Medicinal Chemist Consultant: Chemistry Leadership for Drug Discovery and Preclinical Development

Technical Consultant #1606


Expertise

  • Medicinal chemistry and target identification, preclinical lead compound development and small molecule drug discovery process.
  • Expansion and lead optimization for protein structure based and whole cell-based optimization of compounds in therapeutic areas of oncology, CNS, (Central Nervous System) and Inflammation.
  • Optimization for extra-cellular and intra-cellular molecular targets, e.g., GPCR's, CNS, and Kinases.
  • Experience with agonist of human neuronal nAChRs, GABA, BACE as an allosteric modulators with potential of better control of CNS process.
  • Discovery Team Leader for lead candidate RDEA-119, a potent and oral MEK Inhibitor (oncology) and HPP-854 & HPP-693 BACE inhibitors for CNS and Alzheimer's disease.
  • Processes in drug discovery and development in small biotechnology companies and large global pharmaceuticals.
  • Drug discovery programs including therapeutic areas of Oncology, CNS, and Inflammation.
  • Modern techniques in drug design including High Throughput Synthesis, risk analysis of combinatorial libraries, pharmacophore mapping, biomarker and relevant computational methods.
  • Library design and structure-based rational design.
  • Intellectual property strategic planning and management, process development for large scale synthesis.
  • Pharmaceutical chemistry outsource management and CRO protocols.
  • Process development.

Experience

Undisclosed Firm, 2006 - Present

Associate Director and Head of BACE-1 & AMPK Programs

  • Design and delivered a potent and selective preclinical candidate BACE-1 Inhibitor.
  • Oral administration of BACE-1 Inhibitor that inhibited cleavage of APP and lowered brain ą β -40 and ą β -42 in APP transgenic mice.
  • HPP-854 is currently being evaluated in a Phase 1 clinical trial.
  • Selected a hit as an AMPK activator. Lead compounds evaluated in proof-of-concept studies designed to test a series of compounds.

Valeant Pharmaceuticals International, Aliso Viejo, CA, Principal Scientist, Head of Oncology Chemistry, 2002 - 2006

  • Bayer Heathcare and Ardea Bioscience (Valeant International Inc.) entered into global agreement, focused on the development of RDA119 as MEK Inhibitors for treatment of cancer.
  • Design and delivered RDA119 as MEK inhibitor. RDA119 candidate is currently being evaluated in a Phase 1/2 clinical trial in both as a single agent and in combination with Nexavar® (sorafenib) in advanced cancer patients.
  • RDA119 is a potent, non-ATP competitive, highly-selective inhibitor of MEK, which is believed to play an important role in cancer cell proliferation, apoptosis and metastasis.
  • Studied inhibiting MEK signaling which has promise inhibiting RAS/RAF/MEK/ERK signaling pathways which are closely associated with the development of human tumors, such as melanoma, colon, lung and thyroid cancers.

Merck Research Lab., Research Senior Fellow, Head of CNS Program, 1996 - 2002

  • Discover and develop new classes of potent and selective orally active nicotinic receptors agonists targeted at neurodegenerative diseases such as Parkinson's and Alzheimer's. One compound from this work SIB-1553A has now completed Phase II clinical trials and is being developed in collaboration with Lilly Pharmaceuticals Co.
  • SIB-1553A is a novel agonist of human neuronal nAChRs, the neuronal acetylcholine ion channel receptors, which have therapeutic potential for the symptomatic treatment of Alzheimer's disease and other cognitive disorders.

Aventis Pharmaceutical Company, Hoechst Marion Roussel Research Institute Strasbourg Center, Post-Doctoral Fellow, 1994 - 1996

  • Designed and synthesized of new selective class of gamma aminobutyric acid-B (GABA-B) antagonists as potential new drugs.
  • Developed new synthetic approaches for phosphoamine acid derivative analogs of Baclofen.
  • Synthesize of 3 orally active low nanomolar small molecules receptor antagonists of GABA-B (MDL: 76,937A; 76,066A; 76,028A).
  • These molecules interact selectively with GABA-B receptors with high affinity.
  • Their interactions with GABA-A were much weaker, and were absent with other types of receptors (e.g., NMDA, quisqualate, kainite,benziazepine, muscarinic cholinergic, serotoninergic and histaminergic receptors).
  • MDL 76,028A has a good psycopharmacology profile, and attenuates the disruptive effect of baclofen on the motor system in the rotarod test.

Honors & Publications

Academic and Professional Affiliations

  • American Chemical Society
  • French Chemical Society
  • Scientific Council of the Faculty of Pharmacy, University of Louis Pasteur, Strasbourg, France.

Honors

  • SmithKline & Beecham Pharmaceutical Research Award

Publications and Patents

  • Sole or co-inventor of over 15 patents issued in the United States.
  • Published over 12 peer-reviewed articles.

Education

  • Ph.D. Bioorganic Chemistry, Louis Pasteur University, Strasbourg, France
  • M.S. Organic Chemistry, Louis Pasteur University
  • B.S. Organic Chemistry, Mineral & Analytical Chemistry, Louis Pasteur University
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