Vla-4 antagonists

Details Vla-4 antagonists Vla-4 antagonists

C - Chemistry, Metallurgy

07

K

C07K 5/078 (2006.01) A61K 38/05 (2006.01) C07K 5/00 (2006.01) C07K 14/705 (2006.01)

Patent

CA 2604531

Substituted N-[N-(sulphonylphenyl)sulfonyl-prolyl]-phenylalanine derivatives of the present invention are antagonists of the VLA-4 integrin and are useful in the treatment, prevention and suppression of diseases mediated by VLA-4- binding and cell adhesion and activation. Moreover, the compounds of the present invention demonstrate significant receptor occupancy of VLA-4 bearing cells after oral administration and are suitable for once-, twice-, or thrice- a-day oral administration. This invention also relates to compositions containing such compounds and methods of treatment using such compounds.

L'invention concerne des dérivés de N-[N-(sulphonylphényl)sulfonyl-prolyl]-phénylalanine substitués qui sont des antagonistes de l'intégrine VLA-4 et qui sont utilisés pour traiter, prévenir et inhiber des maladies médiées par la liaison à VLA-4 et par l'adhésion et l'activation cellulaire. En outre, les composés de l'invention présentent un taux significatif d'occupation des récepteurs des cellules porteuses de VLA-4 après l'administration orale et conviennent à une administration orale quotidienne, bi- ou triquotidienne. L'invention porte également sur des compositions contenant lesdits composés et sur des procédés de traitement faisant appel auxdits composés.

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