申请人:Sterling Drug Inc.
公开号:US04374141A1
公开(公告)日:1983-02-15
Shown is a process for preparing cardiotonically active 1,3-dihydro-3-R-6-PY-5-Q-2H-imidazo[4,5-b]pyridin-2-ones, where Q is hydrogen or lower-alkyl, R is lower-alkyl, lower-hydroxyalkyl, 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 substituents, by reacting a 2-RNH-5-PY-6-Q-nicotinamide with an alkali metal hypohalite. Also shown are cardiotonic compositions and a method for increasing cardiac contractility using 2-RR'N-5-PY-6-Q-nicotinamides or pharmaceutically acceptable acid-addition salts thereof, where R' is hydrogen or methyl. Also shown is the process for preparing said 2-RR'N-5-PY-6-Q-nicotinamides by reacting a 2-halo-5-PY-6-Q-nicotinamide with an amine of the formula RR'NH.
所示的是一种制备心力活性1,3-二氢-3-R-6-PY-5-Q-2H-咪唑[4,5-b]吡啶-2-酮的过程,其中Q是氢或低烷基,R是低烷基,低羟基烷基,低烷氧基烷基或Y-NB,其中Y是低烷基烯和NB是双-(低烷基)氨基或4-吗啉基,PY是4-或3-吡啶基或带有一个或两个取代基的4-或3-吡啶基,通过将2-RNH-5-PY-6-Q-烟酰胺与碱金属次氯酸盐反应来实现。还显示了心力活性组合物和一种利用2-RR'N-5-PY-6-Q-烟酰胺或其药用可接受的酸盐增加心脏收缩力的方法,其中R'是氢或甲基。还显示了通过将2-卤代-5-PY-6-Q-烟酰胺与RR'NH式胺反应制备所述2-RR'N-5-PY-6-Q-烟酰胺的过程。