3-(5)-HETEROARYL-SUBSTITUTED PYRAZOLES AS KINASE P38 INHIBITORS Russian patent published in 2005 - IPC

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