申请人:Sterling Drug Inc.
公开号:US04276293A1
公开(公告)日:1981-06-30
2-R.sub.2 -3-R.sub.3 -6-PY-5-Q-3H-imidazo[4,5-b]pyridines (I) or 1-R.sub.1 -2-R.sub.2 -6-PY-5-Q-1H-imidazo[4,5-b]pyridines (IA) or pharmaceutically-acceptable acid-addition salts thereof, where Q and R.sub.2 are each 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 having at least two carbon atoms between its connecting linkages and NB is di-(lower-alkyl)amino or 4-morpholinyl, at least one of R.sub.1 or R.sub.3 being hydrogen, and PY is 4- or 3-pyridinyl or 4- or 3-pyridinyl having one or two lower-alkyl substituents, which are useful as cardiotonics, are prepared by reacting 2-R.sub.3 NH-3-R.sub.1 NH-5-PY-6-Q-pyridine (II) with a tri-(lower-alkyl) ortho-(lower-alkanoate). Also shown are: the use of I or IA or salts in cardiotonic compositions and a method for increasing cardiac contractility; and, the preparation of the intermediates II, as well as intermediates used to prepare II.
2-R.sub.2 -3-R.sub.3 -6-PY-5-Q-3H-咪唑并[4,5-b]吡啶(I)或1-R.sub.1 -2-R.sub.2 -6-PY-5-Q-1H-咪唑并[4,5-b]吡啶(IA)或其药用可接受的酸盐,其中Q和R.sub.2分别为氢或低烷基,R.sub.1和R.sub.3分别为氢、低烷基、低羟基烷基、2,3-二羟基丙基、低烷氧基烷基或Y-NB,其中Y为至少在其连接链之间具有两个碳原子的低烷基,NB为二(低烷基)氨基或4-吗啉基,R.sub.1或R.sub.3中至少一个为氢,PY为4-或3-吡啶基或带有一个或两个低烷基取代基的4-或3-吡啶基,这些化合物可用作心力衰竭药物,通过将2-R.sub.3 NH-3-R.sub.1 NH-5-PY-6-Q-吡啶(II)与三(低烷基)邻-(低烷酸酯)反应制备。还显示了:在心力衰竭药物组合物中使用I或IA或盐以及增加心脏收缩力的方法;以及用于制备II的中间体II的制备,以及用于制备II的中间体。