1354404-40-2Relevant academic research and scientific papers
N-Methylanilide and N-methylbenzamide derivatives as phosphodiesterase 10A (PDE10A) inhibitors
Kilburn, John Paul,Kehler, Jan,Langgard, Morten,Erichsen, Mette N.,Leth-Petersen, Sebastian,Larsen, Mogens,Christoffersen, Claus Tornby,Nielsen, Jacob
, p. 6053 - 6062 (2013/09/23)
PDE10A is a recently identified phosphodiesterase with a quite remarkable localization since the protein is abundant only in brain tissue. Based on this unique localization, research has focused extensively on using PDE10A modulators as a novel therapeutic approach for dysfunction in the basal ganglia circuit including Parkinson's disease, Huntington's disease, schizophrenia, addiction and obsessive compulsive disorder. Medicinal chemistry efforts identified the N-methyl-N-[4-(quinolin-2-ylmethoxy)-phenyl]-isonicotinamide (8) as a nanomolar PDE10A inhibitor. A subsequent Lead-optimization program identified analogous N-methylanilides and their corresponding N-methylbenzamides (29) as potent PDE10A inhibitors, concurrently some interesting and unexpected binding modes were identified.
ARYL- AND HETEROARYLAMID DERIVATIVES AS PDE10A ENZYME INHIBITOR
-
Page/Page column 26, (2012/01/14)
The invention relates to compounds of the formula and their use as pharmaceutical ingredients, in particular for the treatment of CNS related diseases (PDE 10A inhibitors).
