Hoechst Aktiengesellschaft

Aventis Pharma Deutschland, Gmbh

Christoph Huls

Dirk Seiffge

Gerhard Kretzschmar

Alexander Toepfer

Volkmar Wehner

Bernward Scholkens

Hans Ulrich Stilz

Eckart Bartnik

Peter Klemm

The present invention relates to compounds of the formula Iwhich 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.

Heterocytes as inhibitors of leucocyte adhesion and as VLA-4 antagonists

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.

Multiply fucosylated dicarboxylic acids possessing antiadhesive

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.

Antiadhesive piperidine-and pyrrolidinecarboxylic acids

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Wackernheim, Germany

Christoph Huls