申请人:Ciba-Geigy Corporation
公开号:US04882339A1
公开(公告)日:1989-11-21
Disclosed are compounds of the formula ##STR1## wherein R.sub.1 represents unsubstituted or lower alkyl-substituted C.sub.3 -C.sub.7 -cycloalkyl, unsubstituted or lower alkyl substituted C.sub.7 -or C.sub.8 -bicycloalkyl, unsubstituted or lower alkyl-substituted adamantyl, 4-piperidinyl or N-lower alkyl or aryl-lower alkyl-substituted piperidinyl, 1- or 2-indanyl, 1- or 2-tetrahydronaphthyl, 1- or 2-perhydroindanyl, 1- or 2-perhydronaphthyl; R.sub.2 represents hydrogen, lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl, aryl-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl-lower alkyl, lower alkanoyl or aryl-lower alkanoyl; or R.sub.1 and R.sub.2 combined with the nitrogen to which they are attached represent pyrrolidino, piperidino, perhydroazepino, morpholino, thiomorpholino, tetrahydro- or perhydro-(isoquinolinyl or quinolinyl), dihydro- or perhydroindolyl, piperazino or N-lower alkyl-piperazino; R.sub.3 represents hydrogen, lower alkyl, halogen or lower alkoxy; pharmaceutically acceptable ester and ether derivatives thereof; and pharmaceutically acceptable acid-addition salts of any said basic compounds of formula I and derivatives thereof; as 5-lipoxygenase inhibitors.
公开的化合物具有以下式子:##STR1## 其中,R.sub.1代表未取代或取代较低烷基的C.sub.3-C.sub.7-环烷基,未取代或取代较低烷基的C.sub.7-或C.sub.8-双环烷基,未取代或取代较低烷基的金刚烷基,4-哌啶基或N-较低烷基或芳基-较低烷基取代的哌啶基,1-或2-茚基,1-或2-四氢萘基,1-或2-过氢基茚基,1-或2-过氢基萘基;R.sub.2代表氢,较低烷基,C.sub.3-C.sub.7-环烷基,芳基-较低烷基,C.sub.3-C.sub.7-环烷基-较低烷基,较低烷酰基或芳基-较低烷酰基;或R.sub.1和R.sub.2与它们附着的氮结合表示吡咯啉基,哌啶基,过氢氮杂环基,吗啉基,硫代吗啉基,四氢-或过氢-(异喹啉基或喹啉基),二氢-或过氢吲哚基,哌嗪基或N-较低烷基-哌嗪基;R.sub.3代表氢,较低烷基,卤素或较低烷氧基;以及其药学上可接受的酯和醚衍生物;以及任何式I和其衍生物的药学上可接受的酸加合盐;作为5-脂氧合酶抑制剂。