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    Spiroimidazolidine derivatives, their preparation, their use and pharmaceutical preparations formed therefrom
    1.
    发明授权
    Spiroimidazolidine derivatives, their preparation, their use and pharmaceutical preparations formed therefrom 有权
    螺咪唑烷衍生物，其制备方法，用途及由其形成的药物制剂

    公开(公告)号：US06399643B1

    公开(公告)日：2002-06-04

    申请号：US09572273

    申请日：2000-05-17

    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： A61K314184

    CPC分类号： C07D235/02

    摘要： The present invention relates to spiroimidazolidine derivatives of the formula I in which E, V, W, X, R1 and R2 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, such as, for example, rheumatoid arthritis, or allergic disorders. The compounds of the formula I are also 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 therapy and prophylaxis of illnesses 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 interactions of VLA-4 receptors with their ligands play a part. The invention also relates to processes for the preparation of the compounds of the formula I, pharmaceutical preparations which contain compounds of the formula I, and methods for treating these disorders.

    摘要翻译： 本发明涉及式Iin的螺咪唑烷衍生物，其中E，V，W，X，R 1和R 2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的化合物也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和预防由白细胞粘附和/或白细胞迁移的不期望程度或与其相关或与VLA-4的相互作用相关的细胞或细胞 - 基质相互作用引起的疾病 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，其含有式I化合物的药物制剂和治疗这些疾病的方法。

    Imidazolidine derivatives, their preparation, their use, and pharmaceutical preparations comprising them
    2.
    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
    3.
    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：US06331552B1

    公开(公告)日：2001-12-18

    申请号：US09516587

    申请日：2000-03-01

    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： A61K31415

    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 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。

    2,4-Substituted imidazolidine derivatives, their preparation, their use and pharmaceutical preparations comprising them
    4.
    发明授权
    2,4-Substituted imidazolidine derivatives, their preparation, their use and pharmaceutical preparations comprising them 有权
    2,4-取代的咪唑烷衍生物，其制备方法及其用途和包含它们的药物制剂

    公开(公告)号：US06423712B1

    公开(公告)日：2002-07-23

    申请号：US09157241

    申请日：1998-09-18

    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： C07D40912

    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 imidazolidine compounds of the formula I, 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的咪唑烷化合物。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引起的疾病，或其中以基于VLA的相互作用为基础的细胞 - 细胞或细胞 - 基质相互作用 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
    5.
    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。

    Hydantoin derivatives as inhibitors of leucocyte adhesion and as VLA-4 antagonists
    7.
    发明授权
    Hydantoin derivatives as inhibitors of leucocyte adhesion and as VLA-4 antagonists 失效
    乙内酰脲衍生物作为白细胞粘附的抑制剂和VLA-4拮抗剂

    公开(公告)号：US06514952B1

    公开(公告)日：2003-02-04

    申请号：US09405843

    申请日：1999-09-27

    申请人： Hans Ulrich Stilz ,  Volkmar Wehner ,  Christoph Huels ,  Dirk Seiffge

    发明人： Hans Ulrich Stilz ,  Volkmar Wehner ,  Christoph Huels ,  Dirk Seiffge

    IPC分类号： A61K31675

    CPC分类号： C07K5/1024 ,  C07K5/0202

    摘要： Compounds of the formula I in which B, D, E, R, W, Y, Z, b, c, d, e, f, g and have the meanings indicated in the claims, are inhibitors of the adhesion and migration of leucocytes and/or antagonists of the adhesion receptor VLA-4 which belongs to the group of integrins. The invention relates to the use of compounds of the formula I, and of pharmaceutical preparations which contain such compounds, for the treatment and prophylaxis of diseases which are caused by an undesired extent of leucocyte adhesion and/or leucocyte migration or which are associated therewith or in which cell—cell or cell-matrix interactions play a part which are based on interactions of VLA-4 receptors with their ligands, for example of inflammatory processes, rheumatoid arthritis or allergic disorders, and it also relates to the use of compounds of the formula I for the production of pharmaceuticals for use in such diseases. It further relates to novel compounds of the formula I.

    摘要翻译： B，D，E，R，W，Y，Z，b，c，d，e，f，g具有权利要求中所示含义的式Iin化合物是白细胞的粘附和迁移的抑制剂， /或属于整联蛋白组的粘附受体VLA-4的拮抗剂。 本发明涉及式I化合物和含有这些化合物的药物制剂的用途，用于治疗和预防由白细胞粘附和/或白细胞迁移的不期望程度或与之相关的或与其相关的疾病 其中细胞 - 细胞或细胞 - 基质相互作用发挥基于VLA-4受体与其配体（例如炎性过程，类风湿性关节炎或过敏性疾病）的相互作用的一部分，并且还涉及使用 用于生产用于此类疾病的药物的配方Ⅰ。 它还涉及式I的新化合物。