Publications by authors named "Keith Demarest"

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Discovery of PEGylated 6-Benzhydryl-4-amino-quinazolines as Peripherally Restricted CBR Inverse Agonists.
Yue-Mei Zhang, Michael Greco, Tonya Le Blanc, Wensheng Lang, Jack Kauffman, Keith Demarest

ACS Med Chem Lett· December 2020

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5,5-Difluoro- and 5-Fluoro-5-methyl-hexose-based C-Glucosides as potent and orally bioavailable SGLT1 and SGLT2 dual inhibitors.
Guozhang Xu, Fuyong Du, Gee-Hong Kuo, June Zhi Xu, Yin Liang, Keith Demarest

Bioorg Med Chem Lett· September 2020

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Discovery of potent and orally bioavailable indazole-based glucagon receptor antagonists for the treatment of type 2 diabetes.
Guozhang Xu, Michael D Gaul, Fengbin Song, Fuyong Du, Yin Liang, Keith Demarest

Bioorg Med Chem Lett· October 2019

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Design, synthesis and structure activity relationships of indazole and indole derivatives as potent glucagon receptor antagonists.
Fengbin Song, Guozhang Xu, Michael D Gaul, Baoping Zhao, Tianbao Lu, Keith Demarest

Bioorg Med Chem Lett· August 2019

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Design, synthesis and biological evaluation of (2S,3R,4R,5S,6R)-5-fluoro-6-(hydroxymethyl)-2-aryltetrahydro-2H-pyran-3,4-diols as potent and orally active SGLT dual inhibitors.
Guozhang Xu, Michael D Gaul, Gee-Hong Kuo, Fuyong Du, June Zhi Xu, Keith Demarest

Bioorg Med Chem Lett· November 2018

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6-Benzhydryl-4-amino-quinolin-2-ones as Potent Cannabinoid Type 1 (CB) Receptor Inverse Agonists and Chemical Modifications for Peripheral Selectivity.
Yue-Mei Zhang, Michael N Greco, Mark J Macielag, Christopher A Teleha, Renee L DesJarlais, Keith Demarest

J Med Chem· November 2018

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Potent Sodium/Glucose Cotransporter SGLT1/2 Dual Inhibition Improves Glycemic Control Without Marked Gastrointestinal Adaptation or Colonic Microbiota Changes in Rodents.
Fuyong Du, Simon A Hinke, Cassandre Cavanaugh, David Polidori, Nathanial Wallace, Keith Demarest

J Pharmacol Exp Ther· June 2018

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Synthesis and biological evaluation of benzocyclobutane-C-glycosides as potent and orally active SGLT1/SGLT2 dual inhibitors.
Gee-Hong Kuo, Micheal D Gaul, Yin Liang, June Z Xu, Fuyong Du, Keith Demarest

Bioorg Med Chem Lett· April 2018

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Discovery of Orally Efficacious Tetrahydrobenzimidazoles as TGR5 Agonists for Type 2 Diabetes.
Xuqing Zhang, Mark Wall, Zhihua Sui, Jack Kauffman, Cuifen Hou, Keith Demarest

ACS Med Chem Lett· May 2017

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Evaluation of anti-diabetic effect and gall bladder function with 2-thio-5-thiomethyl substituted imidazoles as TGR5 receptor agonists.
Xuqing Zhang, Zhihua Sui, Jack Kauffman, Cuifen Hou, Cailin Chen, Keith Demarest

Bioorg Med Chem Lett· April 2017

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Pharmacodynamic effects of canagliflozin, a sodium glucose co-transporter 2 inhibitor, from a randomized study in patients with type 2 diabetes.
Sue Sha, Damayanthi Devineni, Atalanta Ghosh, David Polidori, Marcus Hompesch, Keith Demarest

PLoS One· December 2015

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Canagliflozin: a sodium glucose co-transporter 2 inhibitor for the treatment of type 2 diabetes mellitus.
Norm Rosenthal, Gary Meininger, Kirk Ways, David Polidori, Mehul Desai, Keith Demarest

Ann N Y Acad Sci· November 2015

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Pharmacodynamic effects of canagliflozin, a sodium glucose co-transporter 2 inhibitor, from a randomized study in patients with type 2 diabetes.
Sue Sha, Damayanthi Devineni, Atalanta Ghosh, David Polidori, Marcus Hompesch, Keith Demarest

PLoS One· October 2015

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4-Bicyclic heteroaryl-piperidine derivatives as potent, orally bioavailable stearoyl-CoA desaturase-1 (SCD1) inhibitors: part 2. Pyridazine-based analogs.
Shyh-Ming Yang, Yuting Tang, Thomas Rano, Huajun Lu, Gee-Hong Kuo, Keith T Demarest

Bioorg Med Chem Lett· March 2014

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4-Bicyclic heteroaryl-piperidine derivatives as potent, orally bioavailable Stearoyl-CoA desaturase-1 (SCD1) inhibitors. Part 1: urea-based analogs.
Shyh-Ming Yang, Yuting Tang, Rui Zhang, Huajun Lu, Gee-Hong Kuo, Keith T Demarest

Bioorg Med Chem Lett· December 2013

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Beneficial metabolic effects of CB1R anti-sense oligonucleotide treatment in diet-induced obese AKR/J mice.
Yuting Tang, George Ho, Yaxin Li, Meghan A Hall, Robert L Hills, Keith T Demarest

PLoS One· February 2013

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Phase 0 study of the inhibition of cholesteryl ester transfer protein activity by JNJ-28545595 in plasma from normolipidemic and dyslipidemic humans.
Troy C Sarich, Margery A Connelly, Dorota B Schranz, Atalanta Ghosh, Prasarn Manitpisitkul, Keith T Demarest

Int J Clin Pharmacol Ther· August 2012

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Effect of canagliflozin on renal threshold for glucose, glycemia, and body weight in normal and diabetic animal models.
Yin Liang, Kenji Arakawa, Kiichiro Ueta, Yasuaki Matsushita, Chiaki Kuriyama, Keith Demarest

PLoS One· June 2012

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The use of stable isotope-labeled glycerol and oleic acid to differentiate the hepatic functions of DGAT1 and -2.
Jenson Qi, Wensheng Lang, John G Geisler, Ping Wang, Ioanna Petrounia, Keith T Demarest

J Lipid Res· June 2012

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Discovery of a second generation agonist of the orphan G-protein coupled receptor GPR119 with an improved profile.
Graeme Semple, Juerg Lehmann, Amy Wong, Albert Ren, Marc Bruce, Keith Demarest

Bioorg Med Chem Lett· February 2012

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Discovery of fused bicyclic agonists of the orphan G-protein coupled receptor GPR119 with in vivo activity in rodent models of glucose control.
Graeme Semple, Albert Ren, Beatriz Fioravanti, Guillherme Pereira, Imelda Calderon, Keith T Demarest

Bioorg Med Chem Lett· May 2011

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In vivo characterization of a dual adenosine A2A/A1 receptor antagonist in animal models of Parkinson's disease.
Brian C Shook, Stefanie Rassnick, Melville C Osborne, Scott Davis, Lori Westover, Keith Demarest

J Med Chem· November 2010

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Torcetrapib produces endothelial dysfunction independent of cholesteryl ester transfer protein inhibition.
Margery A Connelly, Tom J Parry, Edward C Giardino, Zhihong Huang, Wai-Man Cheung, Keith T Demarest

J Cardiovasc Pharmacol· May 2010

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Methylene amine substituted arylindenopyrimidines as potent adenosine A(2A)/A(1) antagonists.
Brian C Shook, Stefanie Rassnick, Daniel Hall, Kenneth C Rupert, Geoffrey R Heintzelman, Keith Demarest

Bioorg Med Chem Lett· May 2010

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Synthesis and discovery of 2,3-dihydro-3,8-diphenylbenzo[1,4]oxazines as a novel class of potent cholesteryl ester transfer protein inhibitors.
Aihua Wang, Catherine P Prouty, Patricia D Pelton, Maria Yong, Keith T Demarest

Bioorg Med Chem Lett· February 2010

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