Tricyclic Pyrimidines As Inhibitors of DYRK1A/DYRK1B As Potential Treatment for Down’s Syndrome or Alzheimer’s Disease

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:
Key Structures:
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
Synthesis:	Synthesis of 89 examples is described

The authors declare no competing financial interest.