4-(9-(3, 3-DIFLUOROCYCLOPENTYL) -5, 7, 7-TRIMETHYL-6-OXO-6, 7, 8, 9-TETRAHYDRO-5H-PYRIMIDO [4, 5-B[1, 4] DIAZEPIN-2-YLAMINO)-3-METHOXYBENZAMIDE DERIVATIVES AS INHIBITORS OF THE HUMAN PROTEIN KINASES PLK1 TO PLK4 FOR THE TREATMENT OF PROLIFERATIVE DIS

摘要

Compounds of this invention, and pharmaceutically acceptable compositions thereof, are useful as inhibitors of PLK1 protein kinases. These compounds have the formula I, as defined herein or pharmaceutically acceptable salts thereof. These compounds, and pharmaceutically acceptable salts thereof, are useful for treating or preventing a variety of diseases, disorders or conditions, including, but not limited to, an autoimmune, inflammatory, proliferative, or hyperproliferative disease, a neurodegenerative disease, or an immunologically-mediated disease. Formula I wherein R1is (formula); R6 is C1-4 aliphatic or C3-6 cycloaliphatic, and is optionally substituted with 1 or 2 halogen atoms; X is O and R2 is -CH3; or X is NR5 and, R2 and R5, together with the atoms to which they are attached, form a 1,2,4-triazole; each of R3 and R4 is independently H, methyl, or ethyl; or R3 and R4, together with the atoms to which they are attached, form a cyclopropyl ring; and n is 0 or 1.