76263-11-1Relevant articles and documents
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.
supporting information, 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 29, (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.
FUSED HETEROCYCLIC DERIVATIVES AS PPAR MODULATORS
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Page 91, (2008/06/13)
The present invention is directed to compounds represented by the following structural formula, Formula I: wherein (a) X is selected from the group consisting of a single bond, O, S. S(O)2 and N; (b) U is an aliphatic linker; (c) Y is selected from the group consisting of C, O, S, NH and a single bond; (d) E is C(R3) (R4)A or A and wherein (i) A is selected from the group consisting of carboxyl, tetrazole, C1-C6 alkylnitrile, carboxamidek, sulfonamide and acylsulfonamide; (e) B is selected from the group consisting of S, O, C, and N; (f) Z is selected from the group consisting of N and C; with the proviso that when B is C then Z is N.