Phenylalanine enamide derivatives

Details Phenylalanine enamide derivatives Phenylalanine enamide derivatives

C - Chemistry, Metallurgy

07

D

C07D 471/04 (2006.01) C07D 221/00 (2006.01)

Patent

CA 2492430

Phenylalanine enamide derivatives of formula (1) are described, wherein R1is a -CH(CH3)2, -(CH2)2CH3; -CH2C(CH3)3, -CH2CH2OH, -CH2CH2OCH3, -CH2CH2OCH2CH2OH, - CH2CH2OCH2CH2OCH3, formula (A) group; and the salts, solvates and N-oxides thereof. Compounds according to the invention are potent and selective inhibitors of .alpha.4 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 concerne des dérivés phénylalanine énamide de formule (1) dans laquelle R?1¿ représente un groupe -CH(CH¿3?)¿2?, -(CH¿2?)¿2?CH¿3,? -CH¿2?C(CH¿3?)¿3?, -CH¿2?CH¿2?OH, -CH¿2?CH¿2?OCH¿3?, -CH¿2?CH¿2?OCH¿2?CH¿2?OH, -CH¿2?CH¿2?OCH¿2?CH¿2?OCH¿3?, ou un groupe (A), ainsi que des sels, des solvates et des N-oxydes de ces dérivés. Les composés de cette invention sont des inhibiteurs sélectifs et puissants des intégrines ?4. Ces composés peuvent être utilisés afin de moduler l'adhérence cellulaire et, en particulier, en prophylaxie et dans le traitement de maladies ou de troubles y compris dans ceux de l'inflammation dans lesquels l'extravasation de leucocytes joue un rôle, l'invention concernant aussi une telle utilisation ainsi que l'utilisation de ces composés pour la fabrication d'un médicament permettant de traiter de ces maladies ou troubles.

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