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    • 20. 发明申请
    • DISALICYLATE ANALOG BASED SIALYL LEWIS<x> MIMETICS
    • 低聚糖唾液酸基路易斯效法类似的基于双水杨酸
    • WO99029706A2
    • 1999-06-17
    • PCT/US1998/025788
    • 1998-12-04
    • C07C65/105C07C65/40C07C66/02C07C69/94C07H15/18C07H15/00
    • C07H15/18C07C65/105C07C65/40C07C66/02C07C69/94
    • The present invention discloses medicaments that are selectin-ligand structural mimetics that bind to certain selectins wherein the mimetics may lack the sialic acid and/or fucose of the natural selecting ligand, sialyl Lewis (sLe ), but have a structure capable of mimicking the structural features necessary for selectin recognition. In particular, the invention compounds mimic the key structural features of the oligosaccharides responsible for selectin-mediated cell adhesion. These features consist of the charge-distance-coordination relationship between the carboxylic acid functionality of sialic acid at a distance of 8-12 angstroms of the L-fucose moiety. The invention compounds are disalicylate, its analogs, and disalicylate-based C-glycoside compounds. The present invention also discloses methods of treating selectin-mediated disorders comprising administering the compounds disclosed.
    • 本发明涉及由结构模仿选择素配体,其结合到某些选择素和那些不含唾液酸和/或岩藻糖的天然选择蛋白的配体中,该低聚糖的唾液酸组成的药物 -Lewis x(sLe x),但其具有能够模仿识别选择素所必需的结构特征的结构。 特别地,本发明的化合物具有模拟负责选择素诱导的细胞粘附的寡糖的关键结构特征的性质。 这些特征包括关系唾液酸的羧酸官能团之间的部分L-岩藻糖的8至12埃的距离负载距离协调。 本发明的化合物是二水杨酸酯,其类似物和基于二水杨酸酯的C-糖苷化合物。 本发明还提供了通过施用所呈现的化合物来治疗选择素介导的疾病的方法。