Patent ES-8602623-A1 (ES)
Title: Para-substituted 3-phenoxy-1-carbonylaminoalkylamino-propan-2-ols having beta receptor blocking properties.
IPC: A61K31/535
Filed: 1984-09-01
Abstract: 3-(p-Alkoxyethoxyphenoxy) -2-hydroxy-N-(carbamoylaminoalkyl) propylamine derivs. of formula (I) and their salts are new. In (I) R1 is H, 1-5C alkyl, 3-6C cycloalkyl or 4-6C cycloalkylalkyl; R2 is H, F, Cl or Br; n is 2, 3 or 4; R3 and R4 are H, 1-4C alkyl, 1-4C hydroxy alkyl or 2-4C alkoxyalkyl; or NR3R4 is morpholino; R5 is H or a splitable acyl gp; and R6 and R7 are H or a splitable acyl or acyloxyalkyl gp. Provided that when one of R3 and R4 is H, then (a) the other is H or (b) the other is Me and n is 2, R1 is H, Et or iPr and R2 is H, or (c) the other is methoxyethyl, n is 2, R1 is iPr and R2 is H. - Cpds. (I) are beta-receptor blocking agents, useful for treating cardiac disorders such as essential hypertension and angina pectoris; they have a selective affinity for beta 1-adrenoceptors and a certain degree of intrinsic activity on cardiac beta-adrenoceptors. Dose is 20-500 mg daily perorally or 10-200 mg daily intravenously. EPAB- EP--85286 B A compound of the formula (I) or a pharmaceutically acceptable salt thereof, in which formula R1 is H, a straight or branched alkyl group containing 1-5 carbon atoms, a cycloalkyl group containing 3-6 carbon atoms, or a cycloalkylalkyl group containing 4-6 carbon atoms; R2 is H, Cl, Br, or F; n is 2, 3 or 4; R3 and R4 are the same or different and each an alkyl group containing 1-4 carbon atoms, a hydroxyalkyl group containing 1-4 carbon atoms, an alkoxyalkyl group containing 2-4 carbon atoms in total, or R3 and R4 are both H or R3 and R4 together with the adjacent nitrogen atom form a morpholino group.  (70pp)s GBAB- GB2111500 B 3-(p-Alkoxyethoxyphenoxy) -2-hydroxy-N-(carbamoylaminoalkyl) propylamine derivs. of formula (I) and their salts are new. In (I) R1 is H, 1-5C alkyl, 3-6C cycloalkyl or 4-6C cycloalkylalkyl; R2 is H, F, Cl or Br; n is 2, 3 or 4; R3 and R4 are H, 1-4C alkyl, 1-4C hydroxy alkyl or 2-4C alkoxyalkyl; or NR3R4 is morpholino; R5 is H or a splitable acyl gp; and R6 and R7 are H or a splitable acyl or acyloxyalkyl gp. Provided that when one of R3 and R4 is H, then (a) the other is H or (b) the other is Me and n is 2, R1 is H, Et or iPr and R2 is H, or (c) the other is methoxyethyl, n is 2, R1 is iPr and R2 is H. - Cpds. (I) are beta-receptor blocking agents, useful for treating cardiac disorders such as essential hypertension and angina pectoris; they have a selective affinity for beta 1-adrenoceptors and a certain degree of intrinsic activity on cardiac beta-adrenoceptors. Dose is 20-500 mg daily perorally or 10-200 mg daily intravenously. (25pp) USAB- US4636501 A p-Substd.3-phenoxy-1-carbonyl aminoalkylamino-propanol cpds. of formula (I) and salts are new. In (I), R1 is H, 1-5C alkyl, 3-6C cycloalkyl or 4-6C cycloalkylalkyl; R2 is H; n is 2,3 or 4; R3 and R4 together with attached N form morphilino. - Esp. cpds. include N-(2-((2-hydroxy-3- (4-(2-methoxyethoxy)phenoxy) propyl)amino)ethyl) -4-morpholinecarboxamide.  (I) may be prepd. e.g. by reacting (II) or (IIa) with H2NR, in which R6 is -CH2CH2OCH2R1 and R7 is (CH2)n-NHC(O)NR3R4.