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1. 发明授权

US5679703A Tricyclic compounds having ACAT inhibiting activity 失效
标题翻译：具有ACAT抑制活性的三环化合物
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。

2. 发明授权

US5340807A Tricyclic compounds and intermediates thereof 失效
标题翻译：三环化合物及其中间体
公开(公告)号：US5340807A
公开(公告)日：1994-08-23
申请号：US989906
申请日：1992-12-11
申请人： Toshiaki Kumazawa , Masashi Yanase , Hiroyuki Harakawa , Hiroyuki Obase , Shoji Oda , Shiro Shirakura , Koji Yamada , Kazuhiro Kubo
发明人： Toshiaki Kumazawa , Masashi Yanase , Hiroyuki Harakawa , Hiroyuki Obase , Shoji Oda , Shiro Shirakura , Koji Yamada , Kazuhiro Kubo
IPC分类号： A61K31/335 , A61K31/165 , A61K31/18 , A61K31/19 , A61K31/215 , A61K31/235 , A61K31/275 , A61K31/38 , A61K31/435 , A61K31/44 , A61K31/55 , A61P3/06 , A61P9/10 , A61P43/00 , C07C233/65 , C07C235/46 , C07C235/48 , C07C237/40 , C07C323/40 , C07C323/62 , C07C327/26 , C07C331/08 , C07D221/16 , C07D223/20 , C07D233/58 , C07D313/12 , C07D337/12 , C07D471/04 , C07D491/04 , C07D491/044 , C07D495/04 , A01N43/46 , C07D273/02 , C07D313/06
CPC分类号： C07D491/04 , C07C233/65 , C07D223/20 , C07D313/12 , C07D337/12 , C07C2103/32 , Y10S514/824
摘要： Disclosed is a tricyclic compound represented by the formula (I): ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represents hydrogen, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, amino, C1-6 alkylamino, halogenated C1-6 alkyl, halogenated C1-6 alkoxy, halogen, nitro, cyano, carboxy, C1-6 alkoxycarbonyl, hydroxymethyl, CR.sup.9 R.sup.10 CO.sub.2 R.sup.11 (wherein each of R.sup.9, R.sup.10 and R.sup.11 independently represents hydrogen or C1-6 alkyl) or CONR.sup.12 R.sup.13 (wherein each of R.sup.12 and R.sup.13 independently represents hydrogen or C1-6 alkyl); R.sup.5 represents hydrogen or C1-6 alkyl; each of R.sup.6, R.sup.7 and R.sup.8 independently represents hydrogen, C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkanoyloxy, C1-6 alkylthio, thiocyanato or halogen; X represents CH or N; Y.sup.1 -Y.sup.2 represents CH.sub.2 --O, CH.sub.2 --(O).sub.n, (wherein n represents 0, 1, or 2), CH.sub.2 CH.sub.2, CH.dbd.CH or CON(R.sup.14) (wherein R.sup.14 represents hydrogen or C1-6 alkyl) and Z represents oxygen or sulfur, or a pharmaceutically acceptable salt thereof. The compound possesses an acyl coenzyme A: cholesterol acyltransferase-inhibiting activity, and thus 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R 1，R 2，R 3和R 4各自独立地表示氢，C 1-6烷基，C 1-6烷氧基，C 1-6烷硫基，氨基， C 1-6烷基氨基，卤代C 1-6烷基，卤代C 1-6烷氧基，卤素，硝基，氰基，羧基，C 1-6烷氧基羰基，羟甲基，CR 9 R 10 CO 2 R 11（其中R 9，R 10和R 11各自独立地表示氢或C 1-6烷基）或CONR 12 R 13（其中R 12和R 13各自独立地表示氢或C 1-6烷基）; R5表示氢或C1-6烷基; R 6，R 7和R 8各自独立地表示氢，C 1-6烷基，羟基，C 1-6烷氧基，C 1-6烷酰氧基，C 1-6烷硫基，氰硫基或卤素; X表示CH或N; Y1-Y2表示CH2-O，CH2-（O）n，（其中n表示0,1或2），CH2CH2，CH = CH或CON（R14）（其中R14表示氢或C1-6烷基）和Z 表示氧或硫，或其药学上可接受的盐。该化合物具有酰基辅酶A：胆固醇酰基转移酶抑制活性，因此预期对高脂血症和动脉硬化具有预防和治疗作用。

3. 发明授权

US5478835A Tricyclic compounds and intermediates thereof 失效
标题翻译：三环化合物及其中间体
公开(公告)号：US5478835A
公开(公告)日：1995-12-26
申请号：US236097
申请日：1994-05-02
申请人： Toshiaki Kumazawa , Masashi Yanase , Hiroyuki Harakawa , Hiroyuki Obase , Shoji Oda , Shiro Shirakura , Koji Yamada , Kazuhiro Kubo
发明人： Toshiaki Kumazawa , Masashi Yanase , Hiroyuki Harakawa , Hiroyuki Obase , Shoji Oda , Shiro Shirakura , Koji Yamada , Kazuhiro Kubo
IPC分类号： A61K31/335 , A61K31/165 , A61K31/18 , A61K31/19 , A61K31/215 , A61K31/235 , A61K31/275 , A61K31/38 , A61K31/435 , A61K31/44 , A61K31/55 , A61P3/06 , A61P9/10 , A61P43/00 , C07C233/65 , C07C235/46 , C07C235/48 , C07C237/40 , C07C323/40 , C07C323/62 , C07C327/26 , C07C331/08 , C07D221/16 , C07D223/20 , C07D233/58 , C07D313/12 , C07D337/12 , C07D471/04 , C07D491/04 , C07D491/044 , C07D495/04 , C07C207/00 , C07C237/00
CPC分类号： C07D491/04 , C07C233/65 , C07D223/20 , C07D313/12 , C07D337/12 , C07C2103/32 , Y10S514/824
摘要： Disclosed is a tricyclic compound represented by the formula (I): ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represents hydrogen, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, amino, C1-6 alkylamino, halogenated C1-6 alkyl, halogenated C1-6 alkoxy, halogen, nitro, cyano, carboxy, C1-6 alkoxycarbonyl, hydroxymethyl, CR.sup.9 R.sup.10 CO.sub.2 R.sup.11 (wherein each of R.sup.9, R.sup.10 and R.sup.11 independently represents hydrogen or C1-6 alkyl) or CONR.sup.12 R.sup.13 (wherein each of R.sup.12 and R.sup.13 independently represents hydrogen or C1-6-alkyl); R.sup.5 represents hydrogen or C1-6 alkyl; each of R.sup.6, R.sup.7 and R.sup.8 independently represents hydrogen, C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkanoyloxy, C1-6 alkylthio, thiocyanato or halogen; X represents CH or N; Y.sup.1 -Y.sup.2 represents CH.sub.2 -O, CH.sub.2 -S(O).sub.n, (wherein n represents 0, 1, or 2), CH.sub.2 CH.sub.2, CH.dbd.CH or CON(R.sup.14) (wherein R.sup.14 represents hydrogen or C1-6 alkyl) and Z represents oxygen or sulfur, or a pharmaceutically acceptable salt thereof. The compound possesses an acyl coenzyme A: cholesterol acyltransferase-inhibiting activity, and thus 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R 1，R 2，R 3和R 4各自独立地表示氢，C 1-6烷基，C 1-6烷氧基，C 1-6烷硫基，氨基， C 1-6烷基氨基，卤代C 1-6烷基，卤代C 1-6烷氧基，卤素，硝基，氰基，羧基，C 1-6烷氧基羰基，羟甲基，CR 9 R 10 CO 2 R 11（其中R 9，R 10和R 11各自独立地表示氢或C 1-6烷基）或CONR 12 R 13（其中R 12和R 13各自独立地表示氢或C 1-6 - 烷基）; R5表示氢或C1-6烷基; R 6，R 7和R 8各自独立地表示氢，C 1-6烷基，羟基，C 1-6烷氧基，C 1-6烷酰氧基，C 1-6烷硫基，氰硫基或卤素; X表示CH或N; Y1-Y2表示CH2-O，CH2-S（O）n，（其中n表示0,1或2），CH2CH2，CH = CH或CON（R14）（其中R14表示氢或C1-6烷基） Z表示氧或硫，或其药学上可接受的盐。该化合物具有酰基辅酶A：胆固醇酰基转移酶抑制活性，因此预期对高脂血症和动脉硬化具有预防和治疗作用。

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