FIELD: medicine, pharmaceutics.
SUBSTANCE: present invention refers to new imidazolone derivatives used as drugs being kinase inhibitors, described by formula (I), wherein; R1 represents a C1-C3 alkyl radical or a hydrogen atom, and/or an aryl radical, Ar1 is specified in or , R represents the group R2-S-, R2 is thereby specified in the radicals like T1-(CH2)n, wherein n=0, 1, 2 or 3, and T1 represents a metal, vinyl, alkyl, alkynyl, nitrile, C3- or C4-cycloalkyl radical, hal, Z-O, Z-CO, wherein Z represents C1-C3 alkyl or hal, hal represents F, Cl, Br or I, or the group CCl3, or the group R3-NH-, R3 is thereby specified in the radicals like T2-(CH2)n, wherein n=0, 1 or 2, and T2 represents a metal, vinyl radical, Z-O, Z-CONH-, -CH-(OZ)2, ZCO, wherein Z represents H or C1-C4 linear or branched alkyl, NH2, C3-cycloalkyl, aryl, substituted aryl, or R3 represents H, or the group R4-CONH-, R4 is thereby specified in C3-C5 branched alkyl, or Ar2 - or Ar2-3-, Ar2 is specified in a phenyl radical, substituted phenyl or benzodioxolyl; and have IC50 less than 5 mcM.
EFFECT: invention also refers to pharmaceutical compositions based on the compounds of formula I for treating neurodegenerative disorders and to using these compounds as DYRKIA inhibitors.
11 cl, 2 tbl, 8 ex
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Authors
Dates
2013-08-27—Published
2008-08-01—Filed