Stephen D. Goble

Microscale High-Throughput Experimentation as an Enabling Technology in Drug Discovery: Application in the Discovery of (Piperidinyl)pyridinyl-1 H -benzimidazole Diacylglycerol Acyltransferase 1 Inhibitors

Tim Cernak, Nathan J. Gesmundo, Kevin D. Dykstra, Yang Yu et autres

Miniaturization and parallel processing play an important role in the evolution of many technologies. We demonstrate the application of miniaturized high-throughput experimentation methods to resolve synthetic chemistry challenges on the frontlines of a lead optimization effort to develop diacylglycerol acyltransferase (DGAT1) inhibitors. …

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Investigation of piperazine benzamides as human β3 adrenergic receptor agonists for the treatment of overactive bladder

Bart Harper, Liping Wang, Cheng Gang Zhu, Nam Fung Kar et autres

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CCDC 1421635: Experimental Crystal Structure Determination

Scott D. Edmondson, Cheng Gang Zhu, Nam Fung Kar, Jerry Di Salvo et autres

An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, …

Discovery of Vibegron: A Potent and Selective β3Adrenergic Receptor Agonist for the Treatment of Overactive Bladder

Scott D. Edmondson, Cheng Gang Zhu, Nam Fung Kar, Jerry Di Salvo et autres

The discovery of vibegron, a potent and selective human β3-AR agonist for the treatment of overactive bladder (OAB), is described. An early-generation clinical β3-AR agonist MK-0634 (3) exhibited efficacy in humans for the treatment of OAB, but development was discontinued due to …

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Design, Synthesis, and Evaluation of Conformationally Restricted Acetanilides as Potent and Selective β3Adrenergic Receptor Agonists for the Treatment of Overactive Bladder

Christopher R. Moyes, Richard S. Berger, Stephen D. Goble, Bart Harper et autres

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 …

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A review of 17 years of telephone calls to the Australian Diver Emergency Service (DES).

David M. Wilkinson, Stephen D. Goble

INTRODUCTION: The Diver Emergency Service (DES) in Australia provides specialised medical advice on diving incidents 24 hours a day to divers, dive operators, families and health professionals. It is operated from the Hyperbaric Medicine Unit of the Royal Adelaide Hospital where the …

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Heterocyclic acetamide and benzamide derivatives as potent and selective β3-adrenergic receptor agonists with improved rodent pharmacokinetic profiles

Stephen D. Goble, Liping Wang, Kobporn Lulu Howell, Alka Bansal et autres

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Discovery of a Potent and Orally Bioavailable CCR2 and CCR5 Dual Antagonist

Alexander O. Pasternak, Stephen D. Goble, Mary D. Struthers, Pasquale P. Vicario et autres

This report describes the discovery of a potent, orally bioavailable CC chemokine receptor 2 (CCR2) antagonist which, while optimized for CCR2 potency, also had potent CC chemokine receptor 5 (CCR5) activity.

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Discovery and optimization of novel 4-[(aminocarbonyl)amino]-N-[4-(2-aminoethyl)phenyl]benzenesulfonamide ghrelin receptor antagonists

Alexander O. Pasternak, Stephen D. Goble, Reynalda Keh deJesus, Donna L. Hreniuk et autres

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Design, synthesis, and structure–activity relationship of novel CCR2 antagonists

Shankaran Kothandaraman, Karla L. Donnely, Gabor Butora, Richard Jiao et autres

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Conformational studies of 3-amino-1-alkyl-cyclopentane carboxamide CCR2 antagonists leading to new spirocyclic antagonists

Alexander O. Pasternak, Stephen D. Goble, George A. Doss, Nancy N. Tsou et autres

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CCDC 670426: Experimental Crystal Structure Determination

Alex Pasternak, Stephen D. Goble, George A. Doss, Nancy N. Tsou et autres

An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, …