898563-26-3Relevant articles and documents
RADIOLABELED PDE10A LIGANDS
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, (2014/02/15)
Compounds of formula (I) are disclosed Compounds of formula (I) are useful in treating conditions and disorders prevented by or ameliorated by PDE10A ligands. Radiolabeled compounds of formula (I) are also useful as diagnostic tools as PDE10A positron emi
Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3- yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia
Verhoest, Patrick R.,Chapin, Douglas S.,Corman, Michael,Fonseca, Kari,Harms, John F.,Hou, Xinjun,Marr, Eric S.,Menniti, Frank S.,Nelson, Frederick,O'Connor, Rebecca,Pandit, Jayvardhan,Proulx-LaFrance, Caroline,Schmidt, Anne W.,Schmidt, Christopher J.,Suiciak, Judith A.,Liras, Spiros
experimental part, p. 5188 - 5196 (2010/03/01)
By utilizing structure-based drug design (SBDD) knowledge, a novel class of phosphodiesterase (PDE) 10A inhibitors was identified. The structure-based drug design efforts identified a unique "selectivity pocket" for PDE10A inhibitors, and interactions within this pocket allowed the design of highly selective and potent PDE10A inhibitors. Further optimization of brain penetration and drug-like properties led to the discovery of 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920). This PDE10A inhibitor is the first reported clinical entry for this mechanism in the treatment of schizophrenia.
Heteroaromatic quinoline compounds
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Page/Page column 28-29, (2008/06/13)
The invention pertains to heteroaromatic compounds that serve as effective phosphodiesterase (PDE) inhibitors. In particular, the invention relates to said compounds which are selective inhibitors of PDE10. The invention also relates to intermediates for preparation of said compounds; pharmaceutical compositions comprising said compounds; and the use of said compounds in a method for treating certain central nervous system (CNS) or other disorders.