Synthesis of Vibegron Enabled by a Ketoreductase Rationally Designed for High pH Dynamic Kinetic Reduction
Described here is an efficient stereoselective synthesis of vibegron enabled by an enzymatic dynamic kinetic reduction that proceeds in a high-pH environment. To overcome enzyme performance limitations under these conditions, a ketoreductase was evolved by a computationally and structurally aided strategy to increase cofactor stability through tighter binding.
Xu, Feng,Kosjek, Birgit,Cabirol, Fabien L.,Chen, Haibin,Desmond, Richard,Park, Jeonghan,Gohel, Anupam P.,Collier, Steven J.,Smith, Derek J.,Liu, Zhuqing,Janey, Jacob M.,Chung, John Y. L.,Alvizo, Oscar
p. 6863 - 6867
(2018/05/08)
A process for producing an intermediate agonist GRK 3
The present invention is directed to processes for preparing beta 3 agonists of Formula (I) and Formula (II) and their intermediates. The beta 3 agonists are useful in the treatment of certain disorders, including overactive bladder, urinary incontinence, and urinary urgency.
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(2016/10/10)
PROCESS FOR PREPARING BETA 3 AGONISTS AND INTERMEDIATES
The application is directed to efficient and economical processes as described in more detail below for the preparation of the beta 3 agonists of the formula of I-7 and intermediate compounds that can be used for making these agonists. The present disclosure relates to a process for making beta-3 agonists and intermediates using ketoreductase (KRED) biocatalyst enzymes and methods of using the biocatalysts.
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(2014/10/04)
PROCESS FOR MAKING BETA 3 AGONISTS AND INTERMEDIATES
The present invention is directed to processes for preparing beta 3 agonists of Formula (I) and Formula (II) and their intermediates. The beta 3 agonists are useful in the treatment of certain disorders, including overactive bladder, urinary incontinence, and urinary urgency.
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(2013/05/21)
COMBINATION THERAPY USING A BETA 3 ADRENERGIC RECEPTOR AGONIST AND AN ANTIMUSCARINIC AGENT
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.
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(2011/04/26)
HYDROXYMETHYL PYRROLIDINES AS BETA 3 ADRENERGIC RECEPTOR AGONISTS
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.
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(2009/10/17)
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