.beta.-alanine derivatives as .alpha.4 integrin inhibitors

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 213/79 (2006.01) A61K 31/435 (2006.01) A61P 29/00 (2006.01) A61P 37/00 (2006.01) C07C 233/80 (2006.01) C07D 207/16 (2006.01) C07D 213/56 (2006.01) C07D 213/81 (2006.01) C07D 213/82 (2006.01) C07D 401/12 (2006.01) C07D 403/12 (2006.01) C07D 405/12 (2006.01) C07D 413/12 (2006.01) C07D 417/12 (2006.01) C07D 417/14 (2006.01)

Patent

CA 2347701

Alkanoic acid derivatives of formula (1) are described: Ar1(Alka)rL1Ar2CH(R1)C(Ra)(Ra')R wherein Ar1 is an optionally substituted aromatic or heteroaromatic group; L1 is a covalent bond or a linker atom or group; Ar2 is an optionally substituted phenylene or nitrogen-containing six- membered heteroarylene group; R is a carboxylic acid (-CO2H) or a derivative thereof; 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 d'acides alcanoïques représentés par la formule (1) telle que Ar?1¿(Alk?a¿)¿r?L?1¿Ar?2¿CH(R?1¿)C(R?a¿)(R?a'¿)R, ou l'un des sels, solvates, hydrates et N-oxydes de ces dérivés. Ar?1¿ est un groupe aromatique hétéroaromatique éventuellement substitué. L?1¿ est une liaison par covalence ou un groupe ou atome de liaison. Ar?2¿ est un groupe phénylène éventuellement substitué ou un groupe hétéroarylène azoté à six chaînons. R est acide carboxylique (-CO¿2?H) ou l'un de ses dérivés. Ces composés, qui permettent de bloquer la liaison des .alpha.4 intégrines à leurs ligands, conviennent pour la prophylaxie et le traitement des troubles d'origine immunitaire ou inflammatoire.

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