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    • 3. 发明授权
    • Imidazolidine derivatives, their preparation, their use and pharmaceutical preparations comprising them
    • 咪唑烷衍生物,其制备方法,用途及药物制剂
    • US06680333B2
    • 2004-01-20
    • US10092901
    • 2002-03-08
    • Volkmar WehnerHorst BlumHartmut RüttenHans Ulrich Stilz
    • Volkmar WehnerHorst BlumHartmut RüttenHans Ulrich Stilz
    • A61K3144
    • C07D401/12C07D233/76C07D233/78
    • The present invention relates to novel imidazolidine derivatives of formula I, wherein A, E, Z, R1, R2, R3, R4 and R5 have the meanings indicated in the claims. The compounds of formula I are valuable pharmaceutical active compounds which are suitable, for example, for the treatment of inflammatory diseases, including rheumatoid arthritis, or allergic diseases. The compounds of formula I are inhibitors of the adhesion and migration of leukocytes and/or antagonists of the adhesion receptor VLA-4 belonging to the integrins group. They are generally suitable for the treatment of diseases which are caused by an undesired extent of leukocyte adhesion and/or leukocyte migration or are associated therewith or in which cell-cell or cell-matrix interactions which are based on the interactions of VLA-4 receptors with their ligands play a role. The invention furthermore relates to processes for the preparation of the compounds of formula I, their use and pharmaceutical preparations which contain compounds of formula I.
    • 本发明涉及式I的新型咪唑烷衍生物,其中A,E,Z,R 1,R 2,R 3,R 4和R 5具有权利要求书中所示的含义 。 式I化合物是有价值的药物活性化合物,其适用于例如用于治疗炎性疾病,包括类风湿性关节炎或过敏性疾病。 式I化合物是属于整联蛋白组的粘附受体VLA-4的白细胞和/或拮抗剂的粘附和迁移的抑制剂。 它们通常适用于治疗由白细胞粘附和/或白细胞迁移的不期望程度或与之相关的疾病或其中基于VLA-4受体的相互作用的细胞 - 细胞或细胞 - 基质相互作用引起的疾病 其配体发挥作用。 本发明还涉及制备式I化合物的方法,其用途和含有式I化合物的药物制剂。