3-(5)-HETEROARYL-SUBSTITUTED PYRAZOLES AS KINASE P38 INHIBITORS

FIELD: organic chemistry and pharmaceutical compositions. ^ SUBSTANCE: invention relates to new 3-(5)-heteroaryl-substituted pyrazoles of formula I , tautomers or pharmaceutically acceptable salt of compounds and tautomers. In formula R1 is hydride, piperidinyl substituted with methyl, lower alkyl o...

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Hauptverfasser: KLEHR MAJKL, STILI MAJKL A, GEHN LIFEHN, UIEHR RICHARD M, KHANSON GUNNAR DZH, PARTIS RICHARD A, ANANTANARAJAN ASHOK
Format: Patent
Sprache:eng ; rus
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Zusammenfassung:FIELD: organic chemistry and pharmaceutical compositions. ^ SUBSTANCE: invention relates to new 3-(5)-heteroaryl-substituted pyrazoles of formula I , tautomers or pharmaceutically acceptable salt of compounds and tautomers. In formula R1 is hydride, piperidinyl substituted with methyl, lower alkyl optionally substituted with halogen, hydroxyl, lower alkylanimo or morpholino; R2 is hydride, lower alkyl, amino, aminocarbonylamino, lower alkylaminocarbonylamino, lower alkylsulfonylamino, aminosulfonylamino, lower alkylaminosulfonylamino; Ar1 is phenyl optionally substituted with one or more independently selected halogen; HetAr2 is pyridinyl with the proviso that R2 is not amino or n-propyl when HetAr2 is pyridinyl; and HetAr2 is not 2-pyriridinyl when R2 is hydrogen or lower alkyl. Compounds of formula I have kinase p38 inhibitor activity and are useful in pharmaceutical compositions for treatment of various diseases. ^ EFFECT: new effective kinase p38 inhibitors. ^ 23 cl, 6 dwg, 1 tbl, 1 ex