Publications by authors named "David J Shuster"

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Repression of Organic Anion Transporting Polypeptide (OATP) 1B Expression and Increase of Plasma Coproporphyrin Level as Evidence for OATP1B Downregulation in Cynomolgus Monkeys Treated with Chenodeoxycholic Acid.
Yueping Zhang, Shen-Jue Chen, Cliff Chen, Xue-Qing Chen, Sagnik Chatterjee, David J Shuster

Drug Metab Dispos· August 2022

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Azatricyclic Inverse Agonists of RORγt That Demonstrate Efficacy in Models of Rheumatoid Arthritis and Psoriasis.
Qingjie Liu, Hai-Yun Xiao, Douglas G Batt, Zili Xiao, Yeheng Zhu, David J Shuster

ACS Med Chem Lett· May 2021

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Tricyclic-Carbocyclic RORγt Inverse Agonists-Discovery of BMS-986313.
Michael G Yang, Myra Beaudoin-Bertrand, Zili Xiao, David Marcoux, Carolyn A Weigelt, David J Shuster

J Med Chem· March 2021

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Quantification of surrogate monoclonal antibodies in mouse serum using LC-MS/MS.
John T Mehl, France Landry, Lorell Discenza, Bogdan Sleczka, Qihong Zhao, David J Shuster

Bioanalysis· February 2021

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Tricyclic sulfones as potent, selective and efficacious RORγt inverse agonists - Exploring C6 and C8 SAR using late-stage functionalization.
Qing Shi, Zili Xiao, Michael G Yang, David Marcoux, Robert J Cherney, David J Shuster

Bioorg Med Chem Lett· December 2020

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Biologic-like In Vivo Efficacy with Small Molecule Inhibitors of TNFα Identified Using Scaffold Hopping and Structure-Based Drug Design Approaches.
Hai-Yun Xiao, Ning Li, James J-W Duan, Bin Jiang, Zhonghui Lu, David J Shuster

J Med Chem· December 2020

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Novel Tricyclic Pyroglutamide Derivatives as Potent RORγt Inverse Agonists Identified using a Virtual Screening Approach.
Qingjie Liu, Douglas G Batt, Carolyn A Weigelt, Shiuhang Yip, Dauh-Rurng Wu, David J Shuster

ACS Med Chem Lett· December 2020

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Absence of OATP1B (Organic Anion-Transporting Polypeptide) Induction by Rifampin in Cynomolgus Monkeys: Determination Using the Endogenous OATP1B Marker Coproporphyrin and Tissue Gene Expression.
Yueping Zhang, Cliff Chen, Shen-Jue Chen, Xue-Qing Chen, David J Shuster

J Pharmacol Exp Ther· October 2020

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Rationally Designed, Conformationally Constrained Inverse Agonists of RORγt-Identification of a Potent, Selective Series with Biologic-Like in Vivo Efficacy.
David Marcoux, James J-W Duan, Qing Shi, Robert J Cherney, Anurag S Srivastava, David J Shuster

J Med Chem· November 2019

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Structure-based Discovery of Phenyl (3-Phenylpyrrolidin-3-yl)sulfones as Selective, Orally Active RORγt Inverse Agonists.
James J-W Duan, Zhonghui Lu, Bin Jiang, Sylwia Stachura, Carolyn A Weigelt, David J Shuster

ACS Med Chem Lett· March 2019

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Identification of Tricyclic Agonists of Sphingosine-1-phosphate Receptor 1 (S1P) Employing Ligand-Based Drug Design.
Hai-Yun Xiao, Scott H Watterson, Charles M Langevine, Anurag S Srivastava, Soo S Ko, David J Shuster

J Med Chem· November 2016

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Identification and synthesis of potent and selective pyridyl-isoxazole based agonists of sphingosine-1-phosphate 1 (S1P1).
Junqing Guo, Scott H Watterson, Steven H Spergel, James Kempson, Charles M Langevine, David J Shuster

Bioorg Med Chem Lett· May 2016

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Potent and Selective Agonists of Sphingosine 1-Phosphate 1 (S1P1): Discovery and SAR of a Novel Isoxazole Based Series.
Scott H Watterson, Junqing Guo, Steve H Spergel, Charles M Langevine, Robert V Moquin, David J Shuster

J Med Chem· March 2016

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Discovery of ((4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methylpyrrolo[1,2-f][1,2,4]triazine-6-carbonyl)(propyl)carbamoyloxy)methyl-2-(4-(phosphonooxy)phenyl)acetate (BMS-751324), a Clinical Prodrug of p38α MAP Kinase Inhibitor.
Chunjian Liu, James Lin, John Hynes, Hong Wu, Stephen T Wrobleski, David J Shuster

J Med Chem· October 2015

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Dual Inhibition of Interleukin-23 and Interleukin-17 Offers Superior Efficacy in Mouse Models of Autoimmunity.
Paul R Mangan, Linhui Julie Su, Victoria Jenny, Andrea L Tatum, Caryn Picarillo, David J Shuster

J Pharmacol Exp Ther· August 2015

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Quantification of human mAbs in mouse tissues using generic affinity enrichment procedures and LC-MS detection.
Bogdan G Sleczka, John T Mehl, David J Shuster, Katherine E Lewis, Robin Moore

Bioanalysis· July 2015

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Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38α MAP kinase inhibitors.
Alaric J Dyckman, Tianle Li, Sidney Pitt, Rosemary Zhang, Ding Ren Shen, David J Shuster

Bioorg Med Chem Lett· August 2011

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Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases.
Chunjian Liu, James Lin, Stephen T Wrobleski, Shuqun Lin, John Hynes, David J Shuster

J Med Chem· September 2010

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An LFA-1 (alphaLbeta2) small-molecule antagonist reduces inflammation and joint destruction in murine models of arthritis.
Suzanne J Suchard, Dawn K Stetsko, Patricia M Davis, Stacey Skala, Dominique Potin, David J Shuster

J Immunol· April 2010

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Synthesis and SAR of new pyrrolo[2,1-f][1,2,4]triazines as potent p38 alpha MAP kinase inhibitors.
Stephen T Wrobleski, Shuqun Lin, John Hynes, Hong Wu, Sidney Pitt, David J Shuster

Bioorg Med Chem Lett· April 2008

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The discovery of (R)-2-(sec-butylamino)-N-(2-methyl-5-(methylcarbamoyl)phenyl) thiazole-5-carboxamide (BMS-640994)-A potent and efficacious p38alpha MAP kinase inhibitor.
John Hynes, Hong Wu, Sidney Pitt, Ding Ren Shen, Rosemary Zhang, David J Shuster

Bioorg Med Chem Lett· March 2008

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Design, synthesis, and anti-inflammatory properties of orally active 4-(phenylamino)-pyrrolo[2,1-f][1,2,4]triazine p38alpha mitogen-activated protein kinase inhibitors.
John Hynes, Alaric J Dyckman, Shuqun Lin, Stephen T Wrobleski, Hong Wu, David J Shuster

J Med Chem· January 2008

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Acridone-based inhibitors of inosine 5'-monophosphate dehydrogenase: discovery and SAR leading to the identification of N-(2-(6-(4-ethylpiperazin-1-yl)pyridin-3-yl)propan-2-yl)-2- fluoro-9-oxo-9,10-dihydroacridine-3-carboxamide (BMS-566419).
Scott H Watterson, Ping Chen, Yufen Zhao, Henry H Gu, T G Murali Dhar, David J Shuster

J Med Chem· July 2007

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2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatinib, BMS-354825) as a potent pan-Src kinase inhibitor.
Jagabandhu Das, Ping Chen, Derek Norris, Ramesh Padmanabha, James Lin, David J Shuster

J Med Chem· November 2006

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Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors.
Jagabandhu Das, Joseph A Furch, Chunjian Liu, Robert V Moquin, James Lin, David J Shuster

Bioorg Med Chem Lett· July 2006

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