Publications by authors named "Kenneth Santone"

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Discovery of pyrrolo[2,1-][1,2,4]triazine-based inhibitors of adaptor protein 2-associated kinase 1 for the treatment of pain.
Carolyn D Dzierba, Bireshwar Dasgupta, George Karageorge, Walter Kostich, Brian Hamman, Kenneth S Santone

Med Chem Res· June 2023

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The Discovery of GSK3640254, a Next-Generation Inhibitor of HIV-1 Maturation.
Alicia Regueiro-Ren, Sing-Yuen Sit, Yan Chen, Jie Chen, Jacob J Swidorski, Kenneth S Santone

J Med Chem· September 2022

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Discovery of ()-1-((2',6-Bis(difluoromethyl)-[2,4'-bipyridin]-5-yl)oxy)-2,4-dimethylpentan-2-amine (BMS-986176/LX-9211): A Highly Selective, CNS Penetrable, and Orally Active Adaptor Protein-2 Associated Kinase 1 Inhibitor in Clinical Trials for the Treatment of Neuropathic Pain.
Guanglin Luo, Ling Chen, Walter A Kostich, Brian Hamman, Jason Allen, Kenneth S Santone

J Med Chem· March 2022

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Discovery and Optimization of Biaryl Alkyl Ethers as a Novel Class of Highly Selective, CNS-Penetrable, and Orally Active Adaptor Protein-2-Associated Kinase 1 (AAK1) Inhibitors for the Potential Treatment of Neuropathic Pain.
Guanglin Luo, Ling Chen, Walter A Kostich, Brian Hamman, Jason Allen, Kenneth S Santone

J Med Chem· March 2022

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Structure-Property Basis for Solving Transporter-Mediated Efflux and Pan-Genotypic Inhibition in HCV NS5B Inhibitors.
Kap-Sun Yeung, Brett R Beno, Kathy Mosure, Juliang Zhu, Katherine A Grant-Young, Kenneth Santone

ACS Med Chem Lett· December 2018

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Design, Synthesis, and SAR of C-3 Benzoic Acid, C-17 Triterpenoid Derivatives. Identification of the HIV-1 Maturation Inhibitor 4-((1 R,3a S,5a R,5b R,7a R,11a S,11b R,13a R,13b R)-3a-((2-(1,1-Dioxidothiomorpholino)ethyl)amino)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)-2,3,3a,4,5,5a,5b,6,7,7a,8,11,11a,11b,12,13,13a,13b-octadecahydro-1 H-cyclopenta[ a]chrysen-9-yl)benzoic Acid (GSK3532795, BMS-955176).
Alicia Regueiro-Ren, Jacob J Swidorski, Zheng Liu, Yan Chen, Ny Sin, Kenneth S Santone

J Med Chem· August 2018

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Role of regional absorption and gastrointestinal motility on variability in oral absorption of a model drug.
Ajit S Narang, Anand Balakrishnan, John Morrison, Jinjiang Li, Jennifer Wang, Kenneth Santone

Eur J Pharm Biopharm· August 2017

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Discovery of a Hepatitis C Virus NS5B Replicase Palm Site Allosteric Inhibitor (BMS-929075) Advanced to Phase 1 Clinical Studies.
Kap-Sun Yeung, Brett R Beno, Kyle Parcella, John A Bender, Katherine A Grant-Young, Kenneth Santone

J Med Chem· May 2017

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Difluorocyclobutylacetylenes as positive allosteric modulators of mGluR5 with reduced bioactivation potential.
Andrew P Degnan, Darrell Maxwell, Anand Balakrishnan, Jeffrey M Brown, Amy Easton, Kenneth S Santone

Bioorg Med Chem Lett· December 2016

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Development of 1-Pyrazolo[3,4-]pyridines as Metabotropic Glutamate Receptor 5 Positive Allosteric Modulators.
Matthew D Hill, Haiquan Fang, Jeffrey M Brown, Thaddeus Molski, Amy Easton, Kenneth S Santone

ACS Med Chem Lett· December 2016

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Inhibition of AAK1 Kinase as a Novel Therapeutic Approach to Treat Neuropathic Pain.
Walter Kostich, Brian D Hamman, Yu-Wen Li, Sreenivasulu Naidu, Kumaran Dandapani, Kenneth S Santone

J Pharmacol Exp Ther· September 2016

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Oxazolidinone-based allosteric modulators of mGluR5: Defining molecular switches to create a pharmacological tool box.
Hong Huang, Andrew P Degnan, Anand Balakrishnan, Amy Easton, Michael Gulianello, Kenneth S Santone

Bioorg Med Chem Lett· September 2016

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Discovery of BMS-955176, a Second Generation HIV-1 Maturation Inhibitor with Broad Spectrum Antiviral Activity.
Alicia Regueiro-Ren, Zheng Liu, Yan Chen, Ny Sin, Sing-Yuen Sit, Kenneth S Santone

ACS Med Chem Lett· June 2016

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Discovery and Preclinical Evaluation of BMS-955829, a Potent Positive Allosteric Modulator of mGluR5.
Fukang Yang, Lawrence B Snyder, Anand Balakrishnan, Jeffrey M Brown, Digavalli V Sivarao, Kenneth S Santone

ACS Med Chem Lett· March 2016

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Preclinical Pharmacokinetics and In Vitro Metabolism of Asunaprevir (BMS-650032), a Potent Hepatitis C Virus NS3 Protease Inhibitor.
Kathleen W Mosure, Jay O Knipe, Marc Browning, Vinod Arora, Yue-Zhong Shu, Kenneth Santone

J Pharm Sci· September 2015

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Preclinical pharmacokinetics and in vitro metabolism of BMS-605339: a novel HCV NS3 protease inhibitor.
Susan Jenkins, Paul Scola, Fiona McPhee, Jay Knipe, Christoph Gesenberg, Kenneth Santone

J Pharm Sci· June 2014

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Preclinical characterization of BMS-791325, an allosteric inhibitor of hepatitis C Virus NS5B polymerase.
Julie A Lemm, Mengping Liu, Robert G Gentles, Min Ding, Stacey Voss, Kenneth S Santone

Antimicrob Agents Chemother· June 2014

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Discovery and preclinical characterization of the cyclopropylindolobenzazepine BMS-791325, a potent allosteric inhibitor of the hepatitis C virus NS5B polymerase.
Robert G Gentles, Min Ding, John A Bender, Carl P Bergstrom, Katharine Grant-Young, Kenneth S Santone

J Med Chem· March 2014

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Hepatitis C virus NS5A replication complex inhibitors: the discovery of daclatasvir.
Makonen Belema, Van N Nguyen, Carol Bachand, Dan H Deon, Jason T Goodrich, Kenneth S Santone

J Med Chem· March 2014

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Discovery and early clinical evaluation of BMS-605339, a potent and orally efficacious tripeptidic acylsulfonamide NS3 protease inhibitor for the treatment of hepatitis C virus infection.
Paul M Scola, Alan Xiangdong Wang, Andrew C Good, Li-Qiang Sun, Keith D Combrink, Kenneth S Santone

J Med Chem· March 2014

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Design and characterization of a novel fluorinated magnetic resonance imaging agent for functional analysis of bile Acid transporter activity.
Diana Vivian, Kunrong Cheng, Sandeep Khurana, Su Xu, Valerie Whiterock, Kenneth S Santone

Pharm Res· May 2013

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Inhibitors of HIV-1 attachment. Part 8: the effect of C7-heteroaryl substitution on the potency, and in vitro and in vivo profiles of indole-based inhibitors.
Kap-Sun Yeung, Zhilei Qiu, Zhiwei Yin, Ashok Trehan, Haiquan Fang, Kenneth Santone

Bioorg Med Chem Lett· January 2013

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Inhibitors of HIV-1 attachment. Part 7: indole-7-carboxamides as potent and orally bioavailable antiviral agents.
Kap-Sun Yeung, Zhilei Qiu, Quifen Xue, Haiquan Fang, Zheng Yang, Kenneth Santone

Bioorg Med Chem Lett· January 2013

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Discovery of (5S,6S,9R)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate (BMS-927711): an oral calcitonin gene-related peptide (CGRP) antagonist in clinical trials for treating migraine.
Guanglin Luo, Ling Chen, Charles M Conway, Rex Denton, Deborah Keavy, Kenneth S Santone

J Med Chem· December 2012

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An automated high throughput liquid chromatography-mass spectrometry process to assess the metabolic stability of drug candidates.
Dieter M Drexler, James V Belcastro, Kenneth E Dickinson, Kurt J Edinger, Serhiy Y Hnatyshyn, Kenneth S Santone

Assay Drug Dev Technol· April 2007

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