申请人:Kyowa Hakko Kogyo, Co., Ltd.
公开号:US05679703A1
公开(公告)日:1997-10-21
Disclosed is a tricyclic compound represented by formula (I): ##STR1## where X.sup.1 -X.sup.2 represents CH.dbd.CH--CH.dbd.CH, CH.dbd.CH--CH.dbd.N or S--CH.dbd.CH; Y--Z represents CH.sub.2 --O or CH.sub.2 --S; then L--M represents C.dbd.CR.sup.9 (in which R.sup.9 represents hydrogen or lower alkyl) or CH--CR.sup.10 R.sup.11 (in which each of R.sup.10 and R.sup.11 independently represents hydrogen or lower alkyl); W represents NR.sup.4 (in which R.sup.4 represents hydrogen or lower alkyl) or O; each of R.sup.1, R.sup.2 and R.sup.3 independently represents hydrogen, lower alkyl, lower alkoxy, halogen, nitro, amino or mono or di-lower alkyl-substituted amino; R.sup.5 represents hydrogen or lower alkyl; each of R.sup.6, R.sup.7 and R.sup.8 independently represents hydrogen, halogen, lower alkyl or lower alkoxy; provided that when Y--Z represents CH.dbd.CH or CH.sub.2 CH.sub.2, then L--M represents C.dbd.CR.sup.9 (in which R.sup.9 has the same meaning as defined above),or CH--CR.sup.10a R.sup.11a (in which each of R.sup.10a and R.sup.11a represents lower alkyl of R.sup.10 and R.sup.11); and a pharmaceutically acceptable salt thereto. The compound and its salt have an ACAT inhibiting activity and are expected to have preventive and therapeutic effects on hyperlipemia and arteriosclerosis.
本发明公开了一种三环化合物,其化学式表示为(I):##STR1## 其中X.sup.1-X.sup.2表示CH.dbd.CH--CH.dbd.CH,CH.dbd.CH--CH.dbd.N或S--CH.dbd.CH;Y--Z表示CH.sub.2--O或CH.sub.2--S;然后L--M表示C.dbd.CR.sup.9(其中R.sup.9表示氢或低碳基)或CH--CR.sup.10R.sup.11(其中R.sup.10和R.sup.11各自独立地表示氢或低碳基);W表示NR.sup.4(其中R.sup.4表示氢或低碳基)或O;R.sup.1、R.sup.2和R.sup.3各自独立地表示氢、低碳基、低烷氧基、卤素、硝基、氨基或单个或二个低烷基取代的氨基;R.sup.5表示氢或低碳基;R.sup.6、R.sup.7和R.sup.8各自独立地表示氢、卤素、低碳基或低烷氧基;但当Y--Z表示CH.dbd.CH或CH.sub.2CH.sub.2时,L--M表示C.dbd.CR.sup.9(其中R.sup.9的含义与上述相同)或CH--CR.sup.10aR.sup.11a(其中R.sup.10a和R.sup.11a分别表示R.sup.10和R.sup.11的低碳基);以及其药学上可接受的盐。该化合物及其盐具有ACAT抑制活性,预期具有预防和治疗高脂血症和动脉硬化的效果。