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    Optically active thienotriazolodiazepine compounds
    1.
    发明公开
    Optically active thienotriazolodiazepine compounds 失效
    光学活性thienotriazolodiazepine化合物

    公开(公告)号：EP0480455A1

    公开(公告)日：1992-04-15

    申请号：EP91117375.5

    申请日：1991-10-11

    申请人： YOSHITOMI PHARMACEUTICAL INDUSTRIES, LTD.

    发明人： Moriwaki, Minoru ,  Yuasa, Syuji ,  Kitani, Hiroyuki ,  Terasawa, Michio

    IPC分类号： C07D495/04 ,  A61K31/55

    CPC分类号： C07D495/14

    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.

    摘要翻译： 光学活性噻吩并三唑并二氮杂化合物或其水合物的酸加成盐的稳定晶体，其中R1是氢，R2是被具有1-5个碳原子的烷基取代的2-苯基乙基，2-吗啉代乙基乙基或具有6-12个碳原子的烷基 碳原子，或者R1和R2可以结合形成具有一个选自吗啉代甲基，吗啉代羰基和N，N-二丙基氨基甲酰基的取代基的饱和五元环，R3是卤素，具有1至5个碳原子的烷基或具有1个 至5个碳原子，R4是三氟甲基或具有1至5个碳原子的烷基，R5是氢或甲基，m是1-2，并且n是0-2。 本发明提供具有强PAF-拮抗活性的光学活性噻吩并三唑并二氮杂化合物作为结晶性优异，允许通过重结晶纯化，并具有高化学纯度和光学纯度的显着稳定的晶体，从而可实现工业大规模合成。 此外，其结晶促进了药物标准化和药物制剂。