发明公开
- 专利标题: Optically active thienotriazolodiazepine compounds
- 专利标题(中): 光学活性thienotriazolodiazepine化合物
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申请号: EP91117375.5申请日: 1991-10-11
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公开(公告)号: EP0480455A1公开(公告)日: 1992-04-15
- 发明人: Moriwaki, Minoru , Yuasa, Syuji , Kitani, Hiroyuki , Terasawa, Michio
- 申请人: YOSHITOMI PHARMACEUTICAL INDUSTRIES, LTD.
- 申请人地址: 6-9, Hiranomachi 2-chome Chuo-ku Osaka-shi Osaka 541 JP
- 专利权人: YOSHITOMI PHARMACEUTICAL INDUSTRIES, LTD.
- 当前专利权人: YOSHITOMI PHARMACEUTICAL INDUSTRIES, LTD.
- 当前专利权人地址: 6-9, Hiranomachi 2-chome Chuo-ku Osaka-shi Osaka 541 JP
- 代理机构: VOSSIUS & PARTNER
- 优先权: JP274451/90 19901012; JP214512/91 19910731
- 主分类号: C07D495/04
- IPC分类号: C07D495/04 ; A61K31/55
摘要:
Stable crystals of an acid addition salt of an optically active thienotriazolodiazepine compound or its hydrate of the formula
wherein R 1 is hydrogen, R 2 is 2-phenylethyl substituted by alkyl having 1 to 5 carbon atoms, 2-morpholinocar- bonylethyl or alkyl having 6 to 12 carbon atoms, or R 1 and R 2 may combinedly form a saturated 5-membered ring having one substituent selected from the group consisting of morpholinomethyl, morpholinocarbonyl and N,N-dipropylcarbamoyl, R 3 is halogen, alkyl having 1 to 5 carbon atoms or alkoxy having 1 to 5 carbon atoms, R 4 is trifluoromethyl or alkyl having 1 to 5 carbon atoms, R 5 is hydrogen or methyl, m is 1-2, and n is 0-2. The present invention provides optically active thienotriazolodiazepine compounds having strong PAF-antagonistic activity as markedly stable crystals which are excellent in crystalline property, permit purification by recrystallization, and have high chemical purity and optical purity, thereby rendering industrial large-scale synthesis attainable. In addition, crystallization thereof facilitates medicinal standardization and pharmaceutical formulation.
wherein R 1 is hydrogen, R 2 is 2-phenylethyl substituted by alkyl having 1 to 5 carbon atoms, 2-morpholinocar- bonylethyl or alkyl having 6 to 12 carbon atoms, or R 1 and R 2 may combinedly form a saturated 5-membered ring having one substituent selected from the group consisting of morpholinomethyl, morpholinocarbonyl and N,N-dipropylcarbamoyl, R 3 is halogen, alkyl having 1 to 5 carbon atoms or alkoxy having 1 to 5 carbon atoms, R 4 is trifluoromethyl or alkyl having 1 to 5 carbon atoms, R 5 is hydrogen or methyl, m is 1-2, and n is 0-2. The present invention provides optically active thienotriazolodiazepine compounds having strong PAF-antagonistic activity as markedly stable crystals which are excellent in crystalline property, permit purification by recrystallization, and have high chemical purity and optical purity, thereby rendering industrial large-scale synthesis attainable. In addition, crystallization thereof facilitates medicinal standardization and pharmaceutical formulation.
公开/授权文献
- EP0480455B1 Optically active thienotriazolodiazepine compounds 公开/授权日:1997-01-22
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