68867-17-4Relevant academic research and scientific papers
Design, synthesis, structure-activity relationship, and in vivo activity of azabicyclic aryl amides as α7 nicotinic acetylcholine receptor agonists
Walker, Daniel P.,Wishka, Donn G.,Piotrowski, David W.,Jia, Shaojuan,Reitz, Steven C.,Yates, Karen M.,Myers, Jason K.,Vetman, Tatiana N.,Margolis, Brandon J.,Jacobsen, E. Jon,Acker, Brad A.,Groppi, Vincent E.,Wolfe, Mark L.,Thornburgh, Bruce A.,Tinholt, Paula M.,Cortes-Burgos, Luz A.,Walters, Rodney R.,Hester, Matthew R.,Seest, Eric P.,Dolak, Lester A.,Han, Fusen,Olson, Barbara A.,Fitzgerald, Laura,Staton, Brian A.,Raub, Thomas J.,Hajos, Mihaly,Hoffmann, William E.,Li, Kai S.,Higdon, Nicole R.,Wall, Theron M.,Hurst, Raymond S.,Wong, Erik H.F.,Rogers, Bruce N.
, p. 8219 - 8248 (2007/10/03)
A novel set of azabicyclic aryl amides have been identified as potent and selective agonists of the α7 nAChR. A two-pronged approach was taken to improve the potential hERG liability of previously disclosed α7 nAChR agonist, PNU-282,987, while maintaining the compound's other desirable pharmacological properties. The first approach involved further exploration of the aryl carboxylic acid fragment of PNU-282,987, while the second approach focused on modification of the azabicyclic amine portion of PNU-282,987. The best compounds from each series are characterized by rapid brain penetration, good oral bioavailability in rat, and demonstrate in vivo efficacy in a rat P50 auditory sensory gating assay. At least one analog from each series (1h, 1o, 2a, 9a, and 18a) shows an improved hERG safety profile over PNU-282,987.
INDAZOLES, BENZOTHIAZOLES, BENZOISOTHIAZOLES, BENZISOXAZOLES, AND PREPARATION AND USES THEREOF
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Page/Page column 70-71, (2010/02/14)
The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nACh receptors), activation of nACh receptors, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (e.g., indazoles and benzothiazoles), which act as ligands for the α7 nACh receptor subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
INDAZOLES, BENZOTHIAZOLES, AND BENZOISOTHIAZOLES, AND PREPARATION AND USES THEREOF
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Page 67, (2008/06/13)
The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (indazoles and benzothiazoles), which act as ligands for the α7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
Aminopiperidine quinolines and their azaisosteric analogues with antibacterical activity
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, (2008/06/13)
Aminopiperidine derivatives of formula (I) and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly in man.
NITROGEN-CONTAINING BICYCLIC HETEROCYCLES FOR USE AS ANTIBACTERIALS
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Page/Page column 67, (2010/02/07)
Cyclohexane and cyclohexene derivatives and pharmaceutically acceptable derivatives hereof useful in methods of treatment of bacterial infections in mammals, particularly man.
Quinuclidine-substituted hetero-bicyclic aromatic compounds for the treatment of disease
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, (2008/06/13)
The invention provides compounds of Formula I: wherein W0 is a bicyclic moiety and is These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful to treat diseases or conditions in which α7 is known to be involved.
