Substituted 4,5-dihydro-6-(substituted)-phenyl-3(2H)-pyridazinones and 6-(substituted)phenyl-3(2H)-pyridazinones
申请人:WARNER-LAMBERT COMPANY
公开号:EP0075436A1
公开(公告)日:1983-03-30
Substituted 4,5-dihydro-6-(substituted)-phenyl-3(2H)-pyridazinone compounds and 6-(substituted)phenyl-3(2H)-pyridazinone compounds and pharmaceutically acceptable salts thereof are useful as cardiotonic and antihypertensive agents.
Said compounds cause a significant increase in myocardial contractility in the dog. Said compounds also cause a decrease in blood pressure in the spontaneously hypertensive rat. Said compounds are produced by reacting substituted y-oxobenzene-butanoic acids with suitably substituted hydrazines to provide 4,5-dihydro-6-(substituted)phenyl-3(2H)-pyridazinones which are dehydrogenated to 6-(substituted)phenyl-3(2H)-pyridazinones.
Both the 4,5-dihydro-6-(substituted)-phenyl-3(2H)-pyridazinones and the 6-(substituted)-phenyl-3(2H)-pyridazinones are useful as cardiotonic and antihypertensive agents. The compounds have the formula:
where represents a double or single bond and A is anyone of five types of heterocyclic ring-containing radicals, and R2, R3 and Y are hydrogen or various substituents.
取代的 4,5-二氢-6-(取代)苯基-3(2H)-哒嗪酮化合物和 6-(取代)苯基-3(2H)-哒嗪酮化合物及其药学上可接受的盐类可用作强心剂和降压药。
上述化合物可显著增强狗的心肌收缩力。所述化合物还能降低自发性高血压大鼠的血压。所述化合物是通过取代的 y-氧代苯丁酸与适当取代的肼反应生成 4,5-二氢-6-(取代)苯基-3(2H)-哒嗪酮,后者脱氢生成 6-(取代)苯基-3(2H)-哒嗪酮。
4,5-二氢-6-(取代)苯基-3(2H)-哒嗪酮和 6-(取代)苯基-3(2H)-哒嗪酮均可用作强心剂和降压药。这些化合物的化学式如下
其中代表双键或单键,A 是五种含杂环基中的任何一种,R2、R3 和 Y 是氢或各种取代基。