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editorial
. 2014 Aug 7;5(10):1069. doi: 10.1021/ml5003019

Triazolo Derivatives as Inhibitors of PDE10A

Jean-Francois Brazeau , Gerard Rosse †,‡,*
PMCID: PMC4669985  PMID: 26677404

Title: Triazolo Derivatives as Inhibitors of PDE10A
Patent/Patent Application Number: WO 2013/178512 A1 Publication Date: December 5, 2013
Priority Application: EP 2012-1696954 Priority Date: May 30, 2012
Inventors: Flohr, A.; Groebke Zbinden, K.; Kuhn, B.; Lerner, C.; Rudolph, M.; Schaffhauser, H.
Assignee Company: Hoffmann-La Roche Inc.
Disease Area: CNS Biological Target: PDE10A
Summary: The present application discloses a series of triazolo analogues capable of inhibiting the activity of PDE10A, a unique enzyme from the phosphodiesterase family. It is suggested that this enzyme plays a key role in various physiological functions and diseases that can be treated by PDE10A inhibitors including, but not limited to, certain psychotic and neurodegenerative disorders such as schizophrenia, acute stress disorder, drug addictions, obsessive/compulsive disorders, movement disorders, cognition deficiency disorders, and bipolar disorders.
Important Compound Classes: graphic file with name ml-2014-003019_0002.jpg
Key Structures: graphic file with name ml-2014-003019_0001.jpg
Recent Review Articles: Menniti F. S.; Chappie T. A.; Humphrey J. M.; Schmidt C. J.. Curr. Opin. Invest. Drugs 2007, 8, 54–59.
Biological Assay: Compound efficacy was evaluated using cAMP binding assay.
Pharmacological Data: graphic file with name ml-2014-003019_0005.jpg
Synthesis: 136 compounds were synthesized

The authors declare no competing financial interest.


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