Pteridine derivatives as polo-like kinase inhibitors useful...

C - Chemistry – Metallurgy – 07 – D

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C07D 475/00 (2006.01) A61K 31/519 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2665736

Compound of formula (I) are inhibitors of Polo-like kinases (PLKs), and are useful in treatment of cell proliferative diseases: wherein R1 and R2 are hydrogen, or an optionally substituted (C1-C6)alkyl, (C2- C6)alkenyl, (C2-C6)alkynyl or (C3-C6)cycloalkyl group; R3 and R3' are independently selected from hydrogen, -CN, hydroxyl, halogen, optionally substituted (C1-C6) alkyl, (C2- C6)alkenyl, (C2-C6)alkynyl or (C3-C6)cycloalkyl, -NR5R6 or C1-C4 alkoxy, wherein R5 and R6 are independently hydrogen or optionally substituted (C1-C6)alkyl; ring A is an optionally substituted mono- or bi-cyclic carbocyclic or heterocyclic ring or a ring system having up to 12 ring atoms; T is a radical of formula R-L1 -Y1- wherein R is an alpha amino acid or alpha amino acid ester motif, linked to ring A by linker R-L1-Y1- as defined in the claims.

Les composés de formule (I) sont des inhibiteurs des Polo-like kinases (PLK) et sont utiles dans le traitement de maladies prolifératives des cellules, formule dans laquelle R1 et R2 sont chacun un hydrogène ou un groupe alkyle en C1-C6, alcényle en C2-C6, alkynyle en C2-C6 ou cycloalkyle en C3-C6 éventuellement substitué; R3 et R3' sont chacun indépendamment sélectionnés parmi un hydrogène, -CN, un hydroxyle, un halogène, un alkyle en C1-C6, alcényle en C2-C6, alkynyle en C2-C6 ou cycloalkyle en C3-C6 éventuellement substitué, -NR5R6 ou un alcoxy en C1-C4, R5 et R6 étant chacun indépendamment un hydrogène ou un alkyle en C1-C6 éventuellement substitué; le cycle A est un cycle ou système cyclique carbocyclique ou hétérocyclique monocyclique ou bicyclique éventuellement substitué ayant jusqu'à 12 atomes dans le cycle; T est un radical de formule R-L1-Y1- dans laquelle R est un motif alpha-aminoacide ou ester d'alpha-aminoacide, relié au cycle A par le groupe de liaison R-L1-Y1- tel que défini dans les revendications.

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