1019108-35-0Relevant articles and documents
THIAZOLOPYRIMIDINONES AS MODULATORS OF NMDA RECEPTOR ACTIVITY
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, (2015/04/28)
The present invention relates to certain thiazolopyrimidinone compounds for use in modulating NMDA receptor activity, pharmaceutical compositions comprising such compounds and methods of treating neurological and psychiatric conditions.
Design, synthesis, and evaluation of conformationally restricted acetanilides as potent and selective β3 adrenergic receptor agonists for the treatment of overactive bladder
Moyes, Christopher R.,Berger, Richard,Goble, Stephen D.,Harper, Bart,Shen, Dong-Ming,Wang, Liping,Bansal, Alka,Brown, Patricia N.,Chen, Airu S.,Dingley, Karen H.,Di Salvo, Jerry,Fitzmaurice, Aileen,Gichuru, Loise N.,Hurley, Amanda L.,Jochnowitz, Nina,Miller, Randall R.,Mistry, Shruty,Nagabukuro, Hiroshi,Salituro, Gino M.,Sanfiz, Anthony,Stevenson, Andra S.,Villa, Katherine,Zamlynny, Beata,Struthers, Mary,Weber, Ann E.,Edmondson, Scott D.
, p. 1437 - 1453 (2014/03/21)
A series of conformationally restricted acetanilides were synthesized and evaluated as β3-adrenergic receptor agonists (β3-AR) for the treatment of overactive bladder (OAB). Optimization studies identified a five-membered ring as the preferred conformational lock of the acetanilide. Further optimization of both the aromatic and thiazole regions led to compounds such as 19 and 29, which have a good balance of potency and selectivity. These compounds have significantly reduced intrinsic clearance compared to our initial series of pyridylethanolamine β3-AR agonists and thus have improved unbound drug exposures. Both analogues demonstrated dose dependent β3-AR mediated responses in a rat bladder hyperactivity model.
COMBINATION THERAPY USING A BETA 3 ADRENERGIC RECEPTOR AGONIST AND AN ANTIMUSCARINIC AGENT
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Page/Page column 27, (2011/04/26)
Described herein is an improved method of treating overactive bladder, wherein the method comprises administering to a patient in need thereof a beta 3 adrenergic receptor agonist, an antimuscarinic agent, and an optional selective M2 antagonist. Such combination therapy provides improved efficacy and/or reduced side effects.
HYDROXYMETHYL PYRROLIDINES AS BETA 3 ADRENERGIC RECEPTOR AGONISTS
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Page/Page column 34, (2009/10/30)
The present invention provides compounds of Formula I, pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of β3-adrenoceptor.
HYDROXYMETHYL PYRROLIDINES AS BETA 3 ADRENERGIC RECEPTOR AGONISTS
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Page/Page column 29, (2009/10/17)
The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of β3-adrenoceptor.