COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS

摘要

The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of B-Raf.

主权项

1. A compound of Formula Ia: in which: Y is selected from N and CR6; R2 R3, R5 and R6 are independently selected from hydrogen, halo, cyano, C1-4alkyl, halo-substituted-C1-4alkyl, C1-4alkoxy and halo-substituted-C1-4alkoxy; with the proviso that when R5 is fluoro and R1 is selected from hydrogen, —XR8a, —X1OX2R8a, —X1C(O)NR8aR8b, —X1NR8aX2R8b, —X1NR8aC(O)X2ORB and —X1NR8aS(O)0-2R8b, R3 and R6 are not both hydrogen; R4 is selected from —R9 and —NR10R11; wherein R9 is selected from C1-6alkyl, C3-8cycloalkyl, C3-8heterocycloalkyl, aryl and heteroaryl; wherein said alkyl, cycloalkyl, heterocycloalkyl, aryl or heteroaryl of R9 is optionally substituted with 1 to 3 radicals independently selected from halo, cyano, C1-4alkyl, halo-substituted-C1-4alkyl, C1-4alkoxy and halo-substituted-C1-4alkoxy; and R10 and R11 are independently selected from hydrogen and R9; R7 is selected from hydrogen, C1-4alkyl, C3-5cycloalkyl and C3-5heterocycloalkyl; wherein said alkyl, cycloalkyl or heterocycloalkyl of R7 is optionally substituted with 1 to 3 radicals independently selected from halo, cyano, hydroxyl, C1-4alkyl, halo-substituted-C1-4alkyl, C1-4alkoxy and halo-substituted-C1-4alkoxy; or the tautomers, prodrugs, stereoisomers or pharmaceutically acceptable salts thereof.