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Bruce Roth

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Name
  
Bruce Roth

Education
  
Iowa State University

Role
  
Chemist

Awards
  
Perkin Medal


Bruce D. Roth (b. Jun 1954) is an American chemist who invented atorvastatin, better known as Lipitor, which has become the largest-selling drug in pharmaceutical history.

Contents

Education

Roth received his bachelor's degree from St. Joseph's College, Philadelphia, in 1976. He then went to Iowa State University as a doctoral student under George Kraus. After receiving his Ph.D. in organic chemistry from Iowa State University in 1981, he spent a year as a Postdoctoral Fellow at the University of Rochester.

Career

In 1982 28-year-old Roth was hired by Warner-Lambert. He was promoted to Senior Scientist in 1984. In 1985 he was at Warner-Lambert's Parke-Davis Pharmaceutical Research facility in Ann Arbor, Michigan.

He was promoted to Research Associate in 1986, Senior Research Associate in 1988, Section Director in 1990, Director of Atherosclerosis and Exploratory Chemistry in 1992, and Senior Director of Atherosclerosis, Inflammation and Exploratory Chemistry in 1993. By the early 1990s he held managerial positions and was no longer doing laboratory work. In 2000 Warner-Lambert acquired Parke-Davis. He was appointed Vice President of Chemistry just prior to the merger between Warner-Lambert and Pfizer in 2000 and remained in that role as a part of Pfizer Global Research and Development in Ann Arbor, Michigan until 2007. He then joined Genentech in San Francisco, California as Vice President of Discovery Chemistry.

Before atorvastatin, Roth worked to develop a different drug, but Sandoz AG beat his team to a patent.

Atorvastatin

In 1985 while working at Warner-Lambert's Parke-Davis research facility, Roth "identified a molecule" that inhibited HMG CoA reductase, a "key enzyme in the metabolic pathway the body uses to produce cholesterol."

Roth was listed as the inventor of Trans-6-[2-(3- or 4-carboxamido-substituted pyrrol-1-yl)alkyl]-4-hydroxypyran-2-one that was patented in 1986. It was transformed "into a viable drug, atorvastatin and sold under the brand name Lipitor." Pfizer acquired Warner-Lambert and Lipitor in 2000.

For the discovery, Roth received the 1997 Warner-Lambert Chairman's Distinguished Scientific Achievement Award, the 1999 Inventor of the Year Award from the New York Intellectual Property Law Association, the 2003 American Chemical Society Award for Creative Invention, the 2003 Gustavus John Esselen Award for Chemistry in the Public Service, the 2005 Iowa State University Distinguished Alumni Award, and the 2006 Pfizer Global Research and Development Achievement Award. Roth was named a 2008 Hero of Chemistry by the American Chemical Society. He also received the

Genentech

According to the Chemical Heritage Foundation, in "addition to his discovery of atorvastatin, Roth is the inventor or co-inventor of 42 patents and the author or co-author of 48 manuscripts, 35 published abstracts and eight book chapters."<! This phrase may have been copied from Wikipedia !> From 1996 until 2007, he served as an adjunct professor in the Department of Medicinal Chemistry at the University of Michigan.

Personal life

He and his wife, Michelle, have four children: David, Sarah, Rebecca and Aaron. David Roth was married on July 31, 2010, to Alyssa Roth, formerly Alyssa Dipzinski.

Publications

  • Baumann KL, Butler DE, Deering CF, Mennen KE, Millar A, Nanninga TN, Palmer CW, Roth BD. The convergent synthesis of CI-981, an optically active, highly potent, tissue selective inhibitor of HMG-CoA reductase. Tetrahedron Lett 1992; 33: 2283-4.
  • Brower PL, Butler DE, Deering CF, Le TV, Millar A, Nanninga TN, Roth BD. The synthesis of (4R-Cis)-1, 1-dimethylethyl, 6-cyanomethyl-2,2-dimethyl-1,3- dioxane-4-acetate, a key intermediate for the preparation of CI-981, a highly potent, tissue selective inhibitor of HMG-CoA reductase. Tetrahedron Lett 1992; 33: 2279-82.
  • Roth BD, Blankley CJ, Chucholowski AW, Ferguson E, Hoefle ML, Ortwine DF, Newton RS, Sekerke CS, Sliskovic DR, Stratton CD, et al. Inhibitors of cholesterol biosynthesis. 3. Tetrahydro-4-hydroxy-6-[2-(1H-pyrrol-1-yl)ethyl]-2H-pyran-2-one inhibitors of HMG-CoA reductase. 2. Effects of introducing substituents at positions three and four of the pyrrole nucleus. J Med Chem 1991 Jan; 34(1): 357-66.
  • Roth BD, Bocan TM, Blankley CJ, Chucholowski AW, Creger PL, Creswell MW, Ferguson E, Newton RS, O'Brien P, Picard JA, et al. Relationship between tissue selectivity and lipophilicity for inhibitors of HMG-CoA reductase. J Med Chem 1991 Jan; 34(1): 463-6.
  • Shaw MK, Newton RS, Sliskovic DR, Roth BD, Ferguson E, Krause BR. Hep-G2 cells and primary rat hepatocytes differ in their response to inhibitors of HMG-CoA reductase. Biochem Biophys Res Commun 1990 Jul 31; 170(2): 726-34.
  • Roth BD, Ortwine DF, Hoefle ML, Stratton CD, Sliskovic DR, Wilson MW, Newton RS. Inhibitors of cholesterol biosynthesis. 1. trans-6-(2-pyrrol-1-ylethyl)-4-hydroxypyran-2-ones, a novel series of HMG-CoA reductase inhibitors. 1. Effects of structural modifications at the 2- and 5-positions of the pyrrole nucleus. J Med Chem 1990 Jan; 33(1): 21-31.
  • Sliskovic DR, Roth BD, Wilson MW, Hoefle ML, Newton RS. Inhibitors of cholesterol biosynthesis. 2. 1,3,5-trisubstituted [2-(tetrahydro-4-hydroxy-2-oxopyran-6-yl)ethyl]pyrazoles. J Med Chem 1990 Jan; 33(1): 31-8.
  • Roth BD, Bocan TMA, Blankley CJ, Chucholowski AW, Creger PL, Creswell MW, Ferguson E, Newton RS, O'Brien P, Picard JA, Roark WH, Sekerke CS, Sliskovic DR, Wilson MW. The Relationship Between Tissue Selectivity and Lipophilicity for Inhibitors of HMG-CoA Reductase. J. Med. Chem. 1991, 34, 463-6.
  • Kende AS, Roth B, Sanfilippo PJ. Facile, palladium (II)- mediated synthesis of bridged and spirocyclic bicycloalkenones. J Am Chem Soc 1982; 104: 1784-5.
  • Kende AS, Roth B, Sanfilippo PJ, Blacklock TJ. Mechanism and regioisomeric control in palladium (II) - mediated cycloalkenylations. A novel total synthesis of (+/-)-quadrone. J Am Chem Soc 1982; 104: 5808-10.
  • Roth BD, Roark WH. Synthesis of a chiral synthon for the lactone portion of compactin and mevinolin. Tetrahedron Lett 1988; 29: 1255-8.
  • Roth, Bruce D. The Discovery and Development of Atorvastatin, a Potent Novel Hypolipidemic Agent, Progress in Medical Chemistry, 2002, pp. 1–22, vol. 40.

    • References

    Bruce Roth Wikipedia
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