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editorial
. 2013 Apr 26;4(6):502–503. doi: 10.1021/ml400137s
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:   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: graphic file with name ml-2013-00137s_0001.jpg
Key Structures: graphic file with name ml-2013-00137s_0002.jpg
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
  graphic file with name ml-2013-00137s_0003.jpg
  graphic file with name ml-2013-00137s_0004.jpg
Synthesis: Synthesis of 89 examples is described