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US 5,347,050 AGranted
3-aminopropoxyphenyl derivatives, their preparation and pharmaceutical compositions containing them
OwnerRichard Berthold, William J. Louisinventors
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Abstract
The compounds of formula I, ##STR1## wherein the substituents have various significances, and physiologically acceptable hydrolyzable derivatives thereof having the hydroxy group in the 2 position of the 3-aminopropoxy side chain in esterified form, are useful as cardioselective .beta.-adrenoceptor blocking agents.
Claims7
A compound of formula I ##STR49## wherein R is alkyl, alkenyl, cycloalkyl, cycloalkylalkyl or optionally substituted aryl, aralkyl or aralkenyl,
- R.sub.1 is hydrogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, alkylthio of 1 to 4 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, halogen of atomic number of from 9 to 53, trifluoromethyl, pyrrol-1-yl, cyano, carbamoyl, alkenyl of 2 to 5 carbon atom, alkenyloxy of 3 to 5 carbon atoms wherein the double bond is not attached to the carbon atom adjacent to the oxygen atom, alkanoyl of 2 to 5 carbon atoms, nitro, amino, alkanoylamino of 1 to 5 carbon atoms or alkoxycarbonylamino of 1 to 4 carbon atoms in the alkoxy moiety thereof,
- R.sub.2 is hydrogen or has the significance indicated above for R,
- A is alkylene,
- X is a bond
- Y is an oxygen or a sulfur atom and either Z is an oxygen atom and n is 2 or 3 or Z is a bond and n is 1, 2 or 3,
- with the provisos that
- when R.sub.2 is cycloalkylalkyl and R is alkyl then R.sub.1 is other than hydrogen,
- and when R.sub.2 is hydrogen, then Z is an oxygen atom,
- or physiologically acceptable hydrolyzable derivative thereof having the hydroxy group in the 2 position of the 3-aminopropoxy side chain in esterified form,
- or a pharmaceutically acceptable salt form thereof.
7 more elements
Dependencies are inferred from the claim text.