Aminobenzophenones as inhibitors of il-1.beta. and tnf-.alpha.

C - Chemistry – Metallurgy – 07 – C

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C07C 225/22 (2006.01) A61K 31/095 (2006.01) A61K 31/135 (2006.01) A61K 31/136 (2006.01) A61K 31/15 (2006.01) A61K 45/06 (2006.01) A61P 17/00 (2006.01) A61P 29/00 (2006.01) C07C 251/48 (2006.01) C07C 325/02 (2006.01)

Patent

CA 2393312

A compound of general formula (I), wherein R1 represents a substituent selected from the group consisting of halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, cyano, -CONH2, phenyl, and nitro; R2 represents one or more, same or different substituents selected from the group consisting of hydrogen, halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, cyano, -CONH2, phenyl, and nitro; R3 represents one or more, same or different substituents selected from the group consisting of hydrogen, halogen, hydroxy, mercapto, trifluoromethyl, cyano, carboxy, carbamoyl, (C1-C10)alkyl, (C2-C10)olefinic group, (C3-C8)monocyclic hydrocarbon group, (C1-C10)alkoxy, (C1-C10) alkylthio, (C1-C10)alkoxycarbonyl, and phenyl; R4 represents hydrogen, (C1- C6)alkyl, (C2-C6)olefinic group, or (C3-C6)monocyclic hydrocarbon group; R5 represents one or more, same or different substituents selected from the group consisting of hydrogen and R1; X represents oxygen, sulphur, or N-OH; and salts thereof with pharmaceutically acceptable acids, hydrates and solvates, may be used in the prophylaxis or treatment of inflammatory diseases.

La présente invention concerne un composé représenté par la formule générale (I). Dans cette formule, R¿1? est un substituant du groupe des halogène, hydroxy, mercapto, trifluorométhyle, amino, C¿1?-C¿3? alkyl, groupe oléfinique en C¿2?-C¿3?, C¿1?-C¿3? alcoxy, C¿1?-C¿3? alkylthio, C¿1?-C¿6? alkylamino, C¿1?-C¿3? alkoxycarbonyl, cyano, -CONH¿2?, phényle, et nitro. R¿2? est un ou plusieurs substituants identiques ou différents du groupe des hydrogène, halogène, hydroxy, mercapto, trifluorométhyle, amino, C¿1?-C¿3? alkyle, groupe oléfinique en C¿2?-C¿3?, C¿1?-C¿3? acloxy, C¿1?-C¿3? alkylthio, C¿1?-C¿6? alkylamino, C¿1?-C¿3? alcoxycarbonyle, cyano, -CONH¿2?, phényle, et nitro. R¿3? est un ou plusieurs substituants identiques ou différents du groupe des hydrogène, halogène, hydroxy, mercapto, trifluorométhyle, cyano, carboxy, carbamoyl, C¿1?-C¿10? alkyle, groupe oléfinique en C¿2?-C¿10?, groupe hydrocarbure monocyclique en C¿3?-C¿8?, C¿1?-C¿10? alcoxy, (C¿1?-C¿10?) alkylthio, (C¿1?-C¿10?)alcoxycarbonyle, et phényle. R¿4? est hydrogène, (C¿1?-C¿6?) alkyle, (C¿2?-C¿6?) groupe oléfinique, ou groupe hydrocarbure monocyclique en (C¿3?-C¿6?). R¿5? est un ou plusieurs substituants identiques ou différents du groupe des hydrogène et R¿1?. X est oxygène, soufre, ou N-OH. L'invention concerne également certains sels pharmaceutiquement admis, certains de leurs hydrates et spmvats. Ils conviennent particulièrement pour la prophylaxie ou le traitement d'affections inflammatoires.

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