申请人:Sterling Drug Inc.
公开号:US04317909A1
公开(公告)日:1982-03-02
1,3-Dihydro-3-R-5-PY-2H-imidazo[4,5-b]pyridin-2-ones or 2-thiones of pharmaceutically-acceptable acid-addition salts thereof, which are useful as cardiotonic agents, where R is 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, and PY is 4- or 3-pyridinyl or 4- or 3-pyridinyl having one or two lower-alkyl substituents, are prepared by reacting a 3-amino-2-RNH-6-PY-pyridine with urea or carbonyldiimidazole to produce said -2-ones or with an alkali metal xanthate, thiourea or thiocarbonyldiimidazole to produce said -2-thiones. Also shown is the preparation of the intermediate 3-amino-2-RNH-6-PY-pyridines.
1,3-二氢-3-R-5-PY-2H-咪唑[4,5-b]吡啶-2-酮或其药学上可接受的酸加成盐的2-硫酮,可用作心力衰竭药物。其中R为氢,低碳基,低羟基碳基,2,3-二羟基丙基,低碳氧基碳基或Y-NB,其中Y为低碳链烷基,NB为二(低碳基)氨基或4-吗啡啉基,PY为4-或3-吡啶基或带有一个或两个低碳基取代基的4-或3-吡啶基。该化合物可以通过将3-氨基-2-RNH-6-PY-吡啶与尿素或羰基二咪唑反应制备出-2-酮或与碱性金属黄原酸酯,硫脲或硫代羰基二咪唑反应制备出-2-硫酮。还展示了中间体3-氨基-2-RNH-6-PY-吡啶的制备方法。