BENZOPHENONES AS INHIBITORS OF IL-1 BETA AND TNF-ALPHA, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND USE OF THEM FOR PRODUCING PHARMACEUTICAL COMPOSITIONS

摘要

The present invention relates to a compound of formula (I) wherein R1 is primarily halogen, hydroxy, mercapto, cyano, nitro, amino, alkyl, alkenyl, alkoxy, alkylthio, alkoxycarbonyl, alkylcarbonyloxy, -CONR9R10 wherein R9 and R10 are independently hydrogen, alkyl or aryl; R2 is primarily one or more, the same or different, selected from hydrogen, halogen, haloalkyl, hydroxy, mercapto, cyano, carboxy, nitro, amino, alkyl, alkenyl, alkoxy, alkylthio, alkylamino; a substituent selected from the group consisting of alkoxycarbonyl, -CONR9R10-; R3 is primarily an ortho substituent selected from the group consisting of hydrogen, halogen, haloalkyl, hydroxy, mercapto, cyano, nitro, amino, alkyl, alkenyl, alkoxy, alkylthio, alkoxycarbonyl, -CONR9R10. selected from; R4 is primarily hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, carboxy or aryl; R5 is a heteroaromatic mono-or bicyclic ring containing from 1 to 4 heteroatoms other than triazine and the ring system is optionally substituted X is O, S, N-OH or N R11 wherein R11 is hydrogen or alkyl; and salts, hydrates and solvates thereof, and optionally N-oxides thereof, with pharmaceutically acceptable acids, wherein a nitrogen atom of the R 5 heterocyclyl substituent is oxidized. The present invention also relates to the use of a compound of formula (I) in the manufacture of a medicament for the treatment or prevention of an inflammatory disease or condition, and to a pharmaceutical composition comprising the compound of formula (I) as an active ingredient. Examples of treatable disease include asthma, allergy, arthritis, atherosclerosis, inflammatory bowel syndrome, Crohn's syndrome. HE