Vla-4 antagonists

Details Vla-4 antagonists Vla-4 antagonists

C - Chemistry, Metallurgy

07

D

C07D 401/12 (2006.01)

Patent

CA 2603835

4-Thio, 4-sulfinyl and 4-sulfonyl proline 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.

Des dérivés de 4-thio, 4-sulfinyl et 4-sulfonyl proline selon la présente invention sont des antagonistes de l~intégrine du VLA-4 et sont utiles dans le traitement, la prévention et la suppression des maladies induites par la liaison du VLA-4 et l~adhésion et l~activation cellulaires. De plus, les composés de la présente invention démontrent une occupation significative du récepteur des cellules porteuses du VLA-4 après une administration orale et conviennent à des administrations orales une, deux ou trois fois par jour. Cette invention concerne également des compositions contenant de tels composés et des procédés de traitements les utilisant.

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