Ralph Robinson Email & Phone Number

Mystic, Connecticut

Founding member. Medicinal chemistry consulting in partnership with a team of former senior Pfizer scientists. Supported/supporting clients in areas including covalent inhibitor library design, SARS-CoV-2 Mpro inhibitors, PROTACs (and other bifunctional molecules), 3rd party asset assessment, SGLT2 inhibitors; patent evaluation, prodrug design, kinase inhibitor optimization, expert witness testimony.thamespharmapartners.com

Gales Ferry, Connecticut, United States

Medicinal Chemistry Group Leader, Inflammation, Immunology and Rare Diseases. Led a team of 3-7 B.S./M.S./Ph.D. organic chemists providing support for the synthesis, characterization and early scale-up of molecules designed against biological targets under the remit of the Inflammation, Immunology and Rare Diseases Research Unit.- Led the Synthesis team that made important contributions to the discovery and advancement of abrocitinib (Cibinqo), a JAK1 inhibitor approved in January 2022 for the treatment of atopic dermatitis.- Developed innovative routes to sulfonyl fluoride (SF)-bearing chemical biology probes used for establishing target occupancy in living cells. Generalized the work to develop a toolbox of “clickable” SF monomers that were applied to SF probe synthesis on several Pfizer projects.- Developed a short, highly convergent route to aminoquinoline-containing haemoglobin S modulators, greatly expanding the scope of available starting monomers. Adapted the route to a parallel chemistry format that produced milestone leads for the project.- Organized and chaired “Med. Chem. 101”, an annual 5-day class targeting newly hired Ph.D.’s in Synthesis.- Chair, Pfizer Medicinal Chemistry Chair Symposium 2013.

Groton, Connecticut

Research Project Leader, SGLT2 project, Cardiovascular and Metabolic Diseases. Led the multi-disciplinary and very successful SGLT2 project team from project inception to Proof-of-Mechanism in Phase 1 clinical trials. Communicated project strategy, hurdles, and resource needs to management. Directly supervised 4-5 B.S./M.S./Ph.D. chemists supporting the project.- Obtained support for the project by writing a proposal detailing chemistry opportunities and recommending a medicinal chemistry strategy.- With the team, delivered clinical candidate PF-04971729 (ertugliflozin). Championed the synthetically challenging, yet very successful sugar modification design strategy. Established structure-activity relationships that guided the strategy.- Achieved First Synthesis to Proof-of-Mechanism in just 17 months, a feat accomplished through innovative synthesis, early establishment of quantitative PK/PD relationships, aggressive attention to solid form development, well-informed risk taking, and combined commitments across lines to shave time from standard development timelines.- Oversaw submission of the ertugliflozin IND to the FDA. Ertugliflozin was approved by the US in December 2017 as is now marketed under the brand name Steglatro.

Groton, Connecticut, United States

Medicinal Chemistry Laboratory Head, Cardiovascular and Metabolic Diseases. Led a team of 2-3 B.S./M.S.-level chemists in designing and executing the synthesis of target molecules for the treatment of diabetes and obesity.- In collaboration with chemistry, biology and drug metabolism colleagues led a coordinated strategy to discover microsomal triglyceride transfer protein (MTP) inhibitor “soft drugs". Designed obesity candidate PF-02575799 and oversaw chemistry aspects of its preclinical development and advancement to Phase 1 clinical trials.- For the GPR119 receptor project, developed a conformational hypothesis to explain agonist vs. antagonist SAR. Used this to design a series of potent, conformationally restrained and highly novel diazatricyclodecane GPR119 agonists. These became key proprietary leads for the project.

Groton, Connecticut, United States

Laboratory Head, Inflammation Medicinal Chemistry. Led a team of 2-3 B.S./M.S.-level chemists in designing and executing the synthesis of target molecules for the treatment of inflammatory diseases.- Designed and synthesized CP-144477, a pre-clinical candidate prodrug related to the Phase 3 clinical candidate tenidap. Overcame significant challenges associated with prodrug stability and solubility.- Designed and synthesized two matrix metalloproteinase (MMP) clinical candidates for the treatment of osteoarthritis: CP-471358 and CP-599069. The former compound progressed to Phase 1 clinical trials.- In collaboration with Computational Medicinal Chemistry, employed structure-based drug design to design a series of novel, non-peptide-based MMP inhibitors with high potency and selectivity for MMP-13.- Cosponsor of the Dissociated Agonists of the Glucocorticoid Receptor (DAGR) project. Over two years, made significant advances toward the identification of drug-like molecules possessing candidate-quality pharmacological, ADME and physicochemical properties. The project was transferred to the Inflammation team at Pfizer, St. Louis, which successfully advanced the series into clinical trials, ultimately achieving POC in Phase 2.

Laboratory Head, CNS Medicinal Chemistry. Led a team of 2 B.S./M.S.-level chemists in designing and executing the synthesis of NMDA receptor antagonists for the treatment of cerebral ischemia and Alzheimer’s disease.- Developed a novel cationic rearrangement reaction that led to the discovery of highly potent non-competitive NMDA receptor antagonists.

Advisor: Prof. Lewis N. Mander. Established the feasibility of synthesizing the diterpenoid sordaricin via intramolecular Diels-Alder reaction. Developed a novel directed lithiation reaction for introduction of the isopropyl side chain. Completed synthesis of a fully functionalized sordaricin derivative.

Phd, Organic Chemistry

Thesis advisor: Prof. Harry H. Wasserman. Total synthesis of spermine and spermidine alkaloids via novel ring-expansion approaches. 1984.

Bsc, Chemistry, First Class Honours