Organic compounds -- part of the class 532-570 series – Organic compounds – Four or more ring nitrogens in the bicyclo ring system
Patent
1978-05-02
1980-08-05
Jiles, Henry R.
Organic compounds -- part of the class 532-570 series
Organic compounds
Four or more ring nitrogens in the bicyclo ring system
544310, 544312, 42424854, 424251, C07D41312, C07D23954
Patent
active
042163145
ABSTRACT:
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-R.sup.3)-2,4-dioxypyrimid-6-yl] (ethylene or propylene)diamines wherein R.sup.3 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.
REFERENCES:
patent: 3852291 (1974-12-01), Augstein et al.
patent: 4020071 (1977-04-01), Raabe et al.
Grawinger Otto
Raabe Thomas
Scholtholt Josef
Schraven Eckhard
Cassella Farbwerke Mainkur Aktiengesellschaft
Jiles Henry R.
Ramsuer R. W.
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