Aza-bridged-bicyclic amino acid derivatives as .alpha.4...

C - Chemistry – Metallurgy – 07 – D

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C07D 221/22 (2006.01) A61K 31/439 (2006.01) A61P 29/00 (2006.01) A61P 35/00 (2006.01) A61P 37/02 (2006.01) C07D 209/52 (2006.01) C07D 401/12 (2006.01) C07D 453/06 (2006.01)

Patent

CA 2415088

The invention is directed to aza-bridged-bicyclic compounds having Formula (I): 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 concerne des composés bicycliques pontés aza représentés par la formule (I) : ainsi que leurs sels pharmaceutiquement acceptables. Lesdits composés sont des antagonistes du récepteur intégrine .alpha.4 utiles, en particulier, des antagonistes des récepteurs intégrine .alpha.4.beta.1 et .alpha.4.beta.7. L'invention concerne également des méthodes d'utilisation des composés selon l'invention pour le traitement des troubles induits par les intégrines, notamment mais pas exclusivement, les troubles inflammatoires, les troubles auto-immuns et les troubles liés à une prolifération cellulaire, ainsi que des procédés de préparation desdits composés et de leurs intermédiaires et dérivés, et de compositions pharmaceutiques les contenant.

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