| 摘要 |
Physiologically-acceptable substituted 1,2-ethylenediamines and 1,3-propylenediamines, in free-base and in acid-addition-salt form, have highly pronounced and cardioselective beta -adrenolytic action, antiarrhythmic action and hypotensive action on administration to humans. The diamines are, more specifically, N-[3-aryloxy-2-hydroxypropyl]-N'-[1,3-(di-R3)-2,4-dioxypyrimid-6-yl] (ethylene or propylene)diamines wherein R3 is -H or lower alkyl and the aryl nucleus is either further unsubstituted, further monosubstituted or further disubstituted. The compounds are prepared, e.g, by reacting a corresponding N-[3-phenoxy-2-hydroxypropyl] (ethylene or propylene)diamine with a corresponding 6-chloropyrimidine-2,4-dione in a suitable medium containing an acid-binding agent. Such compounds are administered orally or parenterally in effective, but substantially non-toxic, doses either in substantially pure form, in virtually any standard dosage form or in combination with one or more other pharmacologically- and chemically-compatible drugs. |
