M. Obermeier

发表

Drug safety is a barrier to the discovery and development of new androgen receptor antagonists

J. Arezzo, M. Salvati, A. Balog, 2011, The Prostate.

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.

J. Chen, L. Schweizer, M. Salvati, 2010, Bioorganic & medicinal chemistry letters.

Identification and optimization of a novel series of [2.2.1]-oxabicyclo imide-based androgen receptor antagonists.

Michael A. Galella, A. Fura, S. Krystek, 2008, Bioorganic & medicinal chemistry letters.

In Vitro Characterization and Pharmacokinetics of Dapagliflozin (BMS-512148), a Potent Sodium-Glucose Cotransporter Type II Inhibitor, in Animals and Humans

W. Humphreys, B. Koplowitz, A. Khanna, 2010, Drug Metabolism and Disposition.

The role of chromatographic and chiroptical spectroscopic techniques and methodologies in support of drug discovery for atropisomeric drug inhibitors of Bruton's tyrosine kinase.

A. Tymiak, Yingru Zhang, M. Obermeier, 2017, Journal of chromatography. A.

Plasma Stability-Dependent Circulation of Acyl Glucuronide Metabolites in Humans: How Circulating Metabolite Profiles of Muraglitazar and Peliglitazar Can Lead to Misleading Risk Assessment

W. Humphreys, Donglu Zhang, R. Ramanathan, 2011, Drug Metabolism and Disposition.

Aglycone exploration of C-arylglucoside inhibitors of renal sodium-dependent glucose transporter SGLT2.

W. Humphreys, T. Waldron, Songping Han, 2008, Bioorganic & medicinal chemistry letters.

Application of structure–metabolism relationships in the identification of a selective endothelin A antagonist, BMS-193884, with favourable pharmacokinetic properties

S. Chong, J. Barrish, W. Humphreys, 2003, Xenobiotica; the fate of foreign compounds in biological systems.

Tricyclic Sulfones as Potent, Selective and Efficacious RORγt Inverse Agonists - Exploring C6 and C8 SAR Using Late-Stage Functionalization.

Michael G. Yang, D. Shuster, C. Weigelt, 2020, Bioorganic & medicinal chemistry letters.

Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3-Kinase δ (PI3Kδ) Inhibitor for the Treatment of Immunological Disorders.

K. McIntyre, Sidney Pitt, G. Schieven, 2017, Journal of medicinal chemistry.

The Discovery of BMS-737 as a Potent, CYP17 Lyase-Selective Inhibitor for the Treatment of Castration-Resistant Prostate Cancer.

J. Tokarski, A. Fura, L. Jayaraman, 2022, Bioorganic & medicinal chemistry letters.

Discovery of the Selective CYP17A1 Lyase Inhibitor BMS-351 for the Treatment of Prostate Cancer.

A. Doweyko, G. Trainor, A. Fura, 2016, ACS medicinal chemistry letters.

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).

K. McIntyre, J. Barrish, A. Mathur, 2016, Journal of medicinal chemistry.

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).

Ping Chen, Henry H. Gu, E. Iwanowicz, 2007, Journal of medicinal chemistry.

Driving Potency with Rotationally Stable Atropisomers: Discovery of Pyridopyrimidinedione-Carbazole Inhibitors of BTK.

Michael A. Galella, K. McIntyre, J. Barrish, 2020, ACS medicinal chemistry letters.

Discovery of BMS-641988, a novel and potent inhibitor of androgen receptor signaling for the treatment of prostate cancer.

L. Schweizer, M. Salvati, Weifang Shan, 2009, Cancer research.

Discovery of dapagliflozin: a potent, selective renal sodium-dependent glucose cotransporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes.

W. Humphreys, O. Flint, E. Janovitz, 2008, Journal of medicinal chemistry.

Benzazepinone calcium channel blockers. 5. Effects on antihypertensive activity associated with N1 and aromatic substituents.

J. Das, S. Moreland, D. Floyd, 1992, Journal of medicinal chemistry.

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

Michael A. Galella, K. McIntyre, J. Barrish, 2016, Journal of medicinal chemistry.

Oxidative activation of acylguanidine prodrugs: intestinal presystemic activation in rats limits absorption and can be inhibited by co-administration of ketoconazole

J. Das, R. Moquin, S. Chong, 2003, Xenobiotica; the fate of foreign compounds in biological systems.

2-hydroxy-N-arylbenzenesulfonamides as ATP-citrate lyase inhibitors.

Dong Cheng, Ramesh Padmanabha, Kristen Pike, 2007, Bioorganic & medicinal chemistry letters.

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).

Michael A. Galella, K. McIntyre, J. Macor, 2019, Journal of medicinal chemistry.

Azatricyclic Inverse Agonists of RORγt That Demonstrate Efficacy in Models of Rheumatoid Arthritis and Psoriasis.

Michael G. Yang, D. Shuster, C. Weigelt, 2021, ACS medicinal chemistry letters.

Phase I Dose-Escalation Study of the Novel Antiandrogen BMS-641988 in Patients with Castration-Resistant Prostate Cancer

M. Morris, H. Scher, G. Wilding, 2010, Clinical Cancer Research.

Discovery of BMS-986251: A Clinically Viable, Potent, and Selective RORγt Inverse Agonist.

D. Shuster, J. Macor, C. Weigelt, 2020, ACS medicinal chemistry letters.

Continuous Blood Withdrawal as a Rapid Screening Method for Determining Clearance and Oral Bioavailability in Rats

W. Humphreys, R. Morrison, M. Obermeier, 1998, Pharmaceutical Research.

[2.2.1]-Bicyclic sultams as potent androgen receptor antagonists.

Michael A. Galella, G. Trainor, Weifang Shan, 2016, Bioorganic & medicinal chemistry letters.

A bioanalytical strategy utilizing dried blood spot sampling and LC-MS/MS in discovery toxicology studies.

T. Olah, C. D’arienzo, M. Obermeier, 2012, Bioanalysis.

Prodrugs of BMS-183920: metabolism and permeability considerations.

S. Chong, A. Marino, R. Morrison, 1996, Journal of pharmaceutical sciences.

Identification of 2-amino-5-(thioaryl)thiazoles as inhibitors of nerve growth factor receptor TrkA.

Ping Chen, R. Moquin, J. Tokarski, 2008, Bioorganic & medicinal chemistry letters.

Rationally Designed, Conformationally Constrained Inverse Agonists of RORγt ‒ Identification of a Potent, Selective Series with Biologic-Like In Vivo Efficacy.

K. McIntyre, D. Shuster, J. Macor, 2019, Journal of medicinal chemistry.

Novel Tricyclic Pyroglutamide Derivatives as Potent RORγt Inverse Agonists Identified using a Virtual Screening Approach.

D. Shuster, J. Macor, C. Weigelt, 2020, ACS medicinal chemistry letters.

Effects of bioflavonoids on hepatic P450 activities.

C. S. Yang, M. Obermeier, R. White, 1995, Xenobiotica; the fate of foreign compounds in biological systems.

Tricyclic-Carbocyclic RORγt Inverse Agonists-Discovery of BMS-986313.

Michael G. Yang, D. Shuster, C. Weigelt, 2021, Journal of medicinal chemistry.

Discovery of BMS-641988, a novel and potent inhibitor of androgen receptor signaling for the treatment of prostate cancer.

L. Schweizer, M. Salvati, Weifang Shan, 2009, Cancer research.

Plasma Stability-Dependent Circulation of Acyl Glucuronide Metabolites in Humans: How Circulating Metabolite Profiles of Muraglitazar and Peliglitazar Can Lead to Misleading Risk Assessment

W. Humphreys, Donglu Zhang, R. Ramanathan, 2011, Drug Metabolism and Disposition.