Improved aza-bridged-bicyclic amino acid derivatives as a4...

C - Chemistry – Metallurgy – 07 – D

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C07D 451/14 (2006.01) A61K 31/439 (2006.01) A61P 29/00 (2006.01)

Patent

CA 2543438

The invention is directed to aza-bridged-bicyclic compounds having Formula (I): and pharmaceutically acceptable salts thereof. The compounds are useful .alpha.4 integrin receptor antagonists and, in particular, .alpha.4.beta.1 and .alpha.4.beta.7 integrin receptor antagonists. The invention is further directed to methods for use of the instant compounds for treating integrin mediated disorders including, but not limited to, inflammatory disorders, autoimmune disorders and cell-proliferative disorders, methods for preparing the compounds and methods for preparing the intermediates, derivatives and pharmaceutical compositions thereof.

L'invention porte sur des composés aza-bicyliques à pontage ayant une formule (I) et sur leurs sels pharmaceutiquement acceptables. Les composés sont utilisés comme antagonistes du récepteur de l'intégrine .alpha.4 et, plus particulièrement, comme antagonistes du récepteur de l'intégrine .alpha.4.beta.1 et .alpha.4.beta.7. L'invention porte également sur des procédés d'utilisation des composés en cours en vue du traitement des troubles induits par l'intégrine, entre autres, les troubles inflammatoires, les maladies auto-immunes et les troubles à prolifération cellulaire, sur des procédés des préparations desdits composés et des procédés de préparation des intermédiaires, des dérivés et des compositions pharmaceutiques de ceux-ci.

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