Novel 5-membered ring heterocycles, their preparation, their...

Details Novel 5-membered ring heterocycles, their preparation, their... Novel 5-membered ring heterocycles, their preparation, their...

C - Chemistry, Metallurgy

07

K

C07K 5/072 (2006.01) A61K 31/415 (2006.01) A61K 31/675 (2006.01) A61K 38/05 (2006.01) C07D 233/74 (2006.01) C07D 233/86 (2006.01) C07F 9/6506 (2006.01) C07K 5/02 (2006.01) C07K 5/117 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2247735

The present invention relates to compounds of the formula I, Image in which B, E, W, Y, Z, R, R2, R2a, R2b, R3, g 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 the therapy and prophylaxis of the disease states mentioned and pharmaceutical preparations which contain the compounds of the formula I.

L'invention concerne des composés de la formule I, Image , dans laquelle B, E, W, Y, Z, R, R2, R2a, R2b, R3, g et h ont les significations indiquées dans les revendications. Les composés de la formule I sont des composés actifs pharmaceutiques précieux qui conviennent, par exemple, pour traiter et prévenir les troubles inflammatoires, par exemple, la polyarthrite rhumatoïde, ou les troubles allergiques. Ils sont des inhibiteurs de l'adhésion et de la migration des leucocytes et/ou des antagonistes des récepteurs de l'adhésion VLA-4 appartenant au groupe des intégrines. Ils conviennent généralement pour le traitement curatif ou prophylactique des maladies causées par une adhésion et/ou une migration des leucocytes plus importantes qu'il n'est souhaitable ou associées à ces deux phénomènes, ou dans lesquelles les interactions entre cellules ou entre cellules et matrice qui sont basées sur les interactions des récepteurs VLA-4 avec leurs ligands jouent un rôle. L'invention a aussi trait à des processus pour préparer des composés de la formule I, à leur utilisation pour traiter ou prévenir des types de maladie mentionnés et à des préparations pharmaceutiques qui contiennent les composés de la formule I.

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