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    Xanthines in the 7th position with a benzyl acetic acid moiety
    52.
    发明授权
    Xanthines in the 7th position with a benzyl acetic acid moiety 失效
    第七位的黄嘌呤与苄基乙酸部分

    公开(公告)号：US5714494A

    公开(公告)日：1998-02-03

    申请号：US710503

    申请日：1996-09-18

    申请人： Richard Connell ,  Siegfried Goldmann ,  Ulrich Muller ,  Stefan Lohmer ,  Hilmar Bischoff ,  Dirk Denzer ,  Rudi Grutzmann ,  Stefan Wohlfeil

    发明人： Richard Connell ,  Siegfried Goldmann ,  Ulrich Muller ,  Stefan Lohmer ,  Hilmar Bischoff ,  Dirk Denzer ,  Rudi Grutzmann ,  Stefan Wohlfeil

    IPC分类号： A61K31/52 ,  A61K31/522 ,  A61P9/00 ,  A61P9/10 ,  C07D473/06 ,  C07D473/08 ,  C07D473/22

    CPC分类号： C07D473/06 ,  C07D473/08

    摘要： Substituted xanthines of formula ##STR1## in which A represents a radical of the formula ##STR2## in which R.sup.3, R.sup.4, R.sup.6 and R.sup.7 denote hydrogen, cycloalkyl, aryl having 6 to 10 carbon atoms, or denote straight-chain of branched alkyl or alkenyl, each of which is optionally substituted; T, V, X and Y are identical or different and denote an oxygen or sulphur atom; R.sup.5 and R.sup.8 are identical or different and denote hydrogen, halogen, cycloalkyl having 3 to 8 carbon atoms or straight-chain or branched alkyl or alkenyl in each case having up to 8 carbon atoms, optionally substituted or R.sup.5 and R.sup.8 denote aryl having 6 to 10 carbon atoms or a 5- to 7-membered aromatic, optionally benzo-fused heterocycle having up to 3 heteroatoms S, N and/or O, each of which is optionally substituted; L represents an oxygen or sulphur atom; R.sup.2 represents mercapto, hydroxyl, straight-chain or branched alkoxy having up to 8 carbon atoms or the group of the formula ##STR3## in which R.sup.13 denotes hydrogen or straight-chain or branched alkyl having up to 4 carbon atoms; R.sup.14 denotes hydrogen, phenyl or a 5- to 6-membered aromatic heterocycle having up to 3 heteroatoms S, N and/or O; and R.sup.15 denotes hydrogen or straight-chain or branched alkyl having up to 8 carbon atom, optionally substituted by hydroxyl, and their salts are prepared by reaction of the suitable unsubstituted xanthines with halogenomethylphenylacetic acids and subsequent reaction of the carboxylic esters or acids with phenylglycinolamine. The substituted xanthines are suitable as active compounds in medicaments, in particular in antiatherosclerotic medicaments.

    摘要翻译： 式（I）的取代黄嘌呤其中A表示式为“IMAGE”的基团，其中R 3，R 4，R 6和R 7表示氢，环烷基，具有6至10个碳原子的芳基，或表示直链 支链烷基或烯基，其各自任选被取代; T，V，X和Y相同或不同，表示氧或硫原子; R5和R8相同或不同，表示氢，卤素，具有3-8个碳原子的环烷基或具有至多8个碳原子的直链或支链烷基或链烯基，任选取代或R 5和R 8表示具有6至 10个碳原子或5至7元芳族，任选苯并稠合的杂环，其具有至多3个杂原子S，N和/或O，每个杂原子任选被取代; L表示氧或硫原子; R 2表示具有至多8个碳原子的巯基，羟基，直链或支链烷氧基或式“IMAGE”的基团，其中R13表示氢或具有至多4个碳原子的直链或支链烷基; R14表示氢，苯基或具有至多3个S，N和/或O的杂原子的5至6元芳族杂环; 并且R 15表示氢或具有至多8个碳原子的直链或支链烷基，任选被羟基取代，并且它们的盐通过合适的未取代黄嘌呤与卤代甲基苯基乙酸的反应制备，随后羧酸酯或酸与苯基甘氨酚的反应来制备。 取代黄嘌呤在药物，特别是抗动脉粥样硬化药物中适合作为活性化合物。