874449-99-7Relevant academic research and scientific papers
Novel alpha-7 nicotinic acetylcholine receptor agonists containing a urea moiety: Identification and characterization of the potent, selective, and orally efficacious agonist 1-[6-(4-Fluorophenyl)pyridin-3-yl]-3-(4-piperidin-1- ylbutyl) Urea (SEN34625/WYE-103914)
Ghiron, Chiara,Haydar, Simon N.,Aschmies, Suzan,Bothmann, Hendrick,Castaldo, Cristiana,Cocconcelli, Giuseppe,Comery, Thomas A.,Di, Li,Dunlop, John,Lock, Tim,Kramer, Angela,Kowal, Dianne,Jow, Flora,Grauer, Steve,Harrison, Boyd,La Rosa, Salvatore,MacCari, Laura,Marquis, Karen L.,Micco, Iolanda,Nencini, Arianna,Quinn, Joanna,Robichaud, Albert J.,Roncarati, Renza,Scali, Carla,Terstappen, Georg C.,Turlizzi, Elisa,Valacchi, Michela,Varrone, Maurizio,Zanaletti, Riccardo,Zanelli, Ugo
experimental part, p. 4379 - 4389 (2010/09/04)
Alpha-7 nicotinic acetylcholine receptor (α7 nAChR) agonists are promising therapeutic candidates for the treatment of cognitive impairment. We report a series of novel, potent small molecule agonists (4-18) of the α7 nAChR deriving from our continuing efforts in the areas of Alzheimer's disease and schizophrenia. One of the compounds of the series containing a urea moiety (16) was further shown to be a selective agonist of the α7 nAChR with excellent in vitro and in vivo profiles, brain penetration, and oral bioavailability and demonstrated in vivo efficacy in multiple behavioral cognition models. Structural modifications leading to the improved selectivity profile and the biological evaluation of this series of compounds are discussed.
MODULATORS OF ALPHA7 NICOTINIC ACETYLCHOLINE RECEPTORS AND THERAPEUTIC USES THEREOF
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Page/Page column 32; 44; 46; 58, (2010/02/15)
The present invention relates to compounds with α7 nAChR agonistic activity, processes for their preparation, pharmaceutical compositions containing the same and the use thereof for the treatment of neurological, psychiatric, cognitive, immunological and inflammatory disorders.
