This document summarizes the qualifications of Frederic Feru, an experienced medicinal chemist. Over his 30 year career, Feru has worked at several pharmaceutical companies and research institutions. He has expertise in medicinal chemistry, drug design, organic synthesis, and leading projects from hit identification to clinical trials. Some of Feru's accomplishments include advancing a PDE4 inhibitor into first-in-human trials, progressing 5 projects to in vivo proof of concept, and helping to develop a FAAH inhibitor that reached Phase II clinical trials.
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1. FREDERIC FERU
10 Murdock Street
Somerville, MA 02145
Tel. (home): 617 625 1177
Tel. (cell): 617-620-1305
f.feru2006@rcn.com
http://www.linkedin.com/in/fredericferu
SUMMARY
Enthusiastic medicinal and organic chemist with 30 years of research experience in a variety of
therapeutic areas such as: oncology, inflammation, inflammatory pain, cardiovascular and metabolic
disease. Use extensively Structure-Activity Relationship (SAR) and Structure-Property Relationship
(SPR). Expert in medicinal and parallel chemistry approaches (solid and solution phase) for a wide
variety of novel chemical entities for new biological targets. Highly adept for the scale-up
optimization of reactions. Proficient in using chemical databases/searching software and other
proprietary computational software for property prediction and data visualization. Focus in
communication, autonomy and team working skills. Demonstrate leadership in successful programs
by delivering:
• A selective phosphodiesterase type 4 (PDE-IV) inhibitor into First In Human.
• Advancing 5 projects from high-throughput screen hit stage to in vivo proof of concept.
• A Fatty Amino Acid Hydrolase (FAAH) inhibitor, PF-04457845 into phase II clinical trials.
• 2 technology projects that target DFG-Out conformation protein kinases for HTS binding
assay.
EXPERTISE
• Medicinal chemistry, Structure-Activity Relationship (SAR) analysis, molecular modeling, Drug
Design (SBDD).
• Synthetic route design and performance of multi-step, complex organic synthesis.
• Optimization of reaction conditions for parallel liquid and solid phase synthesis.
• Purification (flash chromatography, preparative HPLC, supported reagents and crystallization).
• High Performance Liquid Chromatography: Quality Control of the compounds synthesized.
• Lc Ms expertise using Mass Lynx software
• Gas Chromatography expertise.
• Independent characterization and interpretation of experimental results (NMR 1D, 2D, Magic-
Angle Spinning NMR, mass spectra, Fournier Transform Infrared Spectroscopy (FT-IR)).
EXPERIENCE
HepatoChem Inc., Beverly, MA 05/2014-09/15/2015
Scientist:
Based on a late-stage functionalization platform: Synthesis of metabolites and analogs.
Generation and production of metabolites and analogs for biological testing.
HepatoChem Inc., Beverly, MA 05/2013-10/31/2013
Scientist:
Northeastern University, Boston, MA. 09/2010-10/2011
Department of Chemistry and Chemical Biology: Associate Professor Michael Pollastri’s
laboratory.
Visiting Research Scientist:
Neglected disease and Drug Discovery.
Design and synthesize novel potential small molecule therapeutics for inflammatory and infection
diseases. Perform Structure-Activity Relationship (SAR) and Structure-Property Relationship (SPR)
studies for multi parameter optimization of lead chemical series. Mentor graduate students.
• Chagas disease: Histone Deacetylase (HDAC) inhibitor.
2. • Aryl hydrocarbon receptor (AhR) inhibitor.
FREDERIC FERU PAGE 2
Pfizer, Inc. 2001-2010
Biotherapeutics and Bioinnovations Center, Cambridge, MA. Medicinal Chemistry Department.
Senior Scientist: 2008-2010
• Designed novel RNA and DNA mimics with improved nuclease stability.
• Synthesized novel nucleosides for incorporation into siRNA and antisense oligonucleotides.
FREDERIC FERU PAGE 2
Research Technology Center, Cambridge, MA. 2007-2008
Senior Scientist: Medicinal Chemistry Department.
Designed and synthesized novel potential small molecule therapeutics. Performed Structure-Activity
Relationship (SAR) and Structure-Property Relationship (SPR) studies for multi parameter
optimization of lead chemical series, including potency, ADME properties (solubility, permeability,
metabolic stability & bioavailability), and toxicity.
• Cardiovascular and Metabolic disease: Research focused on novel non-classical kinase
inhibitors (Type II) as potential treatment for a chronic disease.
• Oncology: Led a chemistry team effort in developing a Type II kinase inhibitor project from
high-throughput screening Hit to Lead. Demonstration of in vivo proof-of-concept.
• Inflammation: Led a chemistry team effort focused on the design and synthesis of
fluorescent probes for non-classical p38α assay development. Two novel non-classical p38α
inhibitors were identified and co-crystallized with the inactive form of p38α. Received a Pfizer
Personal Achievement Award for this contribution (2006).
Scientist: 2003-2007
• Key synthetic and medicinal chemist in the following drug discovery programs that
progressed successfully from high-throughput screen to in vivo proof of concept:
- Oncology: PLK1 adenosyl triphosphate (ATP) kinase inhibitor project, (Type I).
- Inflammatory Pain: Irreversible Fatty Acid Amide Hydrolase (FAAH) inhibitor. PF-
04457845 in phase II clinical trials.
- Inflammation: Chemokine antagonist project.
• Applied Structure-Based Drug Design (SBDD) for enrichment of the Pfizer Kinase Targeted
Library, enhancing classical and non-classical kinase inhibitor library designs.
Pfizer PGRD, Fresnes (France). Medicinal Chemistry Department.
Associate Scientist II: 2001-2003
Allergy and Respiratory:
Led a chemistry team effort through the Hit to Lead stage of a GPCR antagonist project (CRTH2
antagonists), achieving a compound with Advanced Lead status. Received a Team Achievement Award
for this contribution (2002).
IRJ/Parke-Davis, Fresnes (France). Medicinal Chemistry Department. 1997-2001
Associate Scientist I:
Inflammation:
Key medicinal chemistry contributor for design and synthesis and SAR/SPR optimization, from the Hit
to clinical candidate stage of the Lipid Kinase inhibitor project, PI3-Kinaseγ inhibitors, with a declaration
of a First In Human.
Jouveinal, Fresnes (France). Medicinal Chemistry Department. 1992-1997
Associate Scientist I:
Allergy & Respiratory:
Key medicinal chemistry contributor to the phosphodiesterase IV inhibitor project, which advanced from
HTS stage to a declaration of first in Human; Designed and synthesized PDE IV inhibitors, including CI-
1018, the clinical candidate.
3. FREDERIC FERU PAGE 3
ISOCHEM (SNPE Group, France). Process Development Department. 1984-1992
Assistant Scientist:
Process chemistry optimization for the production of key intermediates for major pharmaceutical
companies.
EDUCATION
Master in Science, Chemistry: Faculté de Pharmacie Paris XI (Chatenay Malabry – France). 2002
Bachelor in Science, Chemistry: Institut Universitaire de Technologie, (Rouen – France). 1982
COMPUTING SKILLS
• Database searching (MDL databases, Scifinder, Beilstein) to develop of well-designed
inhibitors/antagonists and improved synthetic routes.
• Thoroughly familiar with IsisBase, Chemdraw, Microsoft Office, SYBIL (3D QSAR), Docking
and data visualization software (i.e. Spotfire).
COMMUNICATION AND TEAM SKILLS
• Demonstrated medicinal chemistry leadership for individual chemical series as part of a project
team.
• Extensive experience in presenting project summaries, results and progress, both internally
and externally.
• Routinely interacted with project team members from different disciplines.
• Successful mentorship of junior chemists.
• Coordinated project work with other department members.
ADDTIONAL INFORMATION
• Served as the Chemistry Representative on the Pfizer RTC Safety Committee.
• Chairman of Français du Monde, ADFE New England. French Nonprofit Association. For 3
years.
• American Chemical Society member (medicinal chemistry, organic division). For 8 years.
PUBLICATIONS
Enhanced selectivity profile of pyrazole-urea based DFG-out p38α inhibitors. Bioorganic &
Medicinal Chemistry Letters (2010), 20, 4885-4891.
Hu Liu, Cyrille Kuhn, Fred Feru, Suzanne L. Jacques, Gayatri D. Deshmukh, Ping Ye, Glen Rennie,
Theresa Johnson, Steven Kazmirski, Simon Low, Rocco Coli, Yuan-hua Ding, Haile Tecle, Jessie M.
English, Robert Stanton, and Joe C. Wu. Research Technology Center, Pfizer Inc., 620 Memorial
Drive, Cambridge, MA 02139.
The Design, Synthesis and Potential Utility of Fluorescence Probes That Target DFG-Out
Conformation of p38α for HTS Binding Assay. Chemical Biology & Drug Design (2009), 74 (6),
547-59. Haile Tecle, Frederic Feru, Hu Liu, Cyrille Kuhn, Glen Rennie, Mark Morris, Jiangxing
Shao, Alan C. Cheng, Diana Gikunju, Juan Miret, Rocco Coli, Simon (Hualin) Xi, Susan L. Clugston,
Simon Low, Steven Kazmirski, Yuan-Hua Ding, Qing Cao, Theresa L. Johnson, Gayatri D.
Deshmukh, Joe C. Wu, Jessie M. English. Research Technology Center, Pfizer Inc., 620 Memorial
Drive, Cambridge, MA 02139.
Selectivity-determining Residues in Plk1. Chemical Biology & Drug Design (2007), 70(6), 540-6.
Kothe, Michael; Kohls, Darcy; Low, Simon; Coli, Rocco; Rennie, Glen R; Feru, Frederic; Kuhn,
4. Cyrille; Ding, Yuan-Hua. Research Technology Center, Pfizer Inc., 620 Memorial Drive, Cambridge,
MA 02139.
FREDERIC FERU PAGE 4
Synthesis, Structure-Activity Relationships, and Pharmacological Profile of 9-Amino-4-oxo-1-
phenyl-3,4,6,7-tetrahydro [1,4]diazepino[6,7,1-hi]indoles : Discovery of Potent, Selective
Phosphodiesterase Type 4 Inhibitors. J. Med. Chem. (2000), 43(25), 4850-4867.
Burnouf, C.; Auclair, E.; Avenel, N.; Bertin, B.; Bigot, C.; Calvet, A.; Chan, K.; Durand, C.; Fasquelle, V.;
Feru, F.; Gilbertsen, R.; Jacobelli, H.; Kebsi, A.; Lallier, E.; Maignel, J.; Martin, B.; Milano, S.; Ouagued,
M.; Pascal, Y.; Pruniaux, MP.; Puaud, J.; Rocher, MN.; Terrasse, C.; Wrigglesworth, R.; Doherty, A.;
Pfizer Global Research & Development, Fresnes, France.
Synthesis and structure-activity relationships of 4-oxo-1phenyl-3,4,6,7-tetrahydro-
[1,4]diazepino[6,7,1hi]indoles : novel PDE4 inhibitors. Bioorganic & Medicinal Chemistry
Letters (2000), 10 (1), 35-38.
Pascal, Y.; Andrianjara, C.; Auclair, E.; Avenel, N.; Bertin, B.; Calvet, A.; Feru, F.; Lardon, S.; Moodley,
I.; Ouaged, M.; Payne, A.; Pruniaux, MP.; Szilagyi, C.; I RJ-Parke-Davis, Fresnes, France.
PATENTS
Preparation of acylaminoquinolines as CRTH2 antagonists.
Kuhn, Cyrille; Feru, Frederic; Bazin, Marc; Awad, Mohamed; Goldstein, Steven, Wayne; EP 143356.
Preparation of tetrahydroquinoline derivatives as CRTh2 antagonist.
Awad, Mohamed Ali; Bazin, Marc; Feru, Frederic; Goldstein, Steven Wayne; Kuhn, Cyrille Francois.
WO 2004035543.
A preparation of tetrahydroquinoline derivatives as CRTH2 antagonists.
Kuhn, Cyrille; Feru, Frederic; Bazin, Marc; Awad, Mohamed; Golstein, Steven, Wayne; EP 1413306.
LECTURE
Pharmacology of the novel phosphodiesterase type 4 inhibitor, CI-1018. ACS National Meeting,
Dallas, March 29-April 2 (1998).
Burnouf, C.; Pascal, Y.; Andrianjara, R.; Auclair, E.; Avenel, N.; Bertin, B.; Calvet, A.; Feru, F.;
Gilbertsen, R.; Lardon, S.; Moodley, I.; Pruniaux, M-P.; Szilagyi, C.; Payne, A.
POSTERS
Late-stage functionalization platform for lead optimization and diversification: Generation of
high value compounds for biological testing. ACS National meeting, Boston, August16-20 (2015).
Buzdygon, Ryan S; Cushner, Max; Feru, Frederic; Bazin, Marc J.
Targeting the Kinase DFG-Out Pocket: Probes for identifying Novel NCKI Chemical Matter.
Pfizer RTC, 620 Memorial Drive, Cambridge, MA, 02139.*
Pfizer La Jolla, 10770 Science Drive Road,
San Diego, CA 92121.Pfizer internal medicinal chemistry symposium (2007). England, UK.
Fred Feru; Emilia Bora; Qing Cao; Rocco Coli; Susan Clugston; Gayatri Deshmukh; Jonathan
DiNitto; Jessie English; Yuan-Hua Ding; Ketan Gajiwala*
; Diana Gikunju; Suzanne Jacques-
O’Hagan; Theresa Johnson; Steven Kazmirski; Cyrille Kuhn; Hu Liu; Simon Low; Juan Miret; Glen
Rennie; Tomi Sawyer; Joe Wu; Mark Wysk; Simon Xi; Haile Tecle.
Synthesis and structure-activity relationships of 9-methoxy-4-oxo-1-phenyl-3,4,6,7-tetrahydro-
[1,4]diazepino[6,7,1-hi] indolines : Novel PDE 4 inhibitors. ACS National Meeting, Boston, August
23-27 (1998).
Feru, F.; Pascal, Y.; Andrianjara, C.; Auclair, E.; Avenel, N.; Bertin, B.; Calvet, A.; Dounas, B.; Lardon,
S.; Marsoullier, E.; Moodley, I.; Pruniaux, MP.; Szilagyi, C.; Payne, A.
Synthesis and structure-activity relationships of 4-oxo-1-pheyl-3,4,6,7-tetrahydro-
[1,4]diazepino[6,7,1-hi]indolines: Novel PDE4 inhibitors. ACS National Meeting, Dallas, March
29-April 2 (1998),
Pascal, Y.; Andrianjara, R.; Auclair, E.; Avenel, N.; Bertin, B.; Calvet, A.; Feru, F.; Lardon, S.;