(CH2)2O-R3 and (a) R1 and R5 are hydrogen and R3 is n-propyl, isobutyl, cyclopentylmethyl, benzyl or 2-(p-fluorophenyl)ethyl; (b) R1 is fluorine and R5 is hydrogen and R3 is n-propyl; (c) R1 is methyl and R5 is hydrogen and R3 is cyclopropylmethyl; (d) R1 is cyano and R5 is hydrogen and R3 is n-propyl; (e) R1 is hydrogen, R5 is methyl and R3 is alkyl of 2 to 5 carbon atoms, cycloalkylmethyl of 5 to 7 carbon atoms in the cycloalkyl part thereof or -(CH2)n-R' wherein n is 0, 1 or 2 and R' is phenyl or monofluorophenyl; or (B) R is hydroxy, R1 is fluorine and R5 is hydrogen, and their physiologically hydrolysable derivatives, in which at least one hydroxy group is in esterified form, and their salts, elicit highly cardioselective beta 1 adrenoceptor blockade, and in most cases cardiospecific blockade, and relevant cardiotonic activity. These compounds can be used as therapeutic agents. One obtains these compounds by 3-amino-2-oxypropylation of the respective substituted phenol.