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    • 7. 发明授权
    • 4,5-dihydro-6-(substituted)phenyl-5-methyl-3-(2H)-pyridazinones and
pharmaceutical compositions containing the compounds as active
components
    • 4,5-二氢-6-(取代的)苯基-5-甲基-3-(2H) - 哒嗪酮和含有这些化合物作为活性成分的药物组合物
    • US4717730A
    • 1988-01-05
    • US446797
    • 1982-12-03
    • Ila SircarJames A. Bristol
    • Ila SircarJames A. Bristol
    • C07D403/10A61K31/50
    • C07D403/10
    • A novel method of producing 4,5-dihydro-6-(substituted)phenyl-5-methyl-3(2H)-pyridazinone compounds and the corresponding pharmaceutically acceptable salt compounds is provided as well as pharmaceutical compositions containing one or more of the compounds as active components of the compositions for their pharmacological activity, particularly their cardiotonic and/or antihypertensive activity.Said 5-methylpyridazinone compounds have greatly improved cardiotonic activity in vivo that causes, for example, 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 a stepwise procedure in which one reacts a substituted morpholineacetonitrile with crotononitrile to obtain the corresponding 4-(substituted)-.beta.-methyl.gamma.-oxobenzenebutanoic acid and reacts the latter acid with hydrazine to provide the 4,5-dihydro-6-(substituted)phenyl-5-methyl-3(2 ,uns/H/ )-pyridazinone product.
    • 提供了产生4,5-二氢-6-(取代的)苯基-5-甲基-3(2H) - 哒嗪酮化合物和相应的药学上可接受的盐化合物的新方法以及含有一种或多种化合物的药物组合物 作为其药理学活性的组合物的活性组分,特别是其强心剂和/或抗高血压活性。 所述5-甲基哒嗪酮化合物在体内的强心剂活性大大改善,导致例如狗中心肌收缩力的显着增加。 所述化合物还引起自发性高血压大鼠血压降低。 所述化合物通过逐步方法制备,其中使取代的吗啉乙腈与巴豆腈反应得到相应的4-(取代的)-β-甲基γ-氧苯丁酸,并使后者与肼反应,得到4,5-二氢 - 6-(取代的)苯基-5-甲基-3(2 + E,脱/ H - ) - 哒嗪酮产物。