Aminobenzophenones as inhibitors of interleukin and tnf

C - Chemistry – Metallurgy – 07 – C

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C07C 225/22 (2006.01) A61K 31/135 (2006.01)

Patent

CA 2278798

The compounds of the present invention are represented by general formula (I) in which formula R1 and R2 stand independently for one or more, similar or different substituents selected from the group consisting of hydrogen, halogen, hydroxy, mercapto, trifluoromethyl, amino, alkyl, alkoxy, alkylthio, alkylamino, or alkoxycarbonyl, the C-content of which can be from 1 to 5, cyano, carboxy, carbamoyl, phenyl, or nitro; R3 stands for hydrogen, halogen, hydroxy, mercapto, trifluoromethyl, amino, alkyl, alkoxy, alkylthio, alkylamino, or alkoxycarbonyl, the C-content of which can be from 1 to 5, phenyl, cyano, carboxy, or carbamoyl; R4, R5 and R6 stand independently for hydrogen, trifluoromethyl, alkyl, carbamoyl, alkoxycarbonyl, or alkyloxo, the C-content of which can be from 1 to 5; X stands for oxygen, N-OH, N-O-alkyl, dialkoxy, cyclic dialkoxy, dialkylthio, or cyclic dialkylthio, the C-content of which can be from 1 to 5. The present compounds are of value in the human and veterinary practice as systemic and topical therapeutic agents for the treatment and prophylaxis of asthma, allergy, rheumatoid arthritis, spondyloarthritis, gout, atherosclerosis, chronic inflammatory bowel disease, proliferative and inflammatory skin disorders, such as psoriasis, and atopic dermatitis.

Composés représentés par la formule suivante (I) dans laquelle R1 et R2 représentent indépendamment un ou plusieurs substituants semblables ou différents sélectionnés dans le groupe constitué par hydrogène, halogène, hydroxy, mercapto, trifluorométhyle, amino, alkyle, alkoxy, alkylthio, alkylamino ou alkoxycarbonyle, dont la teneur en C peut être de 1 à 5, cyano, carboxy, carbamoyle, phényle ou nitro; R3 représente hydrogène, halogène, hydroxy, mercapto, trifluorométhyle, amino, alkyle, alkoxy, alkylthio, alkylamino ou alkoxycarbonyle, dont la teneur en C peut être de 1 à 5, phényle, cyano, carboxy ou carbamoyle; R4, R5 et R6 représentent indépendamment hydrogène, trifluorométhyle, alkyle, carbamoyle, alkoxycarbonyle ou alkyloxo, dont la teneur en C peut être de 1 à 5; X représente oxygène, N-OH, N-O- alkyle, dialkoxy, dialkoxy cyclique, dialkylthio ou dialkylthio cyclique, dont la teneur en C peut être de 1 à 5. Ces composés sont utiles dans les domaines médicaux et vétérinaires en tant qu'agents thérapeutiques systémiques et topiques pour le traitement et la prophylaxie de l'asthme, de l'allergie, de la polyarthrite rhumatoïde, de la spondylarthrite, de la goutte, de l'athérosclérose, de la maladie chronique intestinale inflammatoire, de maladies de la peau prolifératives et inflammatoires, telles que le psoriasis et l'eczéma constitutionnel.

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