Substituted anilides

Details Substituted anilides Substituted anilides

C - Chemistry, Metallurgy

07

C

C07C 275/38 (2006.01) A61K 31/17 (2006.01) A61K 31/185 (2006.01) A61K 31/35 (2006.01) A61K 31/381 (2006.01) A61K 31/42 (2006.01) A61K 31/4406 (2006.01) A61K 31/50 (2006.01) A61P 11/06 (2006.01) C07D 213/82 (2006.01) C07D 237/24 (2006.01) C07D 261/18 (2006.01) C07D 309/06 (2006.01) C07D 333/38 (2006.01)

Patent

CA 2303848

The invention is directed to physiologically active compounds of formula (I) wherein: R1 is hydrogen, halogen, hydroxy, lower alkyl or lower alkoxy; X1, X2 and X6 independently represent N or CR10; and one of X3, X4 and X5 represents CR11 and the others independently represents N or CR10 (where R10 is hydrogen, amino, halogen, hydroxy, lower alkyl, lower alkoxy, lower alkylthio, lower alkylsulphinyl, lower alkylsulphonyl, nitro or trifluoromethyl; and R11 represents a group -L1- Ar1-L2-Y); and the corresponding N-oxides, and their prodrugs; and pharmaceutically acceptable salts and solvates of such compounds and their N-oxides and prodrugs. Such compounds have valuable pharmaceutical properties, in particular the ability to regulate the interaction of VCAM-1 and fibronectin with the integrin VLA-4 (.alpha.4.beta.1).

L'invention concerne des composés physiologiquement actifs de formule (I), dans laquelle R<1> est hydrogène, halogène, hydroxy, alkyle inférieur ou alcoxy inférieur; X<1>, X<2> et X<6> représentent indépendamment N ou CR<10>; et X<3>, X<4> ou X<5> représente CR<11>, les deux autres représentant indépendamment N ou CR<10> (où R<10> est hydrogène, amino, halogène, hydroxy, alkyle inférieur, alcoxy inférieur, alkylthio inférieur, alkylsulfinyle inférieur, alkylsulfonyle inférieur, nitro ou trifluorométhyle; et R<11> représente un groupe L<1>-Ar<1>-L<2>-Y); ainsi que les N-oxydes correspondants et leurs promédicaments; les sels et les solvates pharmaceutiquement acceptables desdits composés, leurs N-oxydes et leurs promédicaments. Ces composés ont des propriétés pharmaceutiques intéressantes, notamment la capacité de réguler l'interaction de VCAM-1 et de la fibronectine avec l'intégrine VLA-4 ( alpha 4 beta 1).

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