申请人:Sterling Drug Inc.
公开号:US04294836A1
公开(公告)日:1981-10-13
1,3-Dihydro-3-R-5-PY-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 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2-硫酮或其药用可接受的酸加成盐,其中R是氢,低级烷基,低级羟基烷基,2,3-二羟基丙基,低级烷氧基烷基或Y-NB,其中Y是低级亚烷基,NB是二(低级烷基)氨基或4-吗啡啉基,PY是4-或3-吡啶基或具有一个或两个低级烷基取代基的4-或3-吡啶基,通过将3-氨基-2-RNH-6-PY-吡啶与尿素或碳酰二咪唑反应来制备所述的-2-酮,或与碱金属黄酸盐、硫脲或硫代碳酰二咪唑反应来制备所述的-2-硫酮。还展示了中间体3-氨基-2-RNH-6-PY-吡啶的制备方法。