Alkylenediamine derivatives and processes for their preparation

Details Alkylenediamine derivatives and processes for their preparation Alkylenediamine derivatives and processes for their preparation

C - Chemistry, Metallurgy

07

D

260/258, 260/245

C07D 265/30 (2006.01) C07D 239/545 (2006.01) C07D 295/00 (2006.01)

Patent

CA 1085842

Abstract of the Disclosure Physiologically-acceptable substituted 1,2-ethylene- diamines 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] (ethyle?e or propylene)diamines wherein R3 is -H or lower alkyl and the aryl nucleus is either further unsubstituted, further monosubstituted or further disubsti- tuted. The compounds are prepared e.g., by reacting a corresponding N-[3-phenoxy-2-hydroxypropyl] (ethylene or propylene)diamine with a corresponding 6-chloropyridine- 2,4-dione in a suitable medium containing an acid-binding agent. Such compounds are administered orally or parenter- ally 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 pharamacologi- cally- and chemically-compatible drugs.

303380

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