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    Glycomimetics as selectin antagonists and pharmaceuticals having antiinflammatory activity prepared therefrom
    3.
    发明授权
    Glycomimetics as selectin antagonists and pharmaceuticals having antiinflammatory activity prepared therefrom 失效
    作为选择素拮抗剂的甘油模拟物和由其制备的具有抗炎活性的药物

    公开(公告)号：US06197752B1

    公开(公告)日：2001-03-06

    申请号：US08708475

    申请日：1996-09-05

    申请人： Wolfgang Schmidt ,  Ulrich Sprengard ,  Gerhard Kretzschmar ,  Horst Kunz

    发明人： Wolfgang Schmidt ,  Ulrich Sprengard ,  Gerhard Kretzschmar ,  Horst Kunz

    IPC分类号： A61K3170

    CPC分类号： C07D309/10 ,  C07D307/20

    摘要： The invention relates to novel mimetics of the tetrasaccharides sialyl- Lewis-X (SLeX) and sialyl- Lewis-A (SLeA) having an improved action as inhibitors of cell adhesion, specifically a compound of the formula I in which R1 is —H, —CH3 or —CH2OH, R2 is —H or —OH, R3, R4 and R5 independently of one another are —H, C1-C4-alkyl or —OH, R6, R7, R8, R9 and R10 independently of one another are —H or C1-C4-alkyl D is —O—C(O)—, —C(O)—or —NR6—C(O)—, E is —CR7R8—, —NR7—, or a nitrogen heterocycle of the formula n is 1 or 2, m is 0 or 1, p is an integer from 0 to 10, q is 1 or 2 and X1 and X2 independently of one another are —H, —COOR9, —NR9R10, —OH, —OSO3H, —CH2COOR9 or —CH2OSO3H or together are ═O, to a process for preparing these compounds and to their use as pharmacological active compounds and diagnostic agents.

    摘要翻译： 本发明涉及具有作为细胞粘附抑制剂的改善作用的四糖唾液酸基-LX-X（SLeX）和唾液酸 - 路易斯-A（SLeA）的新型模拟物，特别是式Iin化合物，其中R 1为-H，-CH 3 或-CH 2 OH，R 2是-H或-OH，R 3，R 4和R 5彼此独立地是-H，C 1 -C 4 - 烷基或-OH，R 6，R 7，R 8，R 9和R 10彼此独立地是-H 或C 1 -C 4 - 烷基D为-OC（O） - ， - C（O） - 或-NR 6 -C（O） - ，E为-CR 7 R 8 - ， - NR 7 - 或式 2，m为0或1，p为0至10的整数，q为1或2，X 1和X 2彼此独立地为-H，-COOR 9，-NR 9 R 10，-OH，-OSO 3 H，-CH 2 COOR 9或-CH 2 OSO 3 H 或一起是= O，涉及制备这些化合物的方法及其作为药理活性化合物和诊断剂的用途。