申请人:Leo Pharmaceutical Products Ltd.
公开号:US05157039A1
公开(公告)日:1992-10-20
The present invention relates to compounds of formula ##STR1## in which formula I X stands for O, S, ##STR2## R.sub.1 and R.sub.2 which can be the same or different stand for hydrogen, straight or branched, saturated or unsaturated, unsubstituted or substituted C.sub.1- C.sub.8 -alkyl, aryl or for ar-C.sub.1 -C.sub.4 -alkyl, aryl and ar being unsubstituted or substituted phenyl; R.sub.3, R.sub.4, R.sub.5, and R.sub.6 are the same or different and stand for hydrogen, halogen, pseudo halogen, cyano, nitro, amino, carboxy, hydroxy, alkyl, alkoxy; or R.sub.5 and R.sub.6 form an aromatic ring which is fused to the pyridyl ring, and which aromatic ring may substituted; provided that R.sub.1 and R.sub.2 cannot be hydrogen at the same time, and provided that when R.sub.5 and R.sub.6 both are chlorine and R.sub.1 is hydrogen, then R.sub.2 cannot be n-propyl; and salts and bioreversible derivatives thereof. The compounds of formula I are useful in the human and veterinary therapy, as they exert specific 5-lipoxygenase inhibition.
本发明涉及以下结构的化合物:##STR1## 其中式中 X 代表 O、S、##STR2## R.sub.1 和 R.sub.2 可以相同也可以不同,代表氢、直链或支链、饱和或不饱和、未取代或取代的 C.sub.1-C.sub.8-烷基、芳基或 ar-C.sub.1-C.sub.4-烷基,芳基和 ar 均为未取代或取代的苯基;R.sub.3、R.sub.4、R.sub.5 和 R.sub.6 可以相同也可以不同,代表氢、卤素、伪卤素、氰基、硝基、氨基、羧基、羟基、烷基、烷氧基;或者 R.sub.5 和 R.sub.6 形成与吡啶环融合的芳香环,该芳香环可以被取代;但要求 R.sub.1 和 R.sub.2 不能同时为氢,当 R.sub.5 和 R.sub.6 都是氯且 R.sub.1 是氢时,R.sub.2 不能是 n-丙基;以及其盐和生物可逆衍生物。式中的化合物在人类和兽医治疗中具有特异的5-脂氧酶抑制作用。