Analogue-based Drug Discovery III

Officially endorsed by the IUPACs committee on Medicinal Chemistry and Drug Development, this reference continues the success of the two highly acclaimed volumes by the same editors, adding new chapters on general strategies, eight new analogue classes and seven new case studies. With its wide range across a variety of therapeutic fields and chemical classes, this is of interest to virtually every researcher in drug discovery and pharmaceutical chemistry, and -- together with the previous volumes -- constitutes the first systematic approach to drug analogue development.

J?nos Fischer is a Senior Research Scientist at Richter Plc., Budapest, Hungary. He received his MSc and PhD degrees in organic chemistry from the Eotvos University of Budapest under Professor A. Kucsman. Between 1976 and 1978, he was a Humboldt Fellow at the University of Bonn under Professor W. Steglich. He has worked at Richter Plc. since 1981 where he participated in the research and development of leading cardiovascular drugs in Hungary. His main interest is analogue based drug discovery. He is the author of some 100 patents and scientific publications. In 2004, he was elected as a Titular member of the Chemistry and Human Health Division of IUPAC. He received an honorary professorship at the Technical University of Budapest.

C. Robin Ganellin studied Chemistry at London University, receiving a PhD in 1958 under Professor Michael Dewar, and was a Research Associate at MIT with Arthur Cope in 1960. He then joined Smith Kline & French Laboratories in the UK and was one of the co inventors of the revolutionary drug, cimetidine (also known as Tagamet). In 1986, he was made a Fellow of the Royal Society and appointed to the SK&F Chair of Medicinal Chemistry at University College London, where he is now Professor Emeritus of Medicinal Chemistry. Professor Ganellin is co inventor of over 160 patents and has authored over 260 scientific publications. He was President of the Medicinal Chemistry Section of the IUPAC and is Chairman of the IUPAC Subcommittee on Medicinal Chemistry and Drug Development.

David Rotella is the Margaret and Herman Sokol Professor of Medicinal Chemistry at Montclair State University. He earned a B.S. Pharm. degree at the University of Pittsburgh (1981) and a Ph.D. (1985) at The Ohio State University with Donald. T. Witiak. After postdoctoral studies in organic chemistry at Penn State University with Ken S. Feldman, he was an assistant professor at the University of Mississippi. David worked at Cephalon, Bristol-Myers, Lexicon and Wyeth where he was involved in neurodegeneration, schizophrenia, cardiovascular and metabolic disease drug discovery projects.

PART I: GENERAL ASPECTS

1 Pioneer and Analogue Drugs
2 Competition in the pharmaceutical drug development
3 Metabolic Stability and Analogue-Based Drug Discovery
4 Use of Macrocycles in Drug Design Exemplified with Ulimorelin, a Potential Ghrelin Agonist for Gastrointestinal Motility Disorders

PART II: DRUG CLASSES
5 The Discovery of Anticancer Drugs Targeting Epigenetic Enzymes
6 Thienopyridyl and Direct Acting P2Y12 Receptor Antagonist Antiplatelet Drugs
7 Selective Estrogen Receptor Modulators
8 Discovery of non-peptide vasopressin V2 receptor antagonists
9 The Development of Cysteinyl-Leukotriene Receptor Antagonists

PART III: CASE STUDIES
10 The Discovery of Dabigatran Etexilate
11 The discovery of citalopram and its refinement to escitalopram
12 From Morphine and Tramadol to the Discovery of Tapentadol
13 Novel taxanes: Cabazitaxel case study
14 Discovery of Boceprevir and Narlaprevir. A case study for role of structure based drug design.
15 A new-generation uric acid production inhibitor: Febuxostat