Substituted pyrazole compounds

Details Substituted pyrazole compounds Substituted pyrazole compounds

C - Chemistry, Metallurgy

07

D

C07D 401/14 (2006.01) A61K 31/444 (2006.01)

Patent

CA 2375986

(see formula I) Substituted pyrazole compounds represented by formula (I), or salts thereof are disclosed, wherein R1 is -CH(OH)-CH(R4)-(A)n -Y, -CH2 -CH(R4)-(A)n-Y, -CO-B1-A-Y or the like (wherein A is a lower alkylene; Y is an aryl group which may be substituted, for example, by halogen, or the like; R4 is a hydrogen atom or a lower alkyl group; B1 is -CH(R4)- or -N(R4)-; and n is 0 or 1); R2 is a hydrogen atom, a lower alkyl group which may be substituted by hydroxyl or the like, or an aralkyl group; R3 is a phenyl group which may be substituted by halogen or the like, or a pyridyl group; and Q is a pyridyl or quinolyl group. These substituted pyrazole compounds or their salts have an excellent p38MAP kinase inhibiting effect and are hence useful in the prevention or treatment of tumor necrosis factor .alpha.-related diseases, interleukin 1-related diseases, interleukin 6-related diseases or cyclooxygenase II-related diseases.

Cette invention concerne des composés à base de pyrazole substitué représentés par la formule (I), qui possèdent un excellent effet inhibiteur de la protéine p38 MAP kinase et qui conviennent pour la prévention ou le traitement des maladies en rapport avec le facteur de nécrose tumorale alpha , les maladies en rapport avec l'interleukine 1, les maladies en rapport avec l'interleukine 6 ou les maladies en rapport avec la cyclogénase II. Dans la formule (I), R<1> est -CH(OH)-CH(R<4>)-(A)n-Y, -CH2-CH(R<4>)-(A)n-Y, -CO-B<1>-A-Y, ou analogue (A étant un alkylène inférieur; Y un aryle qui peut être remplacé par halogéno ou analogue; R<4> hydrogène ou alkyle inférieur; B<1> CH(R<4>)- ou -N(R<4>)-; et n 0 ou 1); R<2> est hydrogène, alkyle inférieur pouvant être remplacés par hydroxyle ou analogue, ou aralkyle; R<3> est phényle pouvant être remplacé par halogéno ou analogue, ou pyridyle; et Q est pyridyle ou quinolyle.

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