申请人:Sterling Drug Inc.
公开号:US04331672A1
公开(公告)日:1982-05-25
2-[R.sub.1 NHN(R)]-3-Q'-5-Py-6-Q-pyridines or pharmaceutically-acceptable acid-addition salts thereof are useful as cardiotonic agents, where Q is hydrogen or lower-alkyl, PY is 4- or 3-pyridinyl or 4- or 3-pyridinyl having one or two lower-alkyl substituents, Q' is hydrogen or halo, R is hydrogen, lower-alkyl or lower-hydroxyalkyl, and R.sub.1 is hydrogen or when R is other than hydrogen R.sub.1 is the same as R. These compounds are prepared by reacting a 2-halo-3-Q'-5-PY-6-Q-pyridine with R.sub.1 NHNHR where 2-halo is bromo or chloro. Also shown are: the use of said 2-[R.sub.1 NN(R)]-3-Q'-5-PY-6-Q-pyridines as cardiotonic agents; and, the intermediates, 2,3-dihalo-5-PY-6-Q-pyridines, and their preparation from 3-nitro-5-PY-6-Q-2(1H)-pyridinones.
2-[R.sub.1 NHN(R)]-3-Q'-5-Py-6-Q-吡啶或其药学上可接受的酸盐是作为心脏强心剂有用的化合物,其中Q为氢或较低的烷基,PY为4-或3-吡啶基或具有一个或两个较低的烷基取代基的4-或3-吡啶基,Q'为氢或卤素,R为氢、较低的烷基或较低的羟基烷基,而R.sub.1为氢或当R不是氢时,R.sub.1与R相同。这些化合物是通过将2-卤代-3-Q'-5-PY-6-Q-吡啶与R.sub.1 NHNHR反应制备的,其中2-卤代为溴或氯。还显示了:所述2-[R.sub.1 NN(R)]-3-Q'-5-PY-6-Q-吡啶作为心脏强心剂的用途;以及中间体2,3-二卤代-5-PY-6-Q-吡啶和它们从3-硝基-5-PY-6-Q-2(1H)-吡啶酮的制备。