John W. F. Whitehead, Ph.D.
 215-968-8976 or 267-207-8529
155 North State Street,
Newtown, PA, 18940.
jwfwhitehead@verizon.net
Nationality: British citizen
With US Green Card
PROFILE
An Oxford educated Senior Principal Scientist with over 20 years of innovative drug discovery
experience in the pharmaceutical/ biotech industry. Drove forward a range of drug discovery and
development projects in 10-year career with GSK, 4+ years with Napp Pharmaceuticals (Purdue UK), and
12 years in the US with Purdue Pharma. Possessor of a unique skill set which include an excellent
knowledge of organic chemistry, a wide experience of medicinal and process chemistry, superb
leadership ability and well-developed analytical skills and an attention to detail that leads to successful
project outcomes.
Excellent man management skills; ORL-1 pain program joint team leader for Purdue Pharma from 20072012 managing team of 20 people from Purdue, Cranbury, NJ and Shionogi Pharmaceuticals, Osaka,
Japan. Strong record of adding value to pharma R&D organizations by applying talent and focus to
programs; named inventor of 10 PCT patents and author of 12 highly-cited scientific publications. Highvalue inventions include the marketed drug Lotronex™, see https://www.lotronex.com/
PROFESSIONAL EXPERIENCE
Discovery Pharma Consulting LLC, West Chester, PA
May 2012-present
Senior Consultant
Working with the Founder to provide input to clients requesting expert Pharma R&D Consulting services.
Specializing in R&D Strategy, Drug Discovery Innovation including Hit-to-Lead, Lead Optimization,
Preclinical Development and Cheminformatics. Also provided are Medicinal Chemistry guidance, Due
Diligence reviews, IP Expert Witness work for law firms, strategic IP and R&D Portfolio reviews, see:
www.discoverypharm.com
Purdue Pharma, Cranbury, NJ
2000-April 2012
Senior Principal Scientist
Relocated from Napp Pharmaceuticals, the UK subsidiary of Purdue Pharma, to drive forward
success in the drug discovery group under Dr. Don Kyle.
 Designed a more efficient route for scale-up of a peripheral mu agonist clinical candidate
(V113741), and helped transfer this process to Aerojet Chemicals, Sacramento, California.
 Made a major scientific contribution to ORL-1 agonist program both in ideas, and as joint team
leader 2007-2012. Patent inventor on key ORL1 patents and key contributor to development of
clinical drug candidate (V117957).
 Prepared the first 100g batch of ORL-1 clinical candidate (V117957) for formulation studies.
Made key process improvements to the synthesis of this complex molecule with 6 chiral centers,
reducing the synthesis to 10 steps and enabled method to be transferred to pilot plant at Albany
Molecular, New York. Enabled outsourcing of key intermediate to Albany Molecular in India.

Designed and carried out the process route to a novel TRPV-1 antagonist, and carried out the first
kilo batch synthesis single handedly.
Napp Pharmaceuticals, Cambridge, UK.
1996-Oct. 2000
Consultant Scientist
 Made a major contribution to the design of a shorter more efficient synthesis of a novel PDE4
inhibitor (V11294A) for asthma, which entered phase I development in 1997.
 A major contributor to a Napp (Euroceltique) PDE4 patent application.
GSK, Ware, Hertfordshire, UK .
1986-1996
Senior Scientist
 Inventive patent contributor to process route for 5-HT3 antagonist alosetron (brand name Lotronex™)
marketed in 2000 for female irritable bowel syndrome.
 Made important contribution to identifying a drug candidate GR113808 with a novel mode of action
against irritable bowel syndrome (5-HT4 antagonist) into exploratory development.
 Achieved a highly efficient (>80% yield) kinetic resolution of a racemic 1,4-benzodiazepine-3-amine,
enabling a key pharmacophore to be taken into chemical development.
 Successfully transferred the synthesis of menthyl glyoxylate hydrate from bench scale into pilot plant,
to prepare 75kg.
 Ran a popular Chemistry Literature Club in Med. Chem. at GSK for two years.
AWARDS AND HONOURS
 Full scholarship to The University of Oxford 1979-1983 (Michel Exhibitioner, The Queen’s College).
 Ph. D. Case Award from the Wellcome Foundation 1983-1986.
 Purdue Award for Innovation 2011.
Education
D. Phil.: The University of Oxford, 1983-1986: Research Thesis “An Approach to the Total Synthesis of
the Cytochalasans”.
Supervisor: Dr. E. J. Thomas (now professor of Chemistry at the University of Manchester).
M. A.: The Queen’s College, The University of Oxford, 1979-1983. Chemistry, Upper Second Class.
Research Thesis “The Synthesis of Some New Acridines as Potential Chemotherapeutic Agents”.
Supervisor: R. Morrim Acheson, The Queen’s College, Oxford (now retired).
Professional Societies:
The American Chemical Society
The Royal Society of Chemistry, (M. R. S. C. C. Chem.)
The Society for Medicines Research.
John W. F. Whitehead Ph. D.
ADDENDUM
Page 3 of 4
PUBLICATIONS
1. John W.F. Whitehead*; Gary P. Lee; Parviz Gharagozloo; Peter Hofer; Andre Gehrig, Peter
Wintergerst; Donald Smyth; William Mc Cool; Mohamed Hashisha; Aniket Patel; Donald J.
Kyle; 8-Substituted analogues of 3-(3-cyclopentyloxy-4-methoxy-benzyl)-8-isopropyl
adenine: highly potent and selective PDE4 inhibitors. J. Med. Chem. 2005, 48(4), 1237-1243.
2. P. J. Murray; R. M. Helden; M. R. Johnson; .G. M. Robertson; .D. I. C. Scopes; M. Stokes; J
Wadman; J. W. F. Whitehead; A. G. Hayes; Novel 6-Substituted 2-Aminotetralins with Potent
and Selective Affinity for the Dopamine D3 Receptor. Bioorg. Med. Chem. Lett., 1996, 6(4),
403-8.
3. J. D. Gale, C. J. Crossman, J. W. F. Whitehead; A. W. Oxford; K. T. Bunce; P. P. A.Humphrey;
GR113808 A Novel Selective Antagonist with High Affinity for the 5HT4 Receptor. Br. J.
Pharmacol., 1994, 111, 332-338.
4. M. J. Kelly, R. F. Newton, S. M. Roberts, J. W. F. Whitehead; Synthesis of 9-Deoxy-8,9Oxaprostaglandins. J. Chem. Soc. Perkin Trans. 1, 1990, 8, 2352-3.
5. E. J. Thomas, J. W. F. Whitehead; Cytochalasan Synthesis-Total Synthesis of Cytochalasan H.
J. Chem. Soc. Perkin Trans. 1, 1989, 507-518.
6. E. J. Thomas, J. W. F. Whitehead; Cytochalasan Synthesis, Total Synthesis of the Naturally
Occuring [13] cytochalasan Proxiphomin. J. Chem. Soc. Perkin Trans. 1, 1989, 499-507.
7. M. L. Boys, E. W. Collington, H. Finch, S. Swanson, J. W. F. Whitehead;
𝒂-Fluoromethyl-N-methyl-phenylsulphoximine, a New Fluoromethylenation Reagent.
Tetrahedron Letters, 1988, 29(27), 3365-8.
8. R. M. Acheson, D. H. Birtwhistle, E. C. Constable, G. G. Tester, J. W. F. Whitehead, P. B.
Wyatt; The Synthesis of Some Sterically Hindered Acridines and an High Pressure
Methylation. J. Chem. Res. Synop., 1986, 8, 269-95.
9. E. J. Thomas, J. W. F. Whitehead; Cytochalasan Synthesis-Total Synthesis of Cytochalasan H.
J. Chem. Soc. Chem. Commun., 1986, 9, 727-8.
10. E. J. Thomas, J. W. F. Whitehead; Cytochalasan Synthesis-Synthesis of an 11-Membered
Ring Precursor of Cytochalasan H. J. Chem. Soc. Chem. Commun., 1986, 9, 724-6.
11. A. J. Craven, D. J. Tapolczay, E. J. Thomas, J. W. F. Whitehead; An Approach to the Synthesis
of Cytochalasan D; 11-Membered Ring Formation using an Intramolecular Diels Alder
Reaction. J. Chem. Soc. Chem. Commun., 1985, 3, 145-7.
12. D. J. Tapolczay, E. J. Thomas, J. W. F. Whitehead. Total Synthesis of Proxiphomin, a
naturally occurring Cytochalasan. J. Chem. Soc. Chem. Commun., 1985, 3, 143-5.
GRANTED PATENTS AND PUBLISHED PATENT APPLICATIONS
1. Whitehead, John W. F.; Tsuno, Naoki; Fuchino, Kouki; Substituted Quinoxaline Type
Piperidine Compounds as ORL1 Receptor Modulators and their Preparation,
Pharmaceutical Compositions and use in the Treatment of Diseases. PCT Int. Appl. (2010)
WO 2010010458A1 20100128.
2. Goehring, Richard R; Matsumura, Akira; Shao Bin; Taoda, Yoshiyuki; Tsuno, Naoki; Whitehead,
John William Frank; Yao, Jiangchao; Quinoxaline-piperidine derivatives as ORL-1 receptor
modulators and their preparation, pharmaceutical compositions and use in the treatment of
diseases. PCT Int. Appl. (2009), WO 2009027820 A2 20090305.
3. Brown, Kevin; Doyle, Timothy, J; Whitehead, John W.F.; Process for preparation of 4tetrazolyl-4-phenylpiperidines from 4-cyano-4-phenylpiperidines and sodium azide in the
presence of zinc salts. US Pat. Appl. Publ. (2007) US 20070072909A1 20070329.
John W. F. Whitehead Ph. D.
Page 4 of 4
4. Parviz Gharaogozloo; Khondaker Islam; Donald J. Kyle; Qun Sun; Laykea Tafesse; John William
Frank Whitehead. Therapeutic agents useful for treating pain. US 6,864,261B2 March 8
2005.
5. Gharagozloo, Parviz; Islam, Khondaker; Kyle, Donald,J; Sun, Qun; Tafesse, Laykea; Whitehead,
John, W.F.; Yang, Ji; Zhou, Xiaoming; Preparation of 1-(pyrid-2-yl) piperazines as
metabotropic glutamate receptor antagonists. WO 2003309326A1, May 2 (2003).
6. Goehring, Richard R; Chen, Zhengming; Kyle, Donald; Victory, Sam; Gharagozloo, Parviz;
Whitehead, John William Frank. Nociceptin Analogs. PCT Intl. Appl. (2002) 149pp WO
0285357 A1 20021031.
7. D.J.Cavalla; M. Chasin; J.W.F. Whitehead; L. Walton; A. C. Mansfield; 2-Heteroaryl and 2heterocyclic benzoxazoles as PDE4 inhibitors for the treatment of asthma; US Patent
application 6,166,041 (1997).
8. J. W. F. Whitehead, K. Mills, I. H. Coates, A. W. Oxford, P. C. North; Process for the
preparation of lactam derivatives. US patent 5,196,534, 23 March 1993.
9. A. W. Oxford, J. Knight, J. W. F. Whitehead; Preparation of (Piperidinylmethoxycarbonyl)
indoles as Serotonin Antagonists. European Patent EP 501,322A1, 1992.
10. J. W. F. Whitehead, K. Mills, I. H. Coates, A. W. Oxford, P. C. North; Preparation of
Pyrido[4,3-b]indol-1-ones. European Patent EP458, 624A1, 1991.
OUTSIDE INTERESTS
Enjoys gardening, cycling, walking, coarse fishing, and listening to classical music. Has twice won the
Bucks Beautiful Garden competition in 2004 and 2005 for garden design. Also involved in amateur
dramatics in Barkway, England taking part in four village pantomimes.
Has an extensive knowledge of English and European history, particularly the 17th century. Was a major
contributor to The Chalgrove Battle Group a non-profit society which successfully lobbied English
Heritage to protect the English Civil war Battlefield of Chalgrove 1643 from housing development.
Contributed original historical research to a book “The Controversy of John Hampden’s Death” published
in 2000 by The Chalgrove Battle Group, ISBN 0-9538034-0-6.
Am the Stewardship Chairman at my local Episcopal Church, St. Luke’s in Newtown.
References:
1) Dr. Donald Kyle, Vice President Discovery Research; Purdue Pharma, 6, Cedarbrook Drive,
Cranbury, NJ, 08512. 609.409.5131  Don.Kyle@pharma.com
2) Dr. Laykea Tafesse, Director Medicinal Chemistry; Purdue Pharma, 6, Cedarbrook Drive,
Cranbury, NJ, 08512. 609-409-5837  Laykea.Tafesse@pharma.com
3) Dr. Lars Knutsen, President, Discovery Pharma LLC; 1005, Dunvegan Road, West Chester, PA,
19382. 610.410.5810.  LarsKnutsen@drexelmed.edu