Publications by authors named "Mary Obermeier"

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The discovery of BMS-737 as a potent, CYP17 lyase-selective inhibitor for the treatment of castration-resistant prostate cancer.
Chetan Padmakar Darne, Upender Velaparthi, Mark Saulnier, David Frennesson, Peiying Liu, Mary T Obermeier

Bioorg Med Chem Lett· November 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, Mary T Obermeier

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, Mary T Obermeier

J Med Chem· March 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, Mary Obermeier

Bioorg Med Chem Lett· 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, Mary T Obermeier

ACS Med Chem Lett· December 2020

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Driving Potency with Rotationally Stable Atropisomers: Discovery of Pyridopyrimidinedione-Carbazole Inhibitors of BTK.
Anurag S Srivastava, Soo Ko, Scott H Watterson, Mark A Pattoli, Stacey Skala, Mary T Obermeier

ACS Med Chem Lett· November 2020

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Discovery of BMS-986251: A Clinically Viable, Potent, and Selective RORγt Inverse Agonist.
Robert J Cherney, Lyndon A M Cornelius, Anurag Srivastava, Carolyn A Weigelt, David Marcoux, Mary Obermeier

ACS Med Chem Lett· June 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, Mary T Obermeier

J Med Chem· November 2019

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Discovery of Branebrutinib (BMS-986195): A Strategy for Identifying a Highly Potent and Selective Covalent Inhibitor Providing Rapid in Vivo Inactivation of Bruton's Tyrosine Kinase (BTK).
Scott H Watterson, Qingjie Liu, Myra Beaudoin Bertrand, Douglas G Batt, Ling Li, Mary T Obermeier

J Med Chem· April 2019

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Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3-Kinase δ (PI3Kδ) Inhibitor for the Treatment of Immunological Disorders.
Qingjie Liu, Qing Shi, David Marcoux, Douglas G Batt, Lyndon Cornelius, Mary T Obermeier

J Med Chem· June 2017

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The role of chromatographic and chiroptical spectroscopic techniques and methodologies in support of drug discovery for atropisomeric drug inhibitors of Bruton's tyrosine kinase.
Jun Dai, Chunlei Wang, Sarah C Traeger, Lorell Discenza, Mary T Obermeier

J Chromatogr A· March 2017

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[2.2.1]-Bicyclic sultams as potent androgen receptor antagonists.
Weifang Shan, Aaron Balog, Andrew Nation, Xiao Zhu, Jing Chen, Mary Obermeier

Bioorg Med Chem Lett· December 2016

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Discovery of 6-Fluoro-5-(R)-(3-(S)-(8-fluoro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)-2-methylphenyl)-2-(S)-(2-hydroxypropan-2-yl)-2,3,4,9-tetrahydro-1H-carbazole-8-carboxamide (BMS-986142): A Reversible Inhibitor of Bruton's Tyrosine Kinase (BTK) Conformationally Constrained by Two Locked Atropisomers.
Scott H Watterson, George V De Lucca, Qing Shi, Charles M Langevine, Qingjie Liu, Mary T Obermeier

J Med Chem· October 2016

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Small Molecule Reversible Inhibitors of Bruton's Tyrosine Kinase (BTK): Structure-Activity Relationships Leading to the Identification of 7-(2-Hydroxypropan-2-yl)-4-[2-methyl-3-(4-oxo-3,4-dihydroquinazolin-3-yl)phenyl]-9H-carbazole-1-carboxamide (BMS-935177).
George V De Lucca, Qing Shi, Qingjie Liu, Douglas G Batt, Myra Beaudoin Bertrand, Mary Obermeier

J Med Chem· September 2016

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Discovery of the Selective CYP17A1 Lyase Inhibitor BMS-351 for the Treatment of Prostate Cancer.
Audris Huang, Lata Jayaraman, Aberra Fura, Gregory D Vite, George L Trainor, Mary T Obermeier

ACS Med Chem Lett· January 2016

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A bioanalytical strategy utilizing dried blood spot sampling and LC-MS/MS in discovery toxicology studies.
Lorell Discenza, Mary T Obermeier, Richard Westhouse, Timothy V Olah, Celia J D'Arienzo

Bioanalysis· May 2012

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Drug safety is a barrier to the discovery and development of new androgen receptor antagonists.
William R Foster, Bruce D Car, Hong Shi, Paul C Levesque, Mary T Obermeier

Prostate· April 2011

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Phase I dose-escalation study of the novel antiandrogen BMS-641988 in patients with castration-resistant prostate cancer.
Dana Rathkopf, Glenn Liu, Michael A Carducci, Mario A Eisenberger, Aseem Anand, Mary T Obermeier

Clin Cancer Res· February 2011

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Plasma stability-dependent circulation of acyl glucuronide metabolites in humans: how circulating metabolite profiles of muraglitazar and peliglitazar can lead to misleading risk assessment.
Donglu Zhang, Nirmala Raghavan, Lifei Wang, Yongjun Xue, Mary Obermeier

Drug Metab Dispos· January 2011

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Design and synthesis of 4-[3,5-dioxo-11-oxa-4,9-diazatricyclo[5.3.1.0(2,6)]undec-4-yl]-2-trifluoromethyl-benzonitriles as androgen receptor antagonists.
Hai-Yun Xiao, Aaron Balog, Ricardo M Attar, David Fairfax, Linda B Fleming, Mary Obermeier

Bioorg Med Chem Lett· August 2010

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Discovery of BMS-641988, a novel and potent inhibitor of androgen receptor signaling for the treatment of prostate cancer.
Ricardo M Attar, Maria Jure-Kunkel, Aaron Balog, Mary Ellen Cvijic, Janet Dell-John, Mary Obermeier

Cancer Res· August 2009

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Aglycone exploration of C-arylglucoside inhibitors of renal sodium-dependent glucose transporter SGLT2.
Bruce A Ellsworth, Wei Meng, Manorama Patel, Ravindar N Girotra, Gang Wu, Mary T Obermeier

Bioorg Med Chem Lett· September 2008

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Discovery of dapagliflozin: a potent, selective renal sodium-dependent glucose cotransporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes.
Wei Meng, Bruce A Ellsworth, Alexandra A Nirschl, Peggy J McCann, Manorama Patel, Mary T Obermeier

J Med Chem· March 2008

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Identification and optimization of a novel series of [2.2.1]-oxabicyclo imide-based androgen receptor antagonists.
Mark E Salvati, Aaron Balog, Weifang Shan, Richard Rampulla, Soren Giese, Mary Obermeier

Bioorg Med Chem Lett· March 2008

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Identification of 2-amino-5-(thioaryl)thiazoles as inhibitors of nerve growth factor receptor TrkA.
Soong-Hoon Kim, John S Tokarski, Kenneth J Leavitt, Brian E Fink, Mark E Salvati, Mary T Obermeier

Bioorg Med Chem Lett· January 2008

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