首页> 外国专利> 1,3-Dihydro-6-(pyridinyl)-2H-imidazo 4,5-b!pyridin-2-ones and - imidazo 4, 5-b!pyridine-2-thiones and their cardiotonic use

1,3-Dihydro-6-(pyridinyl)-2H-imidazo 4,5-b!pyridin-2-ones and - imidazo 4, 5-b!pyridine-2-thiones and their cardiotonic use

机译:1,3-二氢-6-(吡啶基)-2H-咪唑4,5-b!吡啶-2-酮和-咪唑4,5-b!吡啶-2-硫酮及其强心剂的用途

摘要

1,3-Dihydro-1-R.sub.1 -3-R.sub.3 -6-PY-5-Q-2H-imidazo 4,5- b!pyridin-2- ones or -2-thiones or pharmaceutically-acceptable acid- addition salts thereof, which are useful as cardiotonic agents, where Q is hydrogen or lower- alkyl, R.sub.1 and R.sub.3 are each hydrogen, lower- alkyl, lower- hydroxyalkyl, 2,3-dihydroxypropyl, lower-alkoxyalkyl or Y- NB where Y is lower-alkylene and NB is di-(lower-alkyl)amino or 4- morpholinyl, at least one of R.sub.1 and R.sub.3 being hydrogen, and PY is 4- or 3-pyridinyl or 4- or 3-pyridinyl having one or two substituents, are prepared by reacting a 2-R.sub.3 NH-3-R.sub. 1 NH-5-PY-6-Q-pyridine with urea or carbonyldiimidazole to produce said -2- one or with an alkali metal xanthate, thiourea or thiocarbonyldiimidazole to produce said -2- thione. Also shown and claimed are cardiotonic compositions and a method for increasing cardiac contractility using said cardiotonic agents. Also shown are processes for preparing said intermediate 2-R.sub.3 NH-3-R.sub. 1 NH-5-PY-6-Q-pyridines and other intermediates used in said processes.
机译:1,3-二氢-1-R.sub.1 -3-R.sub.3 -6-PY-5-Q-2H-咪唑基4,5- b!吡啶-2--2-或-2-硫酮或可以用作强心药的其药学上可接受的酸加成盐,其中Q为氢或低级烷基,R 1和R 3分别为氢,低级烷基,低级羟烷基,2, 3-二羟丙基,低级烷氧基烷基或Y-NB,其中Y为低级亚烷基且NB为二(低级烷基)氨基或4-吗啉基,R 1和R 3中的至少一个为氢PY是通过使2-R 3 NH-3-R 3反应而制备的具有一个或两个取代基的4-或3-吡啶基或4-或3-吡啶基。 1 NH-5-PY-6-Q-吡啶与尿素或羰基二咪唑生成所述-2-一或与碱金属黄药,硫脲或硫代羰基二咪唑生成所述-2-硫酮。还显示并要求保护的是强心剂组合物和使用所述强心剂增加心脏收缩力的方法。还显示了制备所述中间体2-R 3 NH-3-R 3的方法。 1 NH-5-PY-6-Q-吡啶和所述方法中使用的其他中间体。

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