Phenylalanine enamide derivatives containing a...

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 413/12 (2006.01) A61K 31/44 (2006.01) A61K 31/4433 (2006.01) A61K 31/444 (2006.01) A61P 29/00 (2006.01) C07D 213/81 (2006.01) C07D 401/12 (2006.01)

Patent

CA 2492381

Phenylalanine enamide derivatives of formula (1) are described: wherein R1 is a -CH3, -(CH2)3CH3, -CH2CH20H, -CH2CH20CH3, -CH2CH20CH2CH20H, - CH2CH20CH2CH20CH3, Formula (II) group; and the salts, solvates and N-oxides thereof. Compounds according to the invention are potent and selective inhibitors of oA integrins. The compounds are of use in modulating cell adhesion and in particular are of use in the prophylaxis and treatment of diseases or disorders including inflammation in which the extravasation of leukocytes plays a role and the invention extends to such a use and to the use of the compounds for the manufacture of a medicament for treating such diseases or disorders.

L'invention porte sur des dérivés de phénylalanine énamide de formule (I) dans laquelle R?1¿ représente un groupe -CH¿3?, -(CH¿2?)¿3?CH¿3?, -CH¿2?CH¿2?0H, -CH¿2?CH¿2?0CH¿3?, -CH¿2?CH¿2?0CH¿2?CH¿2?0H, -CH¿2?CH¿2?0CH¿2?CH¿2?0CH¿3? ou un groupe de formule (II); ainsi que sur des sels, des solvates et des N-oxydes de ces dérivés. Les composés de cette invention sont de puissants inhibiteurs sélectifs des intégrines .alpha.A. Ces composés sont utiles dans la modulation de l'adhésion cellulaire et notamment dans la prophylaxie et le traitement de maladies ou troubles tels que l'inflammation dans lesquels l'extravasation des leucocytes joue un rôle. L'invention porte également sur cette utilisation et sur l'utilisation des composés dans la fabrication d'un médicament destiné à traiter ces maladies ou troubles.

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