Novel heterocycles as inhibitors of leucocyte adhesion and...

C - Chemistry – Metallurgy – 07 – K

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C07K 5/072 (2006.01) A61K 31/415 (2006.01) A61K 38/05 (2006.01) C07D 233/76 (2006.01) C07K 5/107 (2006.01) C07K 5/11 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2220777

Novel heterocycles as inhibitors of leucocyte adhesion and as VLA-4 antagonists The present invention relates to compounds of the formula I (see fig. 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 related to processes for their preparation, to the use of compounds of the formula I for the treatment or prophylaxis of diseased 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 which are based on interactions of VLA-4 receptors with their ligands play a part, for example of inflammatory processes, of rheumatoid arthritic or of allergic disorder, and also to the use of compounds of the formula I for the production of pharmaceuticals for use in such diseases, and to pharmaceutical preparations which contain the compoundsof the formula I.

Nouveaux hétérocycles, inhibiteurs de l'adhérence des leucocytes et antagonistes de VLA-4. L'invention porte sur des composés de formule I (voir fig. I), inhibiteurs de l'adhérence et de la migration des leucocytes et (ou) antagonistes des récepteurs d'adhérence VLA-4, appartenant au groupe des intégrines. L'invention porte également sur des méthodes pour les préparer, sur l'utilisation des composés de formule I pour le traitement ou la prévention de maladies causées par un excès d'adhérence et (ou) de migration leucocytaire(s), ou qui y sont associées, ou encore dans lesquelles les interactions cellules-cellules ou cellules-matrice, basées sur les interactions des récepteurs VLA-4 avec leurs ligands, jouent un rôle, comme par exemple dans les processus inflammatoires, la polyarthrite rhumatoïde ou certaines allergies; enfin, l'invention porte sur l'emploi des composés de formule I pour la production de produits pharmaceutiques destinés à traiter ces affections, et sur des préparations pharmaceutiques à base de composés de formule I.

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