5-membered ring heterocycles as inhibitors of leucocyte...

Details 5-membered ring heterocycles as inhibitors of leucocyte... 5-membered ring heterocycles as inhibitors of leucocyte...

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) A61K 38/06 (2006.01) C07D 233/76 (2006.01) C07D 405/12 (2006.01) C07F 9/6506 (2006.01) C07K 5/02 (2006.01) C07K 5/093 (2006.01) C07K 5/097 (2006.01) C07K 5/117 (2006.01) C07K 7/06 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2220784

5-Membered ring heterocycles as inhibitors of leucocyte adhesion and as VLA-4 antagonists Compound of the formula I (see fig. I) in which B, D, E, R, W, Y, Z, b, c, d, e, f, g and h 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 pharmaceuticalpreparations 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 which are based on interactions of VLA-4 receptors with their ligands play a part, for example of inflammatory processes, of rheumatoid arthritis or of allergic disorders, and it also relates to the use of compounds of the formula I for the production of pharmaceuticals for use in such disease. It further relates tonovel compounds of the formula I.

Hétérocycles avec noyau de 5 chaînons, inhibiteurs de l'adhérence des leucocytes et antagonistes des récepteurs VLA-4. Composé de formule I (voir fig. I), dans laquelle B, D, E, R, W, Y, Z, b, c, d, e, f, g et h ont la signification donnée dans les revendications, inhibiteur de l'adhérence et de la migration des leucocytes et (ou) antagoniste des récepteurs VLA-4 d'adhérence, appartenant au groupe des intégrines. L'invention porte sur l'emploi de composés de formule I et de préparations pharmaceutiques à base de ces composés, pour le traitement et la prévention de maladies causées par un degré indésirable d'adhérence et (ou) de migration des leucocytes, ou encore associées à ces processus ou dans lesquelles les interactions cellules-cellules ou cellules-substrat basées sur des interactions des récepteurs VLA-4 avec leurs ligands jouent un certain rôle, notamment dans les affections inflammatoires, la polyarthrite rhumatoïde et les troubles allergiques; le brevet porte également sur l'emploi des composés de formule I pour la fabrication de produits pharmaceutiques, destinés à ces maladies. Enfin il porte sur de nouveaux composés de formule I.

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