Chemical compounds containing tocopherol and at least one additional pharmaceutical active substrate
    2.
    发明申请
    Chemical compounds containing tocopherol and at least one additional pharmaceutical active substrate 审中-公开
    含有生育酚的化合物和至少一种另外的药物活性底物

    公开(公告)号:US20060135489A1

    公开(公告)日:2006-06-22

    申请号:US10524147

    申请日:2004-07-01

    CPC分类号: C07D405/12 C07D311/72

    摘要: Compounds in the form of their racemates, enantiomers or diastereomers with general formula I in which R stands for the unchanged portion of a variable pharmaceutical active ingredient molecule, B stands for a spacer, and Toc with the formula and R′, R″ and R′″ are equal to H or methyl stands for tocopherol and A stands for C═X, SOm, X or CH2, whereby X is equal to 0, S or NR1 (when n≧1) or S or NR1 (when n=0), and B means a grouping X—R2—Y with Y equal to C═X, SOm or C(XR3)R4, and n is equal to 0 to 6, and m stands for 1 or 2, whereby R1 stands for H, C1 to C10-alkyl, Het or an aryl or Het radical that is bonded via a C1 to C6-spacer, and whereby R2 is selected from the group alkylene, arylene or Het spacers and combinations thereof, whereby the latter are linked to one another either directly or via radical A or via grouping Xo-A-Xp, whereby o and p are equal to 0, 1 or 2, and the latter can be the same or different, and whereby R3 and R4 stand for H, C1 to C10-alkyl, Het or an aryl or Het radical that is bonded via a C1 to C6 spacer.

    摘要翻译: 其具有通式I的外消旋物,对映异构体或非对映体形式的化合物,其中R表示可变的药物活性成分分子的不变部分,B表示间隔基,且具有式R',R“的Toc和 R“等于H或甲基代表生育酚,A代表CX,SO x,X或CH 2,其中X等于0,S或 NR 1(当n> = 1时)或S或NR 1(当n = 0时),B表示分组XR < Y,Y等于CX,SO m或C(XR 3)R 4,n等于0至6,m 代表1或2,其中R 1代表H,C 1至C 10 - 烷基,Het或芳基或Het基团,其中 通过C 1至C 6 - 间隔键合,由此R 2选自亚烷基,亚芳基或Het间隔基和组合 其中后者直接地或经由基团A或通过分组X