Cv2 Michael D Johnson


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Cv2 Michael D Johnson

  1. 1. Michael D. Johnson 4776 Del Mar Ave, San Diego, CA 92107 760-815-0508 Objective To contribute strong laboratory skills and experience as a synthetic chemist to a dynamic pharmaceutical research organization. Professional • 10 years drug discovery experience as medicinal chemist with over 300 novel compounds synthesized. Profile • Goal-oriented, dedicated scientist with a “can-do” attitude and proven adaptability to change. • Organized, proactive and attentive to detail. • Exceptionally resourceful and skilled at troubleshooting and problem solving. • Proven ability to work independently for extended periods of time. • Strong written and verbal communication skills, able to coordinate with different disciplines and work effectively within a multi-departmental, teamwork matrix. Education Bachelor of Science, Chemistry, University of California at San Diego 1996 • Course work emphasis on Organic Chemistry and laboratory skills. • Completed 1 year independent undergraduate research in Natural Products Chemistry. Employment & Senior Associate Scientist, Medicinal Chemistry, Pfizer La Jolla 2001-2007 * Selected • Solved the over-acylation problem plaguing a pre-divergent step in the synthesis Achievements of a key PKC-β project compound series. The yield was improved from <15% to >80%, resulting in the project’s first picomolar compound. The improved yield was routinely reproduced by other project chemists, leading to a dramatic overall increase in the number of compounds being made. • Accelerated the scale-up of a CAI final target by reducing the time required for reductive amination from 1 week to 2 days while avoiding formation of dimerized side products. Also identified the need for plug filtration of an intermediate in order to obtain a good yield from subsequent chlorosulfonylation. • Resolved a problematic step in a synthesis involving N-arylation via copper acetate catalysis. Used SciFinder to perform extensive literature search and discovered better method using Buchwald-type amido-arylation and improved the yield from 12% to over 85% on this and several other target analogs. • Championed the use of new technologies, such as solid phase extraction techniques, when synthesizing multi-gram quantities of intermediates for the CAI project. Because these non-commercially available compounds were hydrophilic and air-sensitive, implementation of SPE produced a higher recovery of cleaner material in less time. A key thienopyridinol intermediate was delivered 2 days ahead of schedule with 25% more material than expected. • Optimized reaction conditions and purification methods for several key intermediates in need of scale-up. Provided clear and concise data package, including consultation support, to the CRO chemists contracted for the synthesis. • Instrumental in the success of exploratory chemistry efforts. Notably, chemistry with little to no literature precedence, such as alpha-keto fluorination, and highly substrate-dependant reactions, such as indazole sulfonylation. • Evaluated, then successfully lobbied for installation of 2 minute columns in all LC/MS machines, reducing analysis turnaround time by 50% department-wide. • Utilized a nearly discarded Waters HPLC, reconfiguring it with an unused, prep- scale column capable of injections of over 1 gram. Enabled chemists access to HPLC purification on a scale never before available in the department.
  2. 2. Research Assistant I, Assistant Scientist II, Medicinal Chemistry, Agouron 1997-2001 Pharmaceuticals (a Pfizer company) • Received 2001 Employee Recognition Award for “superb contributions to a leading series in the CHK-1 project and lending a great helping hand to others.” • Synthesized a benchmark CHK-1 compound and later scaled it up to produce the 1.4 g needed for dog pharmacokinetic study. By quickly developing an ideal HPLC method and making efficient use of autosampling, purification took less than 5 days, despite limits in injection size and overcrowded lyophilizers. • Designed a set of analogs with different, small amines to produce a series of CHK-1 compounds wherein the enzyme potency improved from nanomolar to picomolar. • Isolated and identified an unexpected side-product which led to the most potent and efficacious series of compounds in the GLP-1 project. • Worked completely independently for 4 months while supervisor was on extended leave. Trained and supervised temp assistant during this period. • Synthesized multi-gram quantities of templates for use in library production and CCT support. • Trained colleagues in the use of analytical and prepatory HPLC and provided guidance for method development. *Adaptation to scale resulted in massive lay-offs at Pfizer. After separation in Sept., 2007, a six month vacation was taken. Henceforth, a continuous and focused effort has been underway to find a quality, permanent position in San Diego where my expertise and experience can be utilized. Technical Skills • Bruker Avance DRX300 and DRX400 NMR • Agilent Series 1100 LC/MS • Agilent Series 1100 HPLC • Dionex preparative HPLC • Waters PrepLC4000 HPLC • Waters 2690 Analytical HPLC • Isco Companion Flash Chromatography System • Analogix Flash Chromatography System • Biotage Flash Chromatography System • Personal Chemistry SmithSynthesizer Microwave • Parr Shaker Hydrogenation Apparatus • Custom built high vacuum manifold system • Electrothermal Mel-Temp • ThermoQuest Finnigan LCQ Duo LC/MS • Finnigan MAT GCQ GC/MS • Perkin Elmer Spectrum BX FT-IR • ACD Labs, HP Chemstation, Chromeleon™ and Millennium™ • ChemDraw, ISIS Draw/Base, QuikVu (3-D molecular modeling) • SciFinder, Beilstein • Rgate, Spotfire • Excel, Word, PowerPoint, Outlook, PC/Windows based systems
  3. 3. Patents • Aminopyrazole Compounds and Use as CHK1 Inhibitors Johnson, Michael David; Teng, Min; Zhu, Jinjiang. WO2005009435 A1 (2005-02-03). • Glucagon Antagonists/Inverse Agonists Anthony Ling, Atsuo Kuki, Shenghua Shi, Michael Bruno Plewe, Jun Feng, Larry Kenneth Truesdale, John May, Dan Kiel, Min Teng, Michael David Johnson, Lars Naerum, Peter Madsen, Christian Sams, Jesper Lau, Ulla Grove Sidelmann, Lotte Bjerre Knudsen. US 6613942 B1 (2003-09-02). • Non-Peptide Antagonist of GLP-1 Receptor and Methods of Use Larry Truesdale, Rick Bychowski, Javier Gonzalez, Atsuo Kuki, Ranjan Rajapakse, Min Teng, Dan Kiel, Dale Dhanoa, Yu-Feng Hong, Tso-Sheng Cho, Anthony Ling, Michael Johnson, Vlad Gregor. WO0033839, US 6,469,021 (2002-10-22). • Indazole Compounds and Pharmaceutical Compositions for Inhibiting Protein Kinases and Method for Their Use Robert Kania, Steven Bender, Allen Borchardt, John Brangaza, Stephan Cripps, Ye Hua, Michael Johnson, Ted Johnson, Hiep Luu, Cynthia Palmer, Siefgried Reich, Min Teng, Christine Thomas, Michael Varney, Michael Wallace. U. S. Patent Application No. 09/609,335, PCT Int. Appl. (2001), WO002369. • Preparation of Quinoxalines as Non-Peptide GLP-1 Agonists Teng, Min; Truesdale, Larry Kenneth; Bhumralkar, Dilip; Kiel, Dan; Johnson, Michael D.; Thomas, Christine; Jorgensen, Anker Steen; Madsen, Peter; Olesen, Preben Houlberg; Knudsen, Liselotte Bjerre; Petterson, Ingrid Vivika; Cornelis De Jong, Johannes; Behrens, Carsten; Kodra, Janos Tibor; Lau, Jesper. PCT Int. Appl. (2000), WO042026. • Preparation of β-Carbolines as Non-Peptide Antagonists of GLP-1 Receptor Truesdale, Larry Kenneth; Bychowski, Richard A.; Gonzalez, Javier; Kuki, Atsuo; Rajapakse, Ranjan Jagath; Teng, Min; Kiel, Dan; Dhanoa, Daljit S.; Hong, Yufeng; Chou, Tso-Sheng; Ling, Anthony L.; Johnson, Michael David; Gregor, Vlad Edward. PCT Int. Appl. (2000), WO033839. • Preparation of Aroylhydrazones as Glucagon Antagonists/Inverse Agonists Gonzales, Javier; Sams, Christian; Teng, Min; Ling, Anthony; Gregor, Vlad; Hong, Yufeng; Kiel, Dan; Kuki, Atsuo; Shi, Shenghua; Naerum, Lars; Madsen, Peter; Lau, Jesper; Plewe, Michael Bruno; Feng, Jun; Johnson, Michael David; Teston, Kimberly Ann; Sidelmann, Ulla Grove; Knudsen, Lotte Bjerre. PCT Int. Appl. (1999), WO9901423. Publications • Structure-Based Design and Synthesis of (5-Arylamino-2H-pyrazol-3-yl)-biphenyl-2',4'- diols as Novel and Potent Human CHK1 Inhibitors Min Teng, Jinjiang Zhu, Michael D. Johnson, Ping Chen, Jill Kornmann, Enhong Chen, Alessandra Blasina, James Register, Kenna Anderes, Caroline Rogers, Yali Deng, Sacha Ninkovic, Stephan Grant, Qiyue Hu, Karen Lundgren, Zhengwei Peng, and Robert S. Kania. Journal of Medicinal Chemistry, 2007, 50, (22), pp 5253-5256. • Small Molecule ago-Allosteric Modulators of the Human Glucagon-Like Peptide-1 (hGLP-1) Receptor Min Teng, Michael D. Johnson, Christine Thomas, Dan Kiel, James N. Lakis, Tim Kercher, Shelley Aytes, Jarek Kostrowicki, Dilip Bhumralkar, Larry Truesdale, John May, Ulla Sidelman, Janos T. Kodra, Anker Steen Jørgensen, Preben Houlberg Olesen, Johannes Cornelis de Jong, Peter Madsen, Carsten Behrens, Ingrid Pettersson, Lotte Bjerre Knudsen et al. Bioorganic and Medicinal Chemistry Letters, 2007, 17, (19), pp 5472-5478. • Small Molecule Agonists for the Glucagon-Like Peptide 1 Receptor Lotte Bjerre Knudnes, Dan Kiel, Min Teng, Carsten Behrens, Dilip Bhumralkar, Ja’nos T. Kodra, Jens J. Holst, Claus B. Jeppesen, Michael D. Johnson, Johannes Cornelis de Jong, Anker Steen Jorgensen, Tim Kercher, Jarek Kostrowicki, Peter Madsen, Preben H. Olesen, Jacob S. Petersen, Fritz Poulsen, Ulla G. Sidelmann, Jeppe Sturis, Larry Truesdale, John May, Jesper Lau. Proceedings of the National Academy of Sciences of the United States of America, 2007, 104, (3), pp 937-942. • Identification and Characterization of 6-Amido Indazoles as Novel Potent and Selective Check Point Kinase (CHK1) Inhibitors Min Teng, Michael D. Johnson, James Register, Ping Chen, Alessandra Blasina, Jill Kornmann. Bioorganic and Medicinal Chemistry Letters (submitted Feb 2007).
  4. 4. • Optimization of Alkylidene Hydrazide Based Human Glucagon Receptor Antagonists. Discovery of the Highly Potent and Orally Available 3-cyano-4-hydroxybenzoic Acid [1-(2,3,5,6- Tetramethylbenzyl)-1H-indol-4-ylmethylene]hydrazide Peter Madsen, Anthony Ling, Michael Plewe, Christian K. Sams, Lotte B. Knudsen, Ulla G. Sidelmann, Lars Ynddal, Christian L. Brand, Birgitte Andersen, Doug Murphy, Min Teng, Larry Truesdale, Dan Kiel, John May, Atsuo Kuki, Shenghua Shi, Michael D. Johnson, Kimberly Ann Teston, Jun Feng, James Lakis, Kenna Anderes, Vlad Gregor, and Jesper Lau Journal of Medicinal Chemistry, 2002, 45, (26), pp 5755-5775. • Alkylidene Hydrazides as Potent Human Glucagon Receptor Antagonists: Further Structure- Activity Relationships and In Vivo Studies (Oral Presentation) Peter Madsen, Jesper Lau, Christian K. Sams, Lotte B. Knudsen, Ulla G. Sidelmann, Lars Ynddal, Christian L. Brand, Anthony Ling, Vlad Gregor, Dan Kiel, Michael Plewe, Atsuo Kuki, Shenghua Shi, Jun Feng, Min Teng, Michael D. Johnson, Kimberly Teston, Doug Murphy, Kenna Anderes. Abstracts of Papers, 220th ACS National Meeting, Washington, DC, United States, August 20-24, 2000, MEDI-167.