2-substituted 4,5-diaryl imidazoles

Details 2-substituted 4,5-diaryl imidazoles 2-substituted 4,5-diaryl imidazoles

C - Chemistry, Metallurgy

07

D

C07D 401/04 (2006.01) A61K 31/44 (2006.01) A61K 31/445 (2006.01) A61K 31/695 (2006.01) C07D 401/14 (2006.01) C07D 403/04 (2006.01) C07D 451/02 (2006.01) C07F 7/08 (2006.01)

Patent

CA 2291758

Novel 2-substituted 4,5-diaryl imidazoles in which: i) the nitrogen atom at the 1 position is substituted by a trialkylsilyl-containing substituent, or ii) the substituent at the 2 position is arylalkyl, arylsulfonyl, arylthio arylseleno, aryltelluro, cycloalkyl, cycloalkenyl, alkylcycloalkyl, alkylcycloalkenyl, amino or hydrazino, or mono- or bicyclic N-heterocyclyl in which the N containing ring has six ring members, are provided, in particular compounds of Formula (I) wherein R1, R2, R3 and R4 are as defined, in free or pharmaceutically-acceptable acid additon salt or physiologically-cleavable ester form, which have p38 MAP kinase (Mitogen Activated Protein Kinase) inhibiting activity. The compounds are used as pharmaceuticals for treating TNF.alpha. and IL-1 mediated diseases such as rheumatoid arthritis and diseases of bone metabolism, e.g. osteoporosis.

L'invention concerne des nouvelles 4,5-diaryle imidazoles substituées en position 2, et dans lesquelles: i) l'atome d'azote situé en position 1 est substitué par un substituant contenant trialkylsilyle, ou ii) le substituant en position 2 est arylalkyle, arylsulfonyle, arylthio, arylséléno, aryltelluro, cycloalkyle, cycloalcényle, alkylcycloalkyle, alkylcycloalcényle, amino ou hydrazino, ou bien monocyclique-N-hérérocyclyle ou bicyclique-N-hétérocyclyle où le noyau contenant N possède six chaînons. L'invention concerne notamment des composés correspondant à la formule (I) dans laquelle R¿1?, R¿2?, R¿3? et R¿4? sont tels que décrits, sous forme libre ou de sel d'addition d'acide pharmacocompatible, ou sous forme d'ester clivable physiologiquement. Ces composés possèdent une activité inhibitrice des p38 MAP kinases (kinases activées par mitogènes) et ils sont utiles en tant que médicaments destinés au traitement de maladies induites par TNF-.alpha. et IL-1, comme la polyarthrite rhumatoïde, et de maladies du métabolisme osseux, comme par exemple l'ostéoporose.

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