Inhibitors of histone demethylases

摘要

The present application discloses compounds capable of modulating the activity of histone demethylases (HDMEs), which are useful for prevention and/or treatment of diseases in which genomic dysregulation is involved in the pathogenesis, such as e.g. cancer. The present application also discloses pharmaceutical compositions comprising said compounds and the use of such compounds as a medicament. The compounds take the form (I);

主权项

1. A compound according to the formula:wherein:
R12 is R13O—, wherein R13 is C1-4 alkyl; A is —CHR2C(O)—; Y is —NR6R7; R1 is —H or methyl; R2 is —H, methyl or hydroxymethyl; Z is a single bond; each of R6 and R7 is independently selected from —H, C1-8 alkyl, C1-4 fluoroalkyl, and C1-4 hydroxyalkyl, wherein alkyl may optionally be substituted with one or more independently selected R8; each R8 is independently selected from C1-6 alkyl, C1-4 fluoroalkyl, C1-4 hydroxyalkyl, —Z—NR10R11, —Z—C(═O)—NR10R11, —Z—OR9, halogen, and —Z—COOR9; and each R9 is independently selected from —H and C1-8 alkyl; and each R10 and R11 is independently selected from —H and C1-6 alkyl; or a pharmaceutically acceptable salt thereof.