The identification of a novel series of Aurora kinase inhibitors and exploitation of their SAR is described. Replacement of the initial quinazoline core with a pyrimidine scaffold and modification of substituents led to a series of very potent inhibitors of cellular proliferation. MK-0457 (VX-680) has been assessed in Phase II clinical trials in patients with treatment-refractory chronic myelogenous leukemia (CML) or Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ALL) containing the T315I mutation.
La presente invention porte sur des composes utiles en tant qu'inhibiteurs de la proteine kinase. L'invention porte egalement sur des compositions pharmaceutiquement acceptables comprenant lesdits composes et sur des procedes d'utilisation des compositions dans le traitement de diverses maladies, etats ou troubles. L'invention concerne egalement des procedes pour preparer des composes de l'invention.