Aminopyrazole derivatives

Details Aminopyrazole derivatives Aminopyrazole derivatives

C - Chemistry, Metallurgy

07

D

C07D 401/04 (2006.01) A61K 31/4439 (2006.01) A61K 31/4709 (2006.01) A61P 1/00 (2006.01) A61P 3/00 (2006.01) A61P 7/00 (2006.01) A61P 9/00 (2006.01) A61P 11/00 (2006.01) A61P 17/00 (2006.01) A61P 19/00 (2006.01) A61P 21/00 (2006.01) A61P 25/00 (2006.01) A61P 27/00 (2006.01) A61P 29/00 (2006.01) A61P 31/00 (2006.01) A61P 37/00 (2006.01) A61P 43/00 (2006.01) C07D 401/14 (2006.01) C07D 405/14 (2006.01) C07D 409/14 (2006.01)

Patent

CA 2356263

Aminopyrazole derivatives represented by formula (I), or salts thereof, wherein X1 and X2 are each a hydrogen atom or a halogen atom, or X1 and X2 may be united together to form a lower alkylenedioxy group, Q is a pyridyl group or a quinolyl group, R1 is a hydrogen atom, a substituted or unsubstituted lower alkyl or aryl group, R2 is a hydrogen atom, a lower alkyl group, or an aralkyl group, and R3 represents a hydrogen atom, an organic sulfonyl group, or -C(=Y)-R4 in which R4 is a hydrogen atom or an organic residue and Y is an oxygen or sulfur atom, provided that, when R3 is a hydro-gen atom, R1 is a group other than a hydrogen atom and R2 is a hydrogen atom. These aminopyrazole derivatives or their salts have excellent p38MAP kinase inhibiting activities and are hence useful in the prevention or treatment of diseases associated with tumor necro-sis factor .alpha., interleukin 1, interleukin 6 or cyclooxygenase II.

L'invention concerne des dérivés d'aminopyrazole de la formule générale (I) ou des sels desdits dérivés, qui présentent une excellente activité d'inhibition de la kinase p38MAP et sont utiles pour la prévention ou le traitement de maladies liées au facteur de nécrose tumorale alpha, à l'interleukine 1, à l'interleukine 6 ou à la cyclo-oxygénase II. Dans ladite formule, X<1> et X<2> sont chacun hydrogène ou halogéno, ou bien X<1> et X<2> peuvent être mis ensemble pour former alkylènedioxy inférieur; Q est pyridyle ou quinolyle; R<1> est hydrogène ou alkyle inférieur éventuellement substitué ou aryle; R<2> est hydrogène, alkyle inférieur ou aralkyle; R<3> est hydrogène, un groupe sulfonyle organique, ou -C(=Y)-R<4>; R<4> est hydrogène ou un résidu organique; et Y est oxygène ou soufre, à condition que, lorsque R<3> est hydrogène, R<1> n'est pas hydrogène et R<2> est hydrogène.

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