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    Imidazolidine derivatives, their preparation, their use, and pharmaceutical preparations comprising them
    1.
    发明授权
    Imidazolidine derivatives, their preparation, their use, and pharmaceutical preparations comprising them 有权
    咪唑烷衍生物，其制备方法，用途及包含它们的药物制剂

    公开(公告)号：US06759424B2

    公开(公告)日：2004-07-06

    申请号：US10147921

    申请日：2002-05-20

    申请人： Volkmar Wehner ,  Hans Ulrich Stilz ,  Wolfgang Schmidt ,  Dirk Seiffge

    发明人： Volkmar Wehner ,  Hans Ulrich Stilz ,  Wolfgang Schmidt ,  Dirk Seiffge

    IPC分类号： C07D23302

    CPC分类号： C07K5/1024 ,  A61K38/00 ,  C07K5/0202 ,  C07K5/0812 ,  C07K5/0821 ,  C07K5/1016 ,  C07K5/1027 ,  Y02A50/411

    摘要： The present invention relates to novel imidazolidine derivatives of the formula I, in which B, E, W, Z, R, R0, R2, R3, e and h have the meanings indicated in the application. The compounds of the formula I are valuable pharmaceutical active compounds, which are suitable, for example, for the therapy and prophylaxis of inflammatory disorders, for example of rheumatoid arthritis, or of allergic disorders. The compounds of the formula I are inhibitors of the adhesion and migration of leucocytes and/or antagonists of the adhesion receptor VLA-4 belonging to the integrins group. They are generally suitable for the therapy or prophylaxis of illnesses which are caused by an undesired extent of leucocyte adhesion and/or leucocyte migration or are associated therewith, or in which cell-cell or cell-matrix interactions which are based on interactions of VLA-4 receptors with their ligands play a part. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use in the therapy and prophylaxis of the disease states mentioned and pharmaceutical preparations which contain compounds of the formula I.

    摘要翻译： 本发明涉及式I的新型咪唑烷衍生物，其中B，E，W，Z，R，R 0，R 2，R 3，e和h具有本申请中指出的含义 。 式I的化合物是有价值的药物活性化合物，其适用于例如治疗和预防炎症性疾病，例如类风湿性关节炎或过敏性疾病。 式I的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或预防由不良程度的白细胞粘附和/或白细胞迁移或与之相关的疾病或其中基于VLA- 4受体与其配体发挥作用。 本发明还涉及制备式I化合物的方法，它们在治疗和预防所述疾病状态中的用途以及含有式I化合物的药物制剂。

    Substituted imidazolidine derivatives, their preparation, their use and pharmaceutical preparations including them
    9.
    发明授权
    Substituted imidazolidine derivatives, their preparation, their use and pharmaceutical preparations including them 有权
    取代的咪唑烷衍生物，其制备方法，用途及包括它们在内的药物制剂

    公开(公告)号：US06521654B2

    公开(公告)日：2003-02-18

    申请号：US09952028

    申请日：2001-09-14

    申请人： Volkmar Wehner ,  Hans Ulrich Stilz ,  Wolfgang Schmidt ,  Dirk Seiffge

    发明人： Volkmar Wehner ,  Hans Ulrich Stilz ,  Wolfgang Schmidt ,  Dirk Seiffge

    IPC分类号： A61K314166

    CPC分类号： C07K5/0202 ,  C07K5/1016

    摘要： Substituted imidazolidine derivatives of the formula I, in which B, E, W, Y, R, R2, R3, R30, e and h have the meanings indicated in the claims. The compounds of the formula I are valuable pharmaceutical active compounds, which are suitable, for example, for the therapy and prophylaxis of inflammatory disorders, for example of rheumatoid arthritis, or of allergic disorders. The compounds of the formula I are inhibitors of the adhesion and migration of leucocytes and/or antagonists of the adhesion receptor VLA-4 belonging to the integrins group. They are generally suitable for the therapy or prophylaxis of illnesses which are caused by an undesired extent of leucocyte adhesion and/or leucocyte migration or are associated therewith, or in which cell-cell or cell-matrix interactions which are based on interactions of VLA-4 receptors with their ligands play a part. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use, in particular as pharmaceutical active compounds, and pharmaceutical preparations which contain compounds of the formula I.

    摘要翻译： 取代的式I的咪唑烷衍生物，其中B，E，W，Y，R，R 2，R 3，R 30，e和h具有权利要求中所示的含义。 式I的化合物是有价值的药物活性化合物，其适用于例如治疗和预防炎症性疾病，例如类风湿性关节炎或过敏性疾病。 式I的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或预防由不良程度的白细胞粘附和/或白细胞迁移或与之相关的疾病或其中基于VLA- 4受体与其配体发挥作用。 本发明还涉及制备式I化合物，其用途，特别是作为药物活性化合物的方法和含有式I化合物的药物制剂。