4-aryl-2-anilino-pyrimidines as plk kinase inhibitors

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 498/08 (2006.01) A61K 31/529 (2006.01) A61P 19/00 (2006.01) A61P 25/00 (2006.01) A61P 35/00 (2006.01) C07D 471/08 (2006.01) C07D 471/18 (2006.01) C07D 471/22 (2006.01) C07D 498/18 (2006.01)

Patent

CA 2716079

The present invention relates to compounds of Formula (Ia) or (Ib), the N- oxide forms, pharmaceutically acceptable addition salts, quaternary amines, stereoisomers, tautomers, racemics, metabolites, prodrugs, hydrates, or solvates thereof, wherein Y1, m, n, R1; X1; X1; R2; X3; X4; R3; and R4 have the meaning defined in the claims. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use in therapy. The invention particularly relates to compounds that are kinase inhibitors useful for the treatment of disease states mediated by kinase, especially PLK4, in particular such compounds that are useful in the treatment of pathological processes which involve an aberrant cellular proliferation, such as tumor growth, rheumatoid arthritis, restenosis and atherosclerosis.

L'invention concerne des composés représentés par la formule (Ia) ou (Ib), des formes de N-oxyde, des sels d'addition pharmaceutiquement acceptables, des amines quaternaires, des stéréo-isomères, des tautomères, des racémiques, des métabolites, des promédicaments, des hydrates ou des solvates de ces composés. Dans les formules, Y1, m, n, R1, X1, X2, R2, X3, X4, R3 et R4 ont les notations définies dans les revendications. L'invention concerne aussi des procédés de préparation de ces composés, des compositions pharmaceutiques contenant ceux-ci et l'utilisation thérapeutique de celles-ci. L'invention concerne en particulier des composés constituant des inhibiteurs de kinases et qui sont utiles dans le traitement d'états pathologiques dans lesquels intervient une kinase, spécialement la PLK4, notamment des composés utiles dans le traitement de processus pathologiques impliquant une prolifération cellulaire aberrante telle que la croissance tumorale, la polyarthrite rhumatoïde, la resténose et l'athérosclérose.

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