M
Mary T. Obermeier
Researcher at Bristol-Myers Squibb
Publications - 34
Citations - 1627
Mary T. Obermeier is an academic researcher from Bristol-Myers Squibb. The author has contributed to research in topics: Prostate cancer & Androgen Receptor Antagonists. The author has an hindex of 17, co-authored 34 publications receiving 1406 citations.
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Journal ArticleDOI
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,P.J. McCann,Manorama Patel,Ravindar N. Girotra,Gang Wu,Philip M. Sher,Eamonn P. Morrison,Scott A. Biller,Robert Zahler,Prashant P. Deshpande,Annie Pullockaran,Deborah Hagan,Nathan Morgan,Joseph R. Taylor,Mary T. Obermeier,William G. Humphreys,Ashish Khanna,Lorell Discenza,James G. Robertson,Aiying Wang,Songping Han,John R. Wetterau,Evan B. Janovitz,Oliver P. Flint,Jean M. Whaley,William N. Washburn +27 more
TL;DR: The C-aryl glucoside 6 (dapagliflozin) was identified as a potent and selective hSGLT2 inhibitor which reduced blood glucose levels in a dose-dependent manner by as much as 55% in hyperglycemic streptozotocin (STZ) rats.
Journal ArticleDOI
In vitro characterization and pharmacokinetics of dapagliflozin (BMS-512148), a potent sodium-glucose cotransporter type II inhibitor, in animals and humans.
Mary T. Obermeier,Ming Yao,Ashish Khanna,Barry Koplowitz,Mingshe Zhu,Wenying Li,Bernard J. Komoroski,Sreeneeranj Kasichayanula,Lorell Discenza,William N. Washburn,Wei Meng,Bruce A. Ellsworth,Jean M. Whaley,William G. Humphreys +13 more
TL;DR: Pharmacokinetic parameters for dapagliflozin in preclinical species revealed a compound with adequate oral exposure, clearance, and elimination half-life, consistent with the potential for single daily dosing in humans.
Journal ArticleDOI
Drug safety is a barrier to the discovery and development of new androgen receptor antagonists
William R. Foster,Bruce D. Car,Hong Shi,Paul Levesque,Mary T. Obermeier,Jinping Gan,Joseph C. Arezzo,Stephanie S. Powlin,Joseph E. Dinchuk,Aaron Balog,Mark E. Salvati,Ricardo M. Attar,Marco M. Gottardis +12 more
TL;DR: The failure to discover new AR antagonists has occurred in the face of continued research; to enable progress, a clear understanding of the reasons for failure is required.
Journal ArticleDOI
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,Douglas G. Batt,Myra Beaudoin Bertrand,Hua Gong,Jun Dai,Shiuhang Yip,Peng Li,Dawn Sun,Dauh-Rurng Wu,Chunlei Wang,Yingru Zhang,Sarah C. Traeger,Mark A. Pattoli,Stacey Skala,Lihong Cheng,Mary T. Obermeier,Rodney Vickery,Lorell Discenza,Celia D’Arienzo,Yifan Zhang,Elizabeth M. Heimrich,Kathleen M. Gillooly,Tracy L. Taylor,Claudine Pulicicchio,Kim W. McIntyre,Michael Galella,Andy J. Tebben,Jodi K. Muckelbauer,Chiehying Chang,Richard Rampulla,Arvind Mathur,Luisa Salter-Cid,Joel C. Barrish,Percy H. Carter,Aberra Fura,James R. Burke,Joseph A. Tino +40 more
TL;DR: The structure-activity relationships (SAR) leading to a novel series of highly potent and selective carbazole and tetrahydrocarbazole based, reversible inhibitors of BTK are detailed, resulting in enhanced potency and selectivity as well as a reduction in safety liabilities.
Journal ArticleDOI
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,Mark A. Pattoli,Stacey Skala,Lihong Cheng,Mary T. Obermeier,Robin Moore,Zheng Yang,Rodney Vickery,Paul A. Elzinga,Lorell Discenza,Celia D’Arienzo,Kathleen M. Gillooly,Tracy L. Taylor,Claudine Pulicicchio,Yifan Zhang,Elizabeth M. Heimrich,Kim W. McIntyre,Qian Ruan,Richard A. Westhouse,Ian M. Catlett,Naiyu Zheng,Charu Chaudhry,Jun Dai,Michael Galella,Andrew J. Tebben,Matt Pokross,Jianqing Li,Rulin Zhao,Daniel Smith,Richard Rampulla,Alban Allentoff,Michael Wallace,Arvind Mathur,Luisa Salter-Cid,John E. Macor,Percy H. Carter,Aberra Fura,James R. Burke,Joseph A. Tino +42 more
TL;DR: The evolution of the strategy to identify a covalent, irreversible inhibitor of BTK that has the intrinsic potency, selectivity, and pharmacokinetic properties necessary to provide a rapid rate of inactivation systemically following a very low dose is outlined.