Phenylalanine derivatives as alpha 4 integrin inhibitors

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 401/12 (2006.01) A61K 31/44 (2006.01) A61K 31/4409 (2006.01) A61K 31/4436 (2006.01) A61K 31/444 (2006.01) A61K 31/4709 (2006.01) A61K 31/497 (2006.01) A61K 31/498 (2006.01) A61K 31/501 (2006.01) A61K 31/506 (2006.01) A61K 31/53 (2006.01) A61K 31/5377 (2006.01) A61P 1/00 (2006.01) A61P 3/10 (2006.01) A61P 11/06 (2006.01) A61P 17/00 (2006.01) A61P 17/06 (2006.01) A61P 19/02 (2006.01) A61P 25/00 (2006.01) A61P 29/00 (2006.01) A61P 37/02 (2006.01) A61P 43/00 (2006.01) C07D 213/02 (2006.01) C07D 213/81 (200

Patent

CA 2338442

Phenylalanine derivatives of formula (1) are described in which: Ar1 is an aromatic or heteroaromatic group; L1 is a linker atom or group; R is a carboxylic acid or a derivative thereof; Ar2 is an optionally substituted aromatic or heteroaromatic group; and the salts, solvates, hydrates and N- oxides thereof. The compounds are able to inhibit the binding of .alpha.4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.

La présente invention concerne des dérivés de phénylalanine de formule (1) dans lesquels Ar?1¿ est un groupe aromatique ou hétéroaromatique, L?1¿ est un atome ou un groupe de liaison, R est un acide carboxylique ou un dérivé de cet acide, Ar?2¿ est un groupe aromatique ou hétéroaromatique éventuellement substitué. L'invention concerne aussi les sels, les solvatés, les hydrates et les N-oxydes de ces dérivés. Les composés peuvent inhiber la liaison d'.alpha.4 intégrines à leurs ligands, et sont utiles en prophylaxie et dans le traitement de troubles d'ordres immun ou inflammatoire.

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