1400633-76-2Relevant academic research and scientific papers
Discovery and SAR of novel series of imidazopyrimidinones and dihydroimidazopyrimidinones as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu5)
Martín-Martín, María Luz,Bartolomé-Nebreda, José Manuel,Conde-Ceide, Susana,Alonso De Diego, Sergio A.,López, Silvia,Martínez-Viturro, Carlos M.,Tong, Han Min,Lavreysen, Hilde,Macdonald, Gregor J.,Steckler, Thomas,Mackie, Claire,Bridges, Thomas M.,Daniels, J. Scott,Niswender, Colleen M.,Noetzel, Meredith J.,Jones, Carrie K.,Conn, P. Jeffrey,Lindsley, Craig W.,Stauffer, Shaun R.
, p. 1310 - 1317 (2015/04/13)
We report the discovery and SAR of two novel series of imidazopyrimidinones and dihydroimidazopyrimidinones as metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulators (PAMs). Exploration of several structural features in the western and eastern part of the imidazopyrimidinone core and combinations thereof, revealed compound 4a as a mGlu5 PAM with good in vitro potency and efficacy, acceptable drug metabolism and pharmacokinetic (DMPK) properties and in vivo efficacy in an amphetamine-based model of psychosis. However, the presence of CNS-mediated adverse effects in preclinical species precluded any further in vivo evaluation.
SUBSTITUTED IMIDAZOPYRIMIDIN-5(6H)-ONES AS ALLOSTERIC MODULATORS OF MGLUR5 RECEPTORS
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Paragraph 0555; 0556, (2013/09/26)
In one aspect, the invention relates to imidazopyrimidin-5(6H)-one analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
SUBSTITUTED IMADAZAPYRINIDIN-5(6H)-ONES AS ALLOSTERIC MODULATORS OF MGLUR5 RECEPTORS
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Page/Page column 197, (2012/10/07)
In one aspect, the invention relates to imidazopyrimidin-5(6H)-one analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
