Pyrazole derivatives for the inhibition of cdk' s and gsk' s

Details Pyrazole derivatives for the inhibition of cdk' s and gsk' s Pyrazole derivatives for the inhibition of cdk' s and gsk' s

C - Chemistry, Metallurgy

07

D

C07D 401/14 (2006.01) A01N 43/56 (2006.01) A61K 31/44 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2593656

The invention provides compounds of the formula (I), or salts, tautomers, N- oxides or solvates thereof wherein: R1 is selected from: (a) 2,6- dichlorophenyl; (b) 2,6-difluorophenyl; (c) a 2,3,6-trisubstituted phenyl group wherein the substituents for the phenyl group are selected from fluorine, chlorine, methyl and methoxy; (d) a group R0; (e) a group R a; (f) a group Rlb; (g) a group Rlc; (h) a group Rld; and 0) 2,6-difluorophenylamino ; wherein R )0.upsilon., r R> llaa, T Rj I1bD, T R) I1cC, r R> Iid.alpha., r R»2zaa, r R>22bD and RJ are as defined in the claims. The compounds have activity as inhibitors of cdk kinase (such as cdkl or cdk2) and glycogen synthase kinase-3 activity.

La présente invention concerne des composés de formule (I), ou leurs sels, tautomères, N-oxydes ou solvates, où : R1 est choisi parmi : (a) le 2,6-dichlorophényle ; (b) le 2,6-difluorophényle; (c) un groupe phényle 2,3,6-trisubstitué dans lequel les substituants du groupe phényle sont choisis parmi le fluor, le chlore, le méthyle et le méthoxy; (d) un groupe R0; (e) un groupe R1a ; (f) un groupe R1b ; (g) un groupe R1c ; (h) un groupe R1d ; et (j) un 2,6-difluorophénylamino ; R0, R1a, R1b, R1c, R1d, R2a, R2b et R3 étant tels que définis dans les revendications. Ces composés présentent une activité d'inhibition de l'activité des kinases cdk (telles que cdk1 ou cdk2) et de l'activité de la glycogène synthase kinase-3.

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