LET'S CONNECT
"Somewhere, something incredible is waiting to be known"
Carl Sagan
ACADEMICS-TO-INDUSTRY
2011 - present
Academics-to-Industry originated as an American Chemical Society Innovative Project Grant (IPG) sponsored program in 2011. A2I is designed for chemists with no industry experience who are considering a career in the biopharmaceutical industry. We aim to provide an introduction to topics such as structure-activity relationships, structure-based drug design, barriers to exposure, metabolism, toxicity, pharmacokinetics, and in vitro and in vivo pharmacology that are often not adequately covered in chemistry graduate programs.
We have presented this lecture series at The Scripps Research Institute, University of California San Diego, University of California Los Angeles & University of California Santa Barbara.
The seminar series received the ChemLuminary Award for the Outstanding or Creative Local Section Younger Chemists Committee Event at the 252nd ACS Fall National Meeting & Exposition in Philadelphia, Pennsylvania, August 2016.
TEACHING
MEDICINAL CHEMISTRY INTENSIVE COURSE
University of California, San Diego, CA, 2008
PHARMACOKINETICS AND PHARMACODYNAMICS: PRINCIPLES AND APPLICATIONS IN PRE-CLINICAL DRUG DEVELOPMENT
American Chemical Society, San Diego, CA, 2009
DRUG DEVELOPMENT AND NON-CLINICAL SAFETY EVALUATION OF DRUGS AND BIOLOGICS
Dr. Shayne Gad, San Diego, CA, 2010
DRUG-LIKE PROPERTIES: OPTIMIZING PHARMACOKINETICS AND SAFETY IN DRUG DISCOVERY
American Chemical Society, San Diego, CA, 2012
ACS LEADERSHIP INSTITUTE
American Chemical Society, Dallas, TX, 2015
COMBINED STATISTICAL TRAINING FOR BOTH NON-CLINICAL AND CLINICAL STUDIES
CfPIE, Al Bartolucci Ph.D., 2016
PROFESSIONAL DEVELOPMENT
PUBLISHED WORK
PATENTS
Therapeutic 5,6,5-Tricyclic Analogs; US 9,012,470 B2.
Gupta, Varsha; Renick, Joel; Freestone, Graeme C.; Kaplan, Alan P
Substituted Naphthyridine and Quinoline Compounds as MAO Inhibitors; US 9,102,674 B2.
Basinger, Jillian; Breitenbucher, James; Freestone, Graeme; Gupta, Varsha; Kaplan, Alan; Mak, Chi-Ching; Pratt, Benjamin; Santora, Vincent; Sengupta, Dipanjan; Valdez, Lino
Substituted [1,2,4] Triazolo [1,5-a] pyrimidin-7-yl Compounds as PDE2 Inhibitors; PCT Int. Appl. (2015), WO 2015/164508 A4. Breitenbucher, James; Freestone, Graeme; Gomez, Laurent; Lemus, Robert; Ly, Kiev; McCarrick, Margaret; Vernier, William; Vickers, Troy
PUBLICATIONS
Synthesis of Enantiopure Dihydropyranones: Aldol-Based Ring Expansion of Dihydrofurans, Org. Lett., 2002, 4, 3059. Donohoe, Timothy J.; Raoof, Ali; Freestone, Graeme C.; Linney, Ian D.; Cowley, Andrew; Helliwell, Madeleine
Enantioselective Partial Reduction of 2,5-Disubstituted Pyrroles via a Chiral Protonation Approach, Org. Lett., 2004, 6, 3055. Donohoe, Timothy J.; Freestone, Graeme C.; Headley, Catherine E.; Rigby, Caroline L.; Cousins, Rick P. C.; Bhalay, Gurdip
Synthesis of Highly Substituted N-Hydroxyindoles by 1,5-Addition of Carbon Nucleophiles to Unsaturated Nitrones, Angew. Chem. Int. Ed., 2006, 45, 32, 5364. Nicolaou, K. C.; Estrada Anthony, A.; Lee, Sang Hyup; Freestone, Graeme C.
New Synthetic Technology for the Construction of N-Hydroxyindoles and Synthesis of Nocathiacin I Model Systems, Tetrahedron, 2007, 63, 27, 6088. Nicolaou, K. C.; Estrada, Anthony A.; Freestone, Graeme C.; Lee, Sang Hyup; Alvarez-Mico, Xavier
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PRESENTATIONS
Synthesis of Enantiopure Dihydropyranones: Aldol-Based Ring Expansion of Dihydrofurans. 226th ACS National Meeting, New York, NY, 2003. ORGN 592. Freestone, Graeme C.; Donohoe, Timothy J. (poster)
Synthesis of Enantiopure Dihydropyranones: Aldol-Based Ring Expansion of Dihydrofurans. Pfizer Organic Chemistry Poster Symposium, London, United Kingdom, 2003. Freestone, Graeme C.; Donohoe, Timothy J. (poster)
Partial Reduction of Aromatic Heterocycles. Pfizer, Sandwich, United Kingdom, 2004. Freestone, Graeme C. (lecture)
Partial Reduction of Aromatic Heterocycles. The James Black Foundation, London, United Kingdom, 2004. Freestone, Graeme C. (lecture)
Identification of Pyrazolo-Pyrrolo Pyridines as Novel GABAA a5 Receptor Modulators. Gordon Research Conference on Medicinal Chemistry, New London, NH, 2011. Freestone, Graeme C.; Gupta, Varsha; Danks, Anne M.; Kaplan, Alan P.; Sugunan, Kavitha; Downing, Scott S.; Gibbs, Terrell T.; Farb, David H. (poster)
M.CHEM, UNIVERSITY OF MANCHESTER, UK
1997-2001
The four-year MChem programme places strong emphasis on theory and laboratory practice. The fundamentals of and advances in inorganic, organic and physical chemistry are taught, in addition to a substantial research project undertaken in the final year.
D.PHIL, UNIVERSITY OF OXFORD, UK
2001-2005
My doctorate research was performed in the laboratory of Prof. Timothy Donohoe. It was focused on the study of the Birch reduction, a particularly useful reaction in synthetic organic chemistry. The numerous novel findings from this research project have greatly advanced our view of this powerful reaction, which has been used to great effect in the synthesis of many natural product and drug-type compounds.
EDUCATION
ACADEMIC RESEARCH
THE SCRIPPS RESEARCH INSTITUTE, CA
Post-doctoral Research Associate, 2005-2007
My focus was to tackle the challenge of the total synthesis of the complex natural product nocathiacin I. Nocathiacin I is an antibiotic discovered during the course of screening for novel antibiotics in microbial fermentations from the culture broth of a strain of Nocardia sp. by a Bristol Myers Squibb team. The general structural characteristics of the complex polycyclic framework indicate that it belongs to the thiazolyl peptide class of antibiotics.
THE JAMES BLACK FOUNDATION, UK
Research Associate, 2004
The James Black Foundation was an institute established by Sir James Black with funding from Johnson and Johnson to engage in drug discovery. My focus there as a temporary research associate was to investigate and synthesize antagonists for the cholecystokinin (CCK1 and CCK2) and histamine (H3) receptor targets.
PROFESSIONAL EXPERIENCE
SCIENTIST 2, DART NEUROSCIENCE
2012 - Present
The rational design and synthesis of drug-like compounds for a range of enzymatic and ion channel targets in the central nervous system (CNS). These targets have demonstrated in validation assays the strong potential to produce therapies for diseases in which normal learning and memory is impaired, e.g. mild cognitive impairment, Alzheimer’s disease, Schizophrenia and Parkinson’s disease.
SCIENTIST 1, HELICON THERAPEUTICS
2009 - 2012
Helicon's therapeutic target population were sufferers of disorders of cognitive function including memory impairment from stroke or head trauma, age-related disorders of learning and memory, inherited forms of mental retardation and memory loss due to pathological conditions such as Alzheimer's disease. My focus was to discover small molecule therapeutics to treat disorders of cognition through an understanding of the genetic basis of long-term memory formation.
RESEARCH SCIENTIST, METABASIS THERAPEUTICS
2007 - 2009
The corporate focus of Metabasis Therapeutics was therapies to treat liver and metabolic diseases. On joining the company I became a member on the thyroid hormone receptor program, whose goal was to discover second-generation drug candidates for treatment of hyperlipidemia. Thyroid hormones play a critical role in growth, development, metabolism, and homeostasis.
