- N-[5-(5-fluoropyridin-3-yl)-1H-pyrazol-3-yl]-4-piperidin-1-ylbutyramide (SEN78702, WYE-308775): A medicinal chemistry effort toward an α7 nicotinic acetylcholine receptor agonist preclinical candidate
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α7 nicotinic acetylcholine receptors (α7 nAChR) represent promising therapeutic candidates for the treatment of cognitive impairment associated with Alzheimer's disease (AD) and schizophrenia. A medicinal chemistry effort around previously reported compound 1 (SEN15924, WAY-361789) led to the identification of 12 (SEN78702, WYE-308775) a potent and selective full agonist of the α7 nAChR that demonstrated improved plasma stability, brain levels, and efficacy in behavioral cognition models.
- Zanaletti, Riccardo,Bettinetti, Laura,Castaldo, Cristiana,Ceccarelli, Ilaria,Cocconcelli, Giuseppe,Comery, Thomas A.,Dunlop, John,Genesio, Eva,Ghiron, Chiara,Haydar, Simon N.,Jow, Flora,Maccari, Laura,Micco, Iolanda,Nencini, Arianna,Pratelli, Carmela,Scali, Carla,Turlizzi, Elisa,Valacchi, Michela
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p. 10277 - 10281
(2013/01/16)
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- NICOTINIC ACETYLCHOLINE RECEPTOR MODULATORS
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The present invention provides compounds of formula (I) and compositions thereof, methods of making them, and methods of using them to modulate alpha7 nicotinic acetylcholine receptors and/or to treat any of a variety of disorders, diseases, and conditions. Provided compounds can affect, among other things, neurological, psychiatric and/or inflammatory system.
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Page/Page column 144; 153
(2008/12/07)
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