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    • 6. 发明申请
    • LABELED DRUGS AND NITROXYL COMPOUNDS TO BE USED THEREIN
    • 使用的标签药物和硝基化合物
    • WO99059642A1
    • 1999-11-25
    • PCT/JP1999/002509
    • 1999-05-14
    • A61K49/00A61K49/18A61K49/20A61K51/04C07B59/00C07D211/94A61K51/00
    • C07D211/94A61K49/0002A61K49/18A61K49/20A61K51/0446A61K51/0455A61K51/0497C07B59/00C07B59/002
    • Drugs containing as the active ingredient compounds having a radioactive element and an organic substituent carrying an unpaired electron in a single molecule, for example, labeled nitroxyl compounds represented by general formula (I) wherein L represents -CO- or -alkylene-CO-; R1, R2, R3 and R4 represent each C1-4 alkyl; R5 represents H, C1-4 alkyl, carboxy or lower alkoxycarbonyl; m and k are each 0 or 1; n is from 1 to 4; R6 represents methyl or ethyl; R7 represents H, methyl, ethyl or carboxy; A represents an aromatic ring having a radioactive element; and - - - represents a single or double bond when m is 0, or a single bond when m is 1. Use of these drugs makes it possible to easily obtain data about the spin labeling positions, thus providing a means for obtaining exact data relating to active oxygen or free radicals in vivo as biological images by nuclear magnetic resonance or biological magnetic measurement.
    • 在单分子中含有具有放射性元素和携带不成对电子的有机取代基的化合物的化合物的药物,例如通式(I)表示的标记的硝酰基化合物,其中L表示-CO-或 - 亚烷基-CO-; R1,R2,R3和R4分别代表C1-4烷基; R5表示H,C1-4烷基,羧基或低级烷氧基羰基; m和k分别为0或1; n为1至4; R 6表示甲基或乙基; R7表示H,甲基,乙基或羧基; A表示具有放射性元素的芳环; 而当m为0时, - - - 表示单键或双键,或当m为1时为单键。使用这些药物可以轻松获取有关自旋标记位置的数据,从而提供 通过核磁共振或生物磁测量获得与活性氧或自由基相关的精确数据作为生物学图像的方法。