公开(公告)号：US5679703A

公开(公告)日：1997-10-21

申请号：US523843

申请日：1995-09-07

申请人： Masashi Yanase ,  Toshiaki Kumazawa ,  Shiro Shirakura ,  Eiko Oishi ,  Koji Yamada

发明人： Masashi Yanase ,  Toshiaki Kumazawa ,  Shiro Shirakura ,  Eiko Oishi ,  Koji Yamada

IPC分类号： C07C275/28 ,  C07D313/12 ,  A61K31/335 ,  A61K31/38 ,  C07D337/12

CPC分类号： C07C275/28 ,  C07D313/12 ,  C07C2103/32

摘要： 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.

摘要翻译： 公开了由式（I）表示的三环化合物：其中X 1 -X 2表示CH = CH-CH = CH，CH = CH-CH = N或S-CH = CH; Y-Z表示CH 2 -O或CH 2 -S; 那么L-M表示C = CR9（其中R9表示氢或低级烷基）或CH-CR10R11（其中R10和R11各自独立地表示氢或低级烷基）; W表示NR4（其中R4表示氢或低级烷基）或O; R 1，R 2和R 3各自独立地表示氢，低级烷基，低级烷氧基，卤素，硝基，氨基或单或二低级烷基取代的氨基; R5代表氢或低级烷基; R 6，R 7和R 8各自独立地表示氢，卤素，低级烷基或低级烷氧基; 条件是当YZ表示CH = CH或CH 2 CH 2时，LM表示C = CR 9（其中R9具有与上述相同的含义）或CH-CR10aR11a（其中R10a和R11a各自表示R10和R11的低级烷基） ; 和其药学上可接受的盐。 该化合物及其盐具有ACAT抑制活性，预期对高脂血症和动脉硬化具有预防和治疗作用。