公开(公告)号：US06838439B2

公开(公告)日：2005-01-04

申请号：US09995631

申请日：2001-11-29

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

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

IPC分类号： C07D277/20 ,  A61K38/00 ,  A61K38/05 ,  A61K38/06 ,  A61K38/07 ,  A61P3/08 ,  A61P9/00 ,  A61P9/10 ,  A61P11/00 ,  A61P11/06 ,  A61P19/02 ,  A61P29/00 ,  A61P33/02 ,  A61P35/00 ,  A61P37/00 ,  A61P37/08 ,  A61P43/00 ,  C07D233/54 ,  C07D233/72 ,  C07D277/34 ,  C07K5/06 ,  C07K5/078 ,  C07K5/097 ,  C07K5/107 ,  C07K5/11 ,  C07K5/117

CPC分类号： C07K5/1016 ,  A61K38/00 ,  C07K5/1019 ,  Y02A50/411

摘要： The present invention relates to compounds of the formula I which 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 also relates to processes for the preparation of formula I, pharmaceutical compositions containing compounds of formula I, and the treatment or prophylaxis of various diseases caused by or are associated with excess leucocyte adhesion and/or leucocyte migration, as well as diseases associated with cell-cell or cell-matrix interactions, which on interactions of VLA-4 receptors with their ligands play a part of, for example, inflammatory processes, rheumatoid arthritis or allergic disorders.

公开(公告)号：US5811405A

公开(公告)日：1998-09-22

申请号：US788269

申请日：1997-01-24

申请人： Alexander Toepfer ,  Gerhard Kretzschmar ,  Eckart Bartnik ,  Christoph Huls ,  Dirk Seiffge

发明人： Alexander Toepfer ,  Gerhard Kretzschmar ,  Eckart Bartnik ,  Christoph Huls ,  Dirk Seiffge

IPC分类号： C07H15/04 ,  A61K31/70 ,  A61K31/7028 ,  A61K31/715 ,  A61K49/00 ,  A61P9/00 ,  A61P9/08 ,  A61P11/00 ,  A61P17/00 ,  A61P29/00 ,  A61P37/06 ,  A61P43/00 ,  C07C55/02 ,  C07C55/22 ,  C07C55/24 ,  C07C55/26 ,  C07C59/235 ,  C07C217/08 ,  C07C219/06 ,  C07C229/24 ,  C07H3/04 ,  C07H3/06 ,  C08B37/00 ,  C07H1/00

CPC分类号： C07H3/06 ,  C07H3/04

摘要： The invention relates to multiply fucosylated dicarboxylic acid derivatives possessing antiadhesive properties, to a process for preparing them, to their use, and to pharmaceuticals and diagnostic agents which are prepared from these derivatives. These multiply fucosylated dicarboxylic acid derivatives are suitable for preparing pharmaceuticals or diagnostic agents for diseases which are associated with an excessive, selectin receptor-mediated cell adhesion in the tissue which is affected by the disease.

摘要翻译： 本发明涉及具有抗粘附性的多重岩藻糖基化二羧酸衍生物，其制备方法及其应用，以及由这些衍生物制备的药物和诊断剂。 这些多重岩藻糖基化二羧酸衍生物适用于制备与受该疾病影响的组织中过度选择素受体介导的细胞粘附相关的疾病的药物或诊断剂。

公开(公告)号：US5739300A

公开(公告)日：1998-04-14

申请号：US726142

申请日：1996-10-04

申请人： Alexander Toepfer ,  Gerhard Kretzschmar ,  Bernward Scholkens ,  Peter Klemm ,  Christoph Huls ,  Dirk Seiffge

发明人： Alexander Toepfer ,  Gerhard Kretzschmar ,  Bernward Scholkens ,  Peter Klemm ,  Christoph Huls ,  Dirk Seiffge

IPC分类号： C07D295/20 ,  A61K31/215 ,  A61K31/33 ,  A61K31/40 ,  A61K31/435 ,  A61K31/445 ,  A61K31/495 ,  A61K31/70 ,  A61K31/7028 ,  A61K31/7034 ,  A61P3/08 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P11/00 ,  A61P17/00 ,  A61P29/00 ,  A61P35/00 ,  A61P37/06 ,  A61P37/08 ,  A61P43/00 ,  C07D207/08 ,  C07D207/16 ,  C07D211/34 ,  C07D211/62 ,  C07D405/00 ,  C07H15/203 ,  C07H15/207 ,  C07H17/00 ,  C07H19/04 ,  C07H3/02 ,  C07H3/06 ,  C07H15/04

CPC分类号： C07H15/207

摘要： The invention relates to conjugates which consist of mono- or polycarboxylated piperidine or pyrrolidine derivatives and pyranoses, furanoses or polyalcohols linked via a chain or a cyclic system. The carboxyl groups of the piperidine derivatives can either be located directly on the ring or linked to the ring via a short chain. The invention additionally relates to the preparation of these compounds and to their use for the production of pharmaceuticals and diagnostics.

摘要翻译： 本发明涉及由单羧酸化或多羧基哌啶或吡咯烷衍生物和吡喃糖，呋喃糖或通过链或环状体系连接的多元醇组成的缀合物。 哌啶衍生物的羧基可以直接位于环上或通过短链连接到环上。 本发明还涉及这些化合物的制备及其用于生产药物和诊断的用途。