- POLY (ADP-RIBOSE) POLYMERASE (PARP) INHIBITORS
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Compounds of the following formula are provided for use in inhibiting Poly (ADP-ribose) Polymerase (PARP): wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds,
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Page/Page column 77-78
(2010/11/04)
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- FUSED HETEROCYCLIC COMPOUND AND USE THEREOF
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The present invention relates to wherein each symbol is as defined in the specification. The compound has a superior mineral corticoidreceptorantagonistic action and is useful as an agent for the prophylaxis or treatment of hypertension, cardiac failure and the like, a compound having a fused heterocycle, or a prodrug thereof, or a salt thereof; and an agent for the prophylaxis or treatment of hypertension, cardiac failure and the like.
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Page/Page column 349-350
(2008/06/13)
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- Design, synthesis, structure-activity relationship, and in vivo activity of azabicyclic aryl amides as α7 nicotinic acetylcholine receptor agonists
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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.
- 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.
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p. 8219 - 8248
(2007/10/03)
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