The present invention is in the field of
medicinal chemistry. In particular, the present invention relates to a new class of
small molecule compounds having a 6,6-heterocyclic structure (e.g., naphthyridine, pyrido-
pyridazine, pyrido-
pyrazine,
quinoline, pyrazino-
pyridazine, pyrimido-
pyrimidine,
quinazoline,
quinoxaline, or cinnoline ring
system) that inhibit the activity of DYRK1A, DYRK1B, DYRK2, DYRK3, CLK1, CLK2, CLK3, CLK4, CDK7, CDK8 / 19, PI3K,
PDGFrA / B, mTOR, WNT, homeodomain-interacting
kinase (HIPK), and / or CMGC-
kinase. The present invention relates to compounds that function as inhibitors of WNT enzymes, leading to the inhibition of WNT signaling, and the use of those compounds as therapeutic agents for the treatment of Alzheimer's
disease, Down'
s syndrome, Parkinson's
disease, Huntington's
disease, diabetes, autoimmune diseases, inflammatory disorders (e.g.,
airway inflammation,
osteoarthritis (e.g., knee-related
osteoarthritis)),
cancer (e.g.,
glioblastoma,
prostate cancer,
metastatic breast cancer, metastatic
lung cancer,
multiple myeloma, secondary metastatic tumors of the brain, colon cancer and metastatic colon cancer (e.g., metastatic colon cancer to the liver)), and other diseases.