K. Cox

发表

Discovery of orally efficacious melanin-concentrating hormone receptor-1 antagonists as antiobesity agents. Synthesis, SAR, and biological evaluation of bicyclo[3.1.0]hexyl ureas.

W. Greenlee, Mark D. McBriar, H. Guzik, 2006, Journal of medicinal chemistry.

Structure based design of iminohydantoin BACE1 inhibitors: identification of an orally available, centrally active BACE1 inhibitor.

Lynn A. Hyde, W. Greenlee, A. Stamford, 2012, Bioorganic & medicinal chemistry letters.

Synthesis, SAR, and biological evaluation of oximino-piperidino-piperidine amides. 1. Orally bioavailable CCR5 receptor antagonists with potent anti-HIV activity.

W. Greenlee, S. Shapiro, A. Palani, 2002, Journal of medicinal chemistry.

Piperazine-based CCR5 antagonists as HIV-1 inhibitors. III: synthesis, antiviral and pharmacokinetic profiles of symmetrical heteroaryl carboxamides.

B. Neustadt, M. Endres, A. Palani, 2003, Bioorganic & medicinal chemistry letters.

Rapid determination of pharmacokinetic properties of new chemical entities: in vivo approaches.

Walter A. Korfmacher, K. Cox, Ronald E. White, 2002, Combinatorial chemistry & high throughput screening.

Role of transporters in the disposition of a novel β-lactamase inhibitor: relebactam (MK-7655).

X. Chu, K. Cox, Meihong Lin, 2019, The Journal of antimicrobial chemotherapy.

Demonstration of the capabilities of a parallel high performance liquid chromatography tandem mass spectrometry system for use in the analysis of drug discovery plasma samples.

Walter A. Korfmacher, K. Cox, X. Zhang, 1999, Rapid communications in mass spectrometry : RCM.

Isolation of circulating metabolites in drug discovery using high-performance liquid chromatography, and their identification by liquid chromatography coupled with tandem mass spectrometry and nuclear magnetic resonance spectroscopy

K. Cox, A. Nomeir, M. Bryant, 2002 .

Structure-activity relationships of 2,4-diphenyl-1H-imidazole analogs as CB2 receptor agonists for the treatment of chronic pain.

W. Greenlee, D. Tulshian, K. Cox, 2011, Bioorganic & medicinal chemistry letters.

Polyethlyene Glycol 200 can Protect Rats against Drug-Induced Kidney Toxicity through Inhibition of the Renal Organic Anion Transporter 3.

X. Chu, K. Cox, Yi-Zhong Gu, 2019, Toxicological sciences : an official journal of the Society of Toxicology.

The discovery of N-((2H-tetrazol-5-yl)methyl)-4-((R)-1-((5r,8R)-8-(tert-butyl)-3-(3,5-dichlorophenyl)-2-oxo-1,4-diazaspiro[4.5]dec-3-en-1-yl)-4,4-dimethylpentyl)benzamide (SCH 900822): a potent and selective glucagon receptor antagonist.

Ping Chen, W. Greenlee, A. Stamford, 2014, Journal of medicinal chemistry.

Oximino-piperidino-piperidine-based CCR5 antagonists. Part 2: synthesis, SAR and biological evaluation of symmetrical heteroaryl carboxamides.

W. Greenlee, S. Shapiro, A. Palani, 2003, Bioorganic & medicinal chemistry letters.

Bicyclic[4.1.0]heptanes as phenyl replacements for melanin concentrating hormone receptor antagonists.

Ruo Xu, William J Greenlee, Daniel J Weston, 2006, Bioorganic & medicinal chemistry.

Piperazine-based CCR5 antagonists as HIV-1 inhibitors. II. Discovery of 1-[(2,4-dimethyl-3-pyridinyl)carbonyl]-4- methyl-4-[3(S)-methyl-4-[1(S)-[4-(trifluoromethyl)phenyl]ethyl]-1-piperazinyl]- piperidine N1-oxide (Sch-350634), an orally bioavailable, potent CCR5 antagonist.

B. Neustadt, K. Cox, M. Murray, 2001, Journal of medicinal chemistry.

Discovery and Characterization of Vicriviroc (SCH 417690), a CCR5 Antagonist with Potent Activity against Human Immunodeficiency Virus Type 1

M. Hirsch, C. Tremblay, G. Reyes, 2005, Antimicrobial Agents and Chemotherapy.

Discovery of 4-[(Z)-(4-bromophenyl)- (ethoxyimino)methyl]-1'-[(2,4-dimethyl-3- pyridinyl)carbonyl]-4'-methyl-1,4'- bipiperidine N-oxide (SCH 351125): an orally bioavailable human CCR5 antagonist for the treatment of HIV infection.

W. Greenlee, M. Endres, S. Shapiro, 2001, Journal of medicinal chemistry.

Novel in vivo procedure for rapid pharmacokinetic screening of discovery compounds in rats

Walter A. Korfmacher, W. H. Barr, K. Cox, 1999 .

Development of an automated mass spectrometry system for the quantitative analysis of liver microsomal incubation samples: a tool for rapid screening of new compounds for metabolic stability.

Walter A. Korfmacher, K. Cox, E. Duchoslav, 1999, Rapid communications in mass spectrometry : RCM.

Cassette-accelerated rapid rat screen: a systematic procedure for the dosing and liquid chromatography/atmospheric pressure ionization tandem mass spectrometric analysis of new chemical entities as part of new drug discovery.

Walter A. Korfmacher, K. Ng, K. Cox, 2001, Rapid communications in mass spectrometry : RCM.

Discovery of the 3-Imino-1,2,4-thiadiazinane 1,1-Dioxide Derivative Verubecestat (MK-8931)-A β-Site Amyloid Precursor Protein Cleaving Enzyme 1 Inhibitor for the Treatment of Alzheimer's Disease.

Qin Jiang, William J Greenlee, Xia Chen, 2016, Journal of medicinal chemistry.

Enhancement of pharmacokinetic properties and in vivo efficacy of benzylidene ketal M(2) muscarinic receptor antagonists via benzamide modification.

J. Lachowicz, K. Cox, V. Coffin, 2002, Bioorganic & Medicinal Chemistry Letters.

Chapter 7 The utility of in vitro screening for the assessment of electrophilic metabolite formation early in drug discovery using hplc-ms/ms

K. Cox, D. Grotz, N. A. Clarke, 2005 .

Metabolic stabilization of benzylidene ketal M(2) muscarinic receptor antagonists via halonaphthoic acid substitution.

W. Greenlee, J. Lachowicz, J. Clader, 2001, Bioorganic & medicinal chemistry letters.

Muscarinic agonists and antagonists in the treatment of Alzheimer's disease.

C. Strader, J. Lachowicz, J. Clader, 2001, Farmaco.

HPLC-API/MS/MS : a powerful tool for integrating drug metabolism into the drug discovery process

Walter A. Korfmacher, K. Ng, K. Cox, 1997 .

The BACE1 inhibitor verubecestat (MK-8931) reduces CNS β-amyloid in animal models and in Alzheimer’s disease patients

Michael Tanen, Matthew E. Kennedy, Wei Li, 2016, Science Translational Medicine.

Systematic LC/MS metabolite identification in drug discovery.

Walter A. Korfmacher, K. Cox, D. Rindgen, 2001, Analytical chemistry.

Piperazine-based CCR5 antagonists as HIV-1 inhibitors. IV. Discovery of 1-[(4,6-dimethyl-5-pyrimidinyl)carbonyl]- 4-[4-[2-methoxy-1(R)-4-(trifluoromethyl)phenyl]ethyl-3(S)-methyl-1-piperazinyl]- 4-methylpiperidine (Sch-417690/Sch-D), a potent, highly selective, and orally bioavailable CCR5 antagonis

J. Lachowicz, K. Cox, G. Varty, 2004, Journal of medicinal chemistry.

Biological evaluation and interconversion studies of rotamers of SCH 351125, an orally bioavailable CCR5 antagonist.

William J Greenlee, Anandan Palani, W. Greenlee, 2003, Bioorganic & medicinal chemistry letters.

MK-8353: Discovery of an Orally Bioavailable Dual Mechanism ERK Inhibitor for Oncology.

K. Cox, P. Kirschmeier, R. Doll, 2018, ACS medicinal chemistry letters.

SCH-C (SCH 351125), an orally bioavailable, small molecule antagonist of the chemokine receptor CCR5, is a potent inhibitor of HIV-1 infection in vitro and in vivo

Serena Xu, Anandan Palani, William J. Greenlee, 2001, Proceedings of the National Academy of Sciences of the United States of America.

Design and validation of bicyclic iminopyrimidinones as beta amyloid cleaving enzyme-1 (BACE1) inhibitors: conformational constraint to favor a bioactive conformation.

William Greenlee, Lynn Hyde, Xia Chen, 2012, Journal of medicinal chemistry.

Discovery of an Orally Available, Brain Penetrant BACE1 Inhibitor that Affords Robust CNS Aβ Reduction.

Suresh Babu, William J Greenlee, Xia Chen, 2012, ACS medicinal chemistry letters.

Structure-Based Design of an Iminoheterocyclic β-Site Amyloid Precursor Protein Cleaving Enzyme (BACE) Inhibitor that Lowers Central Aβ in Nonhuman Primates.

Lynn A. Hyde, W. Greenlee, A. Stamford, 2016, Journal of medicinal chemistry.

Improving the oral efficacy of CNS drug candidates: discovery of highly orally efficacious piperidinyl piperidine M2 muscarinic receptor antagonists.

W. Greenlee, J. Lachowicz, J. Clader, 2002, Journal of Medicinal Chemistry.

Overcoming Time-Dependent Inhibition (TDI) of Cytochrome P450 3A4 (CYP3A4) Resulting from Bioactivation of a Fluoropyrimidine Moiety.

Lynn A. Hyde, A. Stamford, J. Cumming, 2018, Journal of medicinal chemistry.

Bicyclo[3.1.0]hexyl urea melanin concentrating hormone (MCH) receptor-1 antagonists: impacting hERG liability via aryl modifications.

Mark D. McBriar, H. Guzik, S. Shapiro, 2006, Bioorganic & medicinal chemistry letters.