Molecular complexity and retrosynthesis
Journal of Organic Chemistry, 2017, 82, 6968 -6971.
John R. Proudfoot

A path based approach to assessing molecular complexity
Bioorganic and Medicinal Chemistry Letters 2017, 27, 2014-2017
John R. Proudfoot

The Pistoia Alliance Controlled Substance Compliance Service Project: From Start to Finish
Drug Discovery Today2015, 20, 175-180
Daniel Taylor, Stuart G. Bowden, Reinhard Knorr, Derek R. Wilson, John Proudfoot, Anne E. Dunlop

Discovery of a potent and dissociated non-steroidal glucocorticoid receptor agonist containing an alkyl carbinol pharmacophore
Bioorganic and Medicinal Chemistry Letters, 2014, 24, 1934-1940
Hossein Razavi,* Doris Riether, Christian Harcken, Jörg Bentzien, Roger M. Dinallo, Donald Souza, Richard M. Nelson, Alison Kukulka, Tazmeen N. Fadra-Khan, Edward J. Pack Jr., Ljiljana Zuvela-Jelaska, Josephine Pelletier, Mark Panzenbeck, Carol A. Torcellini, John R. Proudfoot, Gerald H. Nabozny, David S. Thomson

Begin with the End in Mind: The hit-to-lead process
John R. Proudfoot
in “Handbook for DNA-Encoded Chemistry” John Wiley & Sons, ed. Robert Goodnow, 2014, 231-245.

Glossary of Terms used in Medicinal Chemistry (free download)
Derek Buckle,* Paul Erhardt, Robin C. Ganellin, John Proudfoot, Joerg Senn-Bilfinger.
Pure and Applied Chemistry, 2013, 85, 1725-1758.
Also published in:
Annual Reports in Medicinal Chemistry,  2013, 48, 387-418.

Reaction Schemes Visualized in Network Form: the syntheses of Strychnine as an example
John Proudfoot
Journal of Chemical Information and Modelling, 2013, 53, 1035–1042.

Discovery of Potent, Selective Chymase Inhibitors via Fragment Linking Strategies
Steven Taylor,* Anil Padyana, Asitha Abeywardane, Shuang Liang, Ming-Hong Hao, Stéphane De Lombaert, John Proudfoot, Bennett Farmer, Xiang Li, Brandon Collins, Leslie Martin, Melissa Hill-Drzewi, Steven Pullen, Hidenori Takahashi.
Journal of Medicinal Chemistry, 2013, 56, 4465–4481.

Fragment Based Discovery of Indole Inhibitors of Matrix Metalloproteinase-13
Steven J.Taylor, Asitha Abeywardane, Shaung Liang, Ingo Muegge, Anil K. Padyana, Zhaoming Xiong, Melissa Hill-Drzewi, Bennett Farmer, Xiang Li, Brandon Collins, John Xiang Li, Alexander Heim-Riether, John Proudfoot, Qiang Zhang, Daniel Goldberg, Ljiljana Zuvela-Jelaska, Hani Zaher, Jun Li, Neil A. Farrow.
Journal of Medicinal Chemistry, 2011, 54, 8174-8187.

Glossary of Terms used in Biomolecular Screening (free download)
John Proudfoot,* Olivier Nosjean, Jan Blanchard, John Wang, Dominique Besson, Denis Crankshaw, Gunter Gauglitz, Robert Hertzberg, Carol Homon, Lyndon Llewellin, Richard Neubig, Larry Walker, Pascal Villa.
Pure and Applied Chemistry, 2011, 83, 1129-1158.

Substituted pyrazoles as novel sEH antagonist: Investigation of key binding interactions within the catalytic domain  
Ho Yin Lo, Chuk C. Man, Roman W. Fleck, Neil A. Farrow, Richard H. Ingraham, Alison Kukulka, John R. Proudfoot, Raj Betageri, Tom Kirrane, Usha Patel, Rajiv Sharma, Mary Ann Hoermann, Alisa Kabcenell, Stéphane De Lombaert
Bioorganic and Medicinal Chemistry Letters, 2010, 20, 6379-6383.

SAR studies of non-zinc-chelating MMP-13 inhibitors: Improving selectivity and metabolic stability
Donghong Amy Gao,* Zhaoming Xiong,* Alexander Heim-Riether, Laura Amodeo, E. Michael August, Xianhua Cao, Leonard Ciccarelli, Brandon K. Collins, Kyle Harrington, Kathleen Haverty, Melissa Hill-Drzewi, Xiang Li, Shuang Liang, Steluta Mariana Margarit, Neil Moss, Nelamangala Nagaraja, John Proudfoot, Rene Roman, Sabine Schlyer, Lana Smith Keenan, Steven Taylor, Bernd Wellenzohn, Dieter Wiedenmayer, Jun Li, Neil A. Farrow
Bioorganic and Medicinal Chemistry Letters, 2010, 20, 5039–5043

Optimizing Drug Analogs
Janos Fischer, C. Robin Ganellin, John Proudfoot, Erika Alapi
in “Analog Based Drug Discovery, Volume II”, eds J. Fischer andC. R. Ganellin, Wiley-VCH, 2010

Standalone Drugs (free download)
Janos Fischer, C. Robin Ganellin, John Proudfoot, A. Ganesan
in “Analog Based Drug Discovery, Volume II”, eds J. Fischer andC. R. Ganellin, Wiley-VCH, 2010

Improving potency and selectivity of a new class of non-Zn-chelating MMP-13 inhibitors
Alexander Heim-Riether, Steven J. Taylor, Shuang Liang, Donghong Amy Gao, Zhaoming Xiong, E. Michael August, Brandon K. Collins, Bennett T. Farmer II, Kathleen Haverty, Melissa Hill-Drzewi, Hans-Dieter Junker, S. Mariana Margarit, Neil Moss, Thomas Neumann, John R. Proudfoot, Lana Smith Keenan, Renate Sekul, Qiang Zhang, Jun Li, and Neil A. Farrow
Bioorganic and Medicinal Chemistry Letters, 2009, 19, 5321

High-Throughput Screening and Drug Discovery
John R. Proudfoot
in “The Practice of Medicinal Chemistry, 3rd edition., ed. Camille Georges Wermuth,  2008 Elsevier Inc. Academic Press 2008.

Identification of Dissociated Nonsteroidal Glucocorticoid Receptor Agonists
Daniel Kuzmich, Tom Kirrane, John Proudfoot, Younes Bekkali, Renee Zindell, Laura Beck, Richard Nelson, Cheng-Kon Shih, Alison J. Kukulka, Zofia Paw, Patty Reilly, Rodney Deleon, Mario Cardozo, Gerald Nabozny, David Thomson.
Bioorganic and Medicinal Chemistry Letters, 2007, 17, 5025

Discovery and SAR study of novel dihydroquinoline-containing glucocorticoid receptor agonists
Hidenori Takahashi*, Younes Bekkali, Alison J. Capolino, Thomas Gilmore, Susan E. Goldrick, Paul V. Kaplita, Lisa Liu, Richard M. Nelson, Donna Terenzio, Ji Wang, Ljiljana Zuvela-Jelaska, John Proudfoot, Gerald Nabozny and David Thomson. 
Bioorganic and Medicinal Chemistry Letters, 2007, 17, 5091

Drug Discovery: Historical Perspective, Current Status and Outlook
Paul Erhardt and John Proudfoot
in “Comprehensive Medicinal Chemistry II, Volume 1” p29-96,  2006, ed. J. Taylor and D. Triggle; Elsevier, Oxford, United Kingdom.

Quinol-4-ones as Steroid A-ring Mimetics in Non-Steroidal Dissociated Glucocorticoid Agonists
John Regan,* Thomas Lee, Renée M. Zindell, Younes Bekkali, Jörg Bentzien, Alison Capolino, Thomas Gilmore, Abdelhakim Hammach, Thomas Kirrane, Daniel Kuzmich, Richard Nelson, John Proudfoot, Josephine Pelletier, Donald Souza, Lijiljana Zuvela-Jelaska, Gerald Nabozny and David Thomson.
Journal of Medicinal Chemistry, 2006, 49, 7887-7896

Discovery and Development of Nevirapine
Karl Grozinger, John Proudfoot and Karl Hargrave
in “Drug Discovery and Development, Volume 1” ed. M. S. Chorghade, John Wiley & Sons, Inc. 2006

Druglikeness and Analogue Based Drug Discovery
John Proudfoot
in “Analog Based Drug Discovery”, eds J. Fischer and C. R. Ganellin, Wiley-VCH, 2006

Discovery and SAR Study of Novel Dihydroquinoline Containing Glucocorticoid Receptor Ligands
Hidenori Takahashi*, Younes Bekkali, Alison J. Capolino, Thomas Gilmore, Susan E. Goldrick, Richard M. Nelson, Donna Terenzio, Ji Wang, John Proudfoot, Gerald Nabozny and David Thomson. 
Bioorganic and Medicinal Chemistry Letters, 2006, 16, 1549

A concise asymmetric route for the synthesis of a novel class of glucocorticoid mimetics containing a trifluoromethyl-substituted alcohol
Thomas W. Lee,* John R. Proudfoot and David S. Thomson
Bioorganic and Medicinal Chemistry Letters, 2006, 16, 654

Tetrazole Compounds: The Effect of Structure and pH on Caco-2 Cell Permeability
Amber M. Young,* Kenneth L. Audus, John Proudfoot and Mehran Yazdanian.
Journal of Pharmaceutical Sciences, 2006, 95, 717-725

The Evolution of Synthetic Oral Drug Properties
John R. Proudfoot
Bioorganic and Medicinal Chemistry Letters, 2005, 15, 1087-1090

A structure-permeability study of small drug-like molecules
Thomas Fichert, Mehran Yazdanian and John R. Proudfoot*
Bioorganic and Medicinal Chemistry Letters, 2003, 13, 719-722

Drugs, Leads and Drug-Likeness: an analysis of some recently launched drugs
John R. Proudfoot
Bioorganic and Medicinal Chemistry Letters, 2002, 12, 1647-1650

Non-peptidic, Monocharged, Cell Permeable Ligands for the p56lck SH2 Domain
John R. Proudfoot,* Rajashekhar Betageri, Mario Cardozo, Thomas A. Gilmore, Susan Glynn, Eugene R. Hickey, Scott Jakes, Alisa Kabcenell, Thomas M. Kirrane, Annette K. Tibolla, Susan Lukas, Usha R. Patel, Rajiv Sharma, Mehran Yazdanian and Neil Moss, Pierre L. Beaulieu, Dale R. Cameron, Jean-Marie Ferland, Jean Gauthier, James Gillard, Vida Gorys, Martin Poirier, Jean Rancourt, Dominik Wernic and Montse Llinas-Brunet. 
Journal of Medicinal Chemistry, 2001, 44, 2421-2431

Mechanisms of transport and structure–permeability relationship of sulfasalazine and its analogsin Caco-2 cell monolayers.
Earvin Liang, John Proudfoot and Mehran Yazdanian.* 
Pharmaceutical Research, 2000, 17, 1168-1173

HIV and AIDS Therapeutics
P.L Beaulieu and J. Proudfoot
Ullmann's Encyclopediaof Industrial Chemistry, 6th ed., Wiley-VCH, Weinheim, June 2000
Pharmaceuticals, 2000, 3, 1291-1317

Practical synthesis of 1,3-diaryl-5-alkylpyrazoles by a highly regioselective N-Arylation of 3,5-disubstituted pyrazoles with 4-fluoronitrobenzene
Xiao-Jun Wang,* Jonathan Tan, Karl Grozinger, Raj Betageri, Tom Kirrane and John R. Proudfoot
Tetrahedron Letters, 2000, 41, 5321-5324

Ligands for the Tyrosine Kinase p56lck SH2 Domain: Discovery of Potent Dipeptide Derivatives with Monocharged, Nonhydrolyzable Phosphate Replacements
Pierre L. Beaulieu,* Dale R. Cameron, Jean-Marie Ferland, Jean Gauthier, Elise Ghiro, James Gillard, Vida Gorys, Martin Poirier, Jean Rancourt, Dominik Wernic, Montse Llinas-Brunet, Raj Betageri, Mario Cardozo, Eugene R. Hickey, Richard Ingraham, Scott Jakes, Alisa Kabcenell, Tom Kirrane, Susan Lukas, Usha Patel, John Proudfoot, Rajiv Sharma, Liang Tong, and Neil Moss. 
Journal of Medicinal Chemistry, 1999, 42, 1757-1766

Phosphotyrosine-Containing Dipeptides as High-Affinity Ligands for the p56lck SH2 Domain
Montse Llinas-Brunet,* Pierre L. Beaulieu, Dale R. Cameron, Jean-Marie Ferland, Jean Gauthier, Elise Ghiro, James Gillard, Vida Gorys, Martin Porier, Jean Rancourt, Dominik Wernic, Raj Betageri, Mario Cardozo, Scott Jakes, Suzanne Lukas, Usha Patel, John Proudfoot and Neil Moss. 
Journal of Medicinal Chemistry, 1999, 42, 722-729

Carboxymethyl-phenylalanine as a replacement for phosphotyrosine in SH2 Domain binding
Liang Tong,* Thomas C. Warren, Susan Lukas, Josephine Schembri-King, Raj Betageri, John R Proudfoot, and Scott Jakes. 
Journal of Biological Chemistry, 1998, 273, 20238-20242

Non-nucleoside Inhibitors of HIV-1 Reverse Transcriptase
John R. Proudfoot
Expert Opinion on Therapeutic Patents, 1998, 8, 971-982

A Dipyrido[2,3-b:3',2'-f]azepine Analog of the HIV-1 Reverse Transcriptase Inhibitor Nevirapine
Alexey B. Dyatkin,* Janice R.Brickwood and John R. Proudfoot*
Bioorganic and Medicinal Chemistry Letters, 1998, 8, 2169-2172

7-Substituted Saccharins, 8-Substituted Oxicams and a Novel Saccharin to Oxicam Transformation
John R. Proudfoot,* Usha R. Patel and Alexey B. Dyatkin
Journal of Organic Chemistry, 1997, 62, 1851-1853

Novel Non-Nucleoside Inhibitors of HIV-1 Reverse Transcriptase 5. 4-Substituted and 2,4-Disubstituted Analogs of Nevirapine
Terence A. Kelly,* John R. Proudfoot, Daniel W. McNeil, Usha R. Patel, Eva David, Karl D. Hargrave, Peter Grob, Mario Cardozo, Atul Agarwal and Julian Adams
Journal of Medicinal Chemistry, 1995, 38, 4839

Novel Non-Nucleoside Inhibitors of HIV-1 Reverse Transcriptase. 4. 2-Substituted Dipyridodiazepinones are Potent Inhibitors of both Wild Type and Cysteine-181 HIV-1 Reverse Transcriptase Enzymes
John R. Proudfoot,* Karl D. Hargrave, Suresh R. Kapadia, Usha R. Patel, Karl G. Grozinger, Daniel W. McNeil, Ernest Cullen, Mario Cardozo, Liang Tong, Terence A. Kelly, Janice Rose, Eva David, Scott C. Mauldin, Victor U. Fuchs, Jana Vitous, MaryAnn Hoermann, Janice M. Klunder, Palayakotai Raghavan, Jerry W. Skiles, Philip Mui, Douglas D. Richman, John L. Sullivan, Cheng-Kon Shih, Peter Grob, and Julian Adams
Journal of Medicinal Chemistry, 1995, 38, 4830-4838

Novel Non-Nucleoside Inhibitors of HIV-1 Reverse Transcriptase. 3. Dipyrido[2,3-b:2',3'-e] diazepinones
John R. Proudfoot,* Usha R. Patel, Suresh R. Kapadia and Karl D. Hargrave
Journal of Medicinal Chemistry, 1995, 38, 1406-1410

The Synthesis Of A Dipyrido[3,2-b:3',4'-e][1,4]Diazepinone: Convenient Access To a C-Ring Isomer of the HIV-1 Reverse Transcriptase Inhibitor Nevirapine
John R. Proudfoot
Bioorganic and Medicinal Chemistry Letters, 1995, 5, 163-166

A Novel Smiles Rearrangement gives Access to the A-Ring Pyridine Isomers of the Nevirapine Ring System
John R. Proudfoot,* Usha R. Patel and Scot J. Campbell
Journal of Organic Chemistry, 1993, 58, 6996-7000

The Synthesis of 11-Cyclopropyl-5,11-dihydro-4-(hydroxymethyl)-6H-dipyrido[3,2-b:2',3'-e] [1,4]diazepin-6-one, a Putative Metabolite of the HIV-1 Reverse Transcriptase Inhibitor Nevirapine.
Usha R. Patel and John R. Proudfoot*
Journal of Organic Chemistry, 1992, 57, 4023-4025

Novel Non-Nucleoside Inhibitors of HIV-1 Reverse Transcriptase. 1. Tricyclic Pyridobenzo- and Dipyridodiazepinones
Karl D. Hargrave,* John R. Proudfoot, Karl G. Grozinger, Ernest Cullen, Suresh R. Kapadia, Usha R. Patel, Victor U. Fuchs, Scott C. Maulden, Jana Vitous, Mark L. Behnke, Janice M. Klunder, Kollol Pal, Jerry W. Skiles, Daniel W. McNeil, Janice M. Rose, Grace C. Chow, Mark T. Skoog, Joe C. Wu, Gunther Schmidt, Wolfhard G. Eberlein, Tracy D, Saboe, Scot J. Campbell, Alan S. Rosenthal and Julian Adams
Journal of Medicinal Chemistry, 1991, 34, 2231-2241

A Novel Dipyridodiazepinone Inhibitor Of HIV-1 Reverse Transcriptase Acts Through a Nonsubstrate Binding Site.
Joe C. Wu,* Thomas C. Warren, Julian Adams, John Proudfoot, Jerry Skiles, Palayakotai Raghavan, Clark Perry, Ian Potoki, Peter R. Farina and Peter M. Grob
Biochemistry, 1991, 30, 2022-2026

 

 

 

Patents

Karl D. Hargrave, John R. Proudfoot, Julian Adams, Karl G. Grozinger, Gunther Schmidt, Wolfhard Engel, Gunther Trummlitz and Wolfgang Eberlein.
Novel 5,11-dihydro-6H-dipyrido [3,2-b:2',3'-e][1,4]diazepin-6-ones and their use in the prevention or treatment of AIDS.
US5366972 (Nov 22 1994).

Karl D. Hargrave, Ernest A. Cullen, John R. Proudfoot, Karl G. Grozinger, Kollol Pal and Julian Adams.
Dipyrido[3,2-b:2',3'-e][1,4]diazepines and their use in the treatment of HIV infection.
U5550117 (Aug 27 1996).

Karl D. Hargrave, Ernest A. Cullen, John R. Proudfoot, Karl G. Grozinger, Kollol Pal and Julian Adams.
Pyrido[2,3-b][1,4]benzodiazepine derivatives useful for the treatment of HIV infection.
US5593979 (Jan 14, 1997).

Karl D. Hargrave, Ernest A. Cullen, John R. Proudfoot, Karl G. Grozinger, Kollol Pal and Julian Adams.
Pyridobenzo and pyridothieno-diazepines useful for the treatment of HIV infection.
US5602113 (Feb 11, 1997).

Karl D. Hargrave, John R. Proudfoot, Julian Adams, Karl G. Grozinger, Gunther Schmidt, Wolfhard Engel, Gunther Trummlitz and Wolfgang Eberlein.
Novel 5,11-dihydro-6H-dipyrido [3,2-b:2',3'-e][1,4]diazepin-6-ones and their use in the prevention or treatment of AIDS.
US5620974(Apr 15, 1997).

Karl D. Hargrave and John R. Proudfoot.
2-Aryl-5,11-dihydro-6H-dipyrido[3,2-b:2’,3’-e][1,4]diazepines and their use in the treatment of HIV-1 infection.
US5747488 (May 5, 1998).

Karl D. Hargrave, Terence A. Kelly, Suresh R. Kapadia, John R. Proudfoot, Daniel W. McNeil, Usha R. Patel, Mario Cardozo.
2-Heteroaryl-5,11-dihydro-6H-dipyrido[3,2-b:2',3'-e][1,4] diazepines and their use in the prevention or treatment of HIV infection.
US5837704 (Nov 17, 1998).

John R. Proudfoot and Alexey B. Dyatkin.
Dipyridoazepines and their use in the prevention or treatment of HIV infection.
U.S. 5869482 (Feb 9, 1999).

Karl D. Hargrave and John R. Proudfoot.
5, 11-Dihydro-6H-dipyrido[3,2-b][2’,3’-e]azepine-6-ones and their use in the prevention or treatment of HIV infection.
US5908841 (June 1, 1999).

 Karl D. Hargrave John R. Proudfoot, Suresh R Kapadia.
5,6-Heteroaryl-dipyrido[2,3-b:3’,2’-f]azepines and their use in the treatment of HIV.
US5919779 (July 6, 1999).

Rajashekhar Betageri, Pierre L. Beaulieu, Montse Llinas-Brunet, Jean-Marie Ferland,  Mario Cardozo, Neil Moss, Usha Patel, John R. Proudfoot.
Pyridones as SRC family SH2 domain Inhibitors.
WO9931066 (June 24, 1999).
US6054470 (April 25, 2000).
US6268365 (July 31, 2001).
US6284768 (September 4, 2001).

Rajashekhar Betageri, Charles L. Cywin, Karl Hargrave, Mary Ann Hoermann, Thomas M. Kirrane, Thomas Parks, Usha R. Patel, John R. Proudfoot, Rajiv Sharma, Sanxing Sun, Xiao-Jun Wang.
Substituted 1-(4-aminophenyl)pyrazoles and their use as anti-inflammatory agents.
WO9962885 (Dec 9, 1999).
US6506747 (Jan 14, 2003).

Rajashekhar Betageri, Jean-Marie Ferland,  Montse Llinas-Brunet, Neil Moss, John R. Proudfoot,  Compounds useful as phosphotyrosine mimics.
WO0062770 (October 26, 2000).
US6156784 (December 5, 2000)

Rajashehar Betageri, Steffen Breitfelder, Pier F Cirillo, Thomas A Gilmore, Eugene R Hickey, Thomas M Kirrane, Monica H. Moriak, Neil Moss, Usha R Patel, John R Proudfoot, John R. Regan, Rajiv Sharma, Sanxing Sun, Alan D. Swinamer, Hidenori Takahashi.
Compounds useful as TNF synthesis inhibitors.
WO0055139 (Feb 16, 2000).
US6660732 (Dec 9, 2003).
US7019006 (March 28, 2006)
US7026476 (April 11, 2006).

Steffen Breitfelder, Pier F. Cirillo, Thomas A. Gilmore, Eugene R. Hickey, John R. Proudfoot, John R. Regan, Alan D. Swinamer, Hidenori Takahashi.
Compounds useful as anti-inflammatory agents.
U.S. 6,358,945 (March 19, 2002).

Richard H. Ingraham, Mario G. Cardozo, Christine A. Grygon, Rachel R. Kroe, John R. Proudfoot.
Fluorescence polarization assay.
WO0282082 (Oct 17, 2002)
US6794158 (September 21, 2004)

Susan E. Goldrick, Richard M. Nelson, James Crute, Ruby Wasti, Gerald H. Nabozny, John R. Proudfoot, David S. Thomson.
Methods and labeled probes for determining ligand binding to steroid receptors.
WO020953354. (Jan 23, 2003).

Richard H. Ingraham, John R. Proudfoot.
Methods of using soluble epoxide hydrolase inhibitors.
WO03002555 (Jan 9, 2003).
US6831082 (December 14, 2004).
US6890925 (May 10, 2005)

 Younes Bekkali, Raj Betageri, Thomas A. Gilmore, Mario G. Cardozo, Thomas M. Kirrane, Daniel Kuzmich, John R. Proudfoot, Hidenori Takahashi, David Thomson, Ji Wang, Renee Zindell, Christian Harcken, Doris Riether.
Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof.
WO03082280 (Oct 9, 2003).

Younes Bekkali, Mario G. Cardozo, Thomas M. Kirrane, Daniel Kuzmich, John R. Proudfoot, Hidenori Takahashi, David Thomson, Ji Wang, Renee Zindell, Christian Harcken, Hossein Razavi.
Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof.
WO03082787 (Oct 9, 2003).
US7268152 (Sept 11, 2007)
US8212040 (July 3, 2012)

David Thomson, Daniel Kuzmich, Thomas M. Kirrane, John Robert Proudfoot.
Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof.
WO03101932 (Dec 11, 2003).
US7186864 (Mar 6, 2007)
US7795272 (Sept 14, 2010)

David Thomson, Daniel Kuzmich, Thomas M. Kirrane,  John Robert Proudfoot, Hossein Rasavi.  4-Aryl or heteroaryl -2-butylamine derivatives and their use as glucocorticoid ligands.
WO03104195 (Dec 18, 2003).
US7074806 (July 11, 2006).

John Robert Proudfoot, John Robinson Regan, David S. Thomson, Daniel Kuzmich, Thomas Wai-Ho Lee, Abdelhakim Hammach, Mark Stephen Ralph, Renee Zindell, Younes Bekkali.
Novel trifluoromethyl-1-propanol and propylamine glucocorticoid receptor modulators useful for treating eg diabetes and obesity.
WO04063163 (July 29 ,2004).
US7579469 (August 25, 2009).

Charles Lawrence Cywin, Tina Marie Morwick, John Proudfoot, David Robert Thomson. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof.
WO04075864 (September 10, 2004).

Weimin Liu, Eugene Richard Hickey, Charles Lawrence Cywin, Roman Wolfgang Fleck, Denice M. Spero, Tina Marie Morwick, John Robert Proudfoot.
Pyrido[3′,2′:4,5]thieno[3,2-d]pyrimidines and related derivatives are IKK inhibitors useful in the treatment of inflammation, autoimmune disorders and cancer”
WO05035537 (21 April 2005).
US7291733 (Nov 6, 2007)

Younes Bekkali, Rajashehar Betageri, Michael J Emmanuel, Abdelhakim Hammach, Hanke Justus Joachim Harcken, Thomas Martin Kirrane, Daniel; Kuzmich, Thomas Wai-ho Lee, Pingrong Liu, Usha R. Patel, Hossein Razavi, Doris Riether, Hidenori Takahashi, David S. Thomson, Ji Wang, Renee Zindell, John Robert Proudfoot.
Preparation of hydroxytrifluoromethylalkylpyrrolopyridines, -indoles, and related compounds as modulators of glucocorticoid receptor function
WO05030213 (7 April, 2005).
US7932392 (26 April 2011)
US8741897 (3 June 2014)

Thomas Martin Kirrane, Jr., Daniel Kuzmich, John Robert Proudfoot.
New glucocorticoid mimetics are glucocortioid receptor modulators - useful for the treatment of type II diabetes and obesity
US20050203128 (15 September, 2005).

Thomas Martin Kirrane, Daniel Kuzmich, John Robert Proudfoot.
2-Propanol and 2-propylamine derivatives and their use as glucocorticoid ligands
WO05090336 (29 September, 2005).

John Robinson Regan, Thomas Wai-Ho Lee, David Thomson, Thomas Martin Kirrane, Daniel Kuzmich, John Robert Proudfoot, Younes Bekkali, Renee Zindell.
New alpha-trifluoromethyl alcohols or amines are glucocorticoid receptor modulators.
WO05095401 (13 October 2005).

Thomas Wai-Ho Lee, John Robert Proudfoot.
Process for the stereoselective preparation of intermediates of glucocorticoid receptor ligands - comprises reacting a trifluoromethyl derivative with a chiral sulfoxide anion source, reducing the sulfoxide and cyclizing.
US20050234250 (20 October 2005).
US7256300 (14 August, 2007).

Nelson, Richard More; Liu, Pingrong; Proudfoot, John Robert; Riether, Doris; Harcken, Christian Hanke Justus Joachim; Thomson, David S.
Anti aromatase compounds pharmaceutical compositions and uses thereof.
US2006030608.