Pyrazole-derivatives as p38 kinase inhibitors

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 403/04 (2006.01) C07D 401/14 (2006.01) C07D 405/14 (2006.01) C07F 9/02 (2006.01) C07F 9/59 (2006.01) C07F 9/6558 (2006.01)

Patent

CA 2488402

This invention is directed generally to pyrazoles that, inter alia, inhibit p38 kinase, TNF, and/or cyclooxygenase-2 activity. Such pyrazoles include compounds generally corresponding in structure to the following formula (I), wherein L1, L2,Xl, X2, X3, X4, X5, X6, Rl, R3A, R3b,R3C, R4, and R5 are as defined in this specification. The pyrazoles further include tautomers of such compounds, as well as salts of such compounds and tautomers. This invention also is directed to compositions of such pyrazoles, intermediates for the syntheses of such pyrazoles, methods for making such pyrazoles, and methods for treating (including preventing) conditions (particularly pathological conditions) associated with p38 kinase, TNF, and/or cyclooxygenase-2 activity.

La présente invention concerne de manière générale des pyrazols qui, en autres, inhibent l'activité de la p38 kinase, de TNF, et de la cyclooxygénase-2. Ces pyrazols comprennent des composés dont la structure correspond de manière générale à la formule (I) dans laquelle L?1¿, L?2¿, X?l¿, X?2¿, X?3¿, X?4¿, X?5¿, X?6¿, R?l¿, R?3A¿, R?3b¿¿, ?R?3C¿¿,? R?4¿, et R?5¿ ont les correspondances indiquées dans cette spécification. Les pyrazols comprennent également des tautomères de ces composés ainsi que des sels de ces composés et de ces tautomères. L'invention a également pour objet des compositions de ces pyrazols, des intermédiaires de la synthèse de ces pyrazols, des procédés pour préparer ces pyrazols, et des procédés pour traiter (y compris prévenir) les états (en particulier les états pathologiques) associés à l'activité de la p38 kinase, de TNF, et/ou de la cyclooxygénase-2.

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