Novel esters of phenylalkanoic acid.

摘要

The esters of phenylalkanoic acid of the formula: <CHEM> wherein R<1> is 4-10 membered, saturated or unsaturated, mono- or bi-cyclic hetero ring containing as hetero atoms: (i) one or two nitrogen, (ii) two or three of nitrogen and sulfur in total, or (iii) one or two sulfur; R<2> is hydrogen; or R<1> and R<2>, taken together with a nitrogen to which they are attached, form 4-7 membered, saturated or unsaturated, mono-cyclic hetero ring containing as hetero atoms: (i) one or two nitrogen, or (ii) two or three of nitrogen and oxygen in total, the aforementioned hetero rings, represented by R<1> or formed by R<1> and R<2>, taken together with a nitrogen to which they are attached, may be substituted by one substituent selected from C1-4 alkyl and C2-5 acyl; R<3> each, independently, is hydrogen or C1-4 alkyl; R<4> is hydrogen, halogen, trihalomethyl, C1-4 alkyl, C1-4 alkoxyl C2-5 acyl, cyano, nitro or nitroxy; R<5> each, independently, is hydrogen, C1-4 alkyl or phenyl; or the two R<5>'s, taken together with a carbon to which they are attached, form cyclopentane or cyclohexane; and the pharmaceutically acceptable acid addition salts thereof, have beta 1-adrenergic receptor blocking activity, and therefore, are useful for the prevention of and/or in the treatment of cardiovascular diseases such as angina pectoris, myocardial infarction, congestive heart failure, hypertension, arrhythmia, etc.