Accounts in Drug Discovery: Case Studies in Medicinal Chemistry

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Joel Barrish, Christopher Barber
Royal Society of Chemistry, 2010 - Medical - 379 pages
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Accounts in Drug Discovery describes recent case studies in medicinal chemistry with a particular emphasis on how the inevitable problems that arise during any project can be surmounted or overcome. The Editors cover a wide range of therapeutic areas and medicinal chemistry strategies, including lead optimization starting from high-throughput screening "hits" as well as rational, structure-based design. The chapters include "follow-ons" and "next generation" compounds that aim to improve upon first-generation agents. This volume surveys the range of challenges commonly faced by medicinal chemistry researchers, including the optimization of metabolism and pharmacokinetics, toxicology, pharmaceutics and pharmacology, including proof-of-concept in the clinic for novel biological targets. The case studies include medicinal chemistry stories on recently approved and marketed drugs, but also chronicle "near-misses," i.e. exemplary compounds that may have proceeded well into the clinic but for various reasons did not result in a successful registration. As the vast majority of projects fail prior to registration, much can be learned from such narratives. By sharing a wide range of drug discovery experiences and information across the community of medicinal chemists in both industry and academia, the Editors believe that these accounts will provide insights into the art of medicinal chemistry as it is currently practiced and will help to serve the needs of active medicinal chemists.
 

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Contents

The Discovery of the Dipeptidyl Peptidase4 DPP4
1
References
20
RSC Drug Discovery Series No 4
51
The Discovery of OSI906 a Smallmolecule Inhibitor of
71
The Genesis of the Antibody Conjugate Gemtuzumab
103
Novel Androgen Receptor Antagonists for the Treatment
120
the Challenge of Targeting
142
The Discovery of the Longacting PDE5 Inhibitor PF489791
166
the Discovery and Development
183
Acknowledgements
208
The Discovery of GS9131 an Amidate Prodrug of
215
20F20CMethyl Nucleosides and Nucleotides for
238
Acknowledgements
263
Turning
287
Acknowledgements
311
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About the author (2010)

Joel C. Barrish was awarded his Ph.D. in Organic Chemistry from Columbia University; spent 25 years as a medicinal chemist in Drug Discovery Research; co-inventor of the anti-cancer agent SPRYCEL and is currently Vice President in Discovery Chemistry responsible for multiple programs across therapeutic areas. Percy H. Carter was awarded his Ph.D. in Organic Chemistry from Harvard University; 10 years as a medicinal chemist in Drug Discovery Research and is currently Group Director in Discovery Chemistry responsible for multiple programs Inflammation Research. Peter T. W. Cheng was awarded Ph.D. in Organic Chemistry from the University of Toronto; approximately 20 yrs as a medicinal chemist in Drug Discovery Research and is currently a Research Fellow in Metabolic Diseases Chemistry. Robert Zahler gained his Ph.D. in Organic Chemistry from the California Institute of Technology; approximately 30 yrs experience as a medicinal chemist in Drug Discovery Research and is the inventor of the anti-infective agent Entecavir.

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