Title: |
Tricyclic Pyrimidines As Inhibitors of DYRK1A/DYRK1B As Potential Treatment for Down’s Syndrome or Alzheimer’s Disease |
Patent/Patent Application Number: |
WO 2013/026806A1 |
Publication date: |
February 28, 2013 |
Priority Application: |
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Priority date: |
August 17, 2012 |
Inventors: |
Leblond, B.; Casagrande, A.-S.; Désiré, L.; Foucourt A.; Besson, T. |
Assignee Company: |
Exonhit SA |
Disease Area: |
Alzheimer’s disease, Down’s Syndrome |
Biological Target: |
DYRK1A/DYRK1B |
Summary: |
The patent application claims tricyclic pyrimidine derivatives as inhibitors of dual-specific tyrosine-regulated kinases (DYRKs) for the treatment of Alzheimer’s disease or Down’s Syndrome. |
Important Compound Classes: |
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Key Structures: |
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Biological Assays: |
Sixty-seven compounds described in this invention were evaluated for their ability to inhibit DYRK1A and DYRK1B using an in vitro kinase functional assay |
Pharmacological Data: |
Inhibition of DYRK1A and DYRK1B |
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Synthesis: |
Synthesis of 89 examples is described |