Analogue-based Drug Discovery III

Most drugs are analogue drugs. There are no general rules how a new drug can be discovered, nevertheless, there are some observations which help to find a new drug, and also an individual story of a drug discovery can initiate and help new discoveries. Volume III is a continuation of the successful book series with new examples of established and recently introduced drugs. The major part of the book is written by key inventors either as a case study or a study of an analogue class. 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.Content: Chapter 1 Pioneer and Analogue Drugs (pages 1–19): Prof. Dr. Janos Fischer, Prof. Dr. C. Robin Ganellin and Prof. Dr. David P. RotellaChapter 2 Competition in the Pharmaceutical Drug Development (pages 21–35): Christian Tyrchan and Fabrizio GiordanettoChapter 3 Metabolic Stability and Analogue?Based Drug Discovery (pages 37–75): Amit S. Kalgutkar and Antonia F. StepanChapter 4 Use of Macrocycles in Drug Design Exemplified with Ulimorelin, a Potential Ghrelin Agonist for Gastrointestinal Motility Disorders (pages 77–110): Dr. Mark L. Peterson, Dr. Hamid Hoveyda, Dr. Graeme Fraser, Eric Marsault and Rene GagnonChapter 5 The Discovery of Anticancer Drugs Targeting Epigenetic Enzymes (pages 111–139): A. GanesanChapter 6 Thienopyridyl and Direct?Acting P2Y12 Receptor Antagonist Antiplatelet Drugs (pages 141–164): Dr. Joseph A. Jakubowski and Atsuhiro SugidachiChapter 7 Selective Estrogen Receptor Modulators (pages 165–185): Amarjit Luniwal, Rachael Jetson and Paul ErhardtChapter 8 Discovery of Nonpeptide Vasopressin V2 Receptor Antagonists (pages 187–209): Kazumi Kondo and Hidenori OgawaChapter 9 The Development of Cysteinyl Leukotriene Receptor Antagonists (pages 211–239): Peter R. BernsteinChapter 10 The Discovery of Dabigatran Etexilate (pages 241–267): Norbert Hauel, Andreas Clemens, Herbert Nar, Henning Priepke, Joanne van Ryn and Wolfgang WienenChapter 11 The Discovery of Citalopram and Its Refinement to Escitalopram (pages 269–294): Klaus P. Bogeso and Connie SanchezChapter 12 Tapentadol – From Morphine and Tramadol to the Discovery of Tapentadol (pages 295–318): Helmut BuschmannChapter 13 Novel Taxanes: Cabazitaxel Case Study (pages 319–341): Dr. Herve Bouchard, Dr. Dorothee Semiond, Dr. Marie?Laure Risse and Dr. Patricia VrignaudChapter 14 Discovery of Boceprevir and Narlaprevir: A Case Study for Role of Structure?Based Drug Design (pages 343–363): Srikanth Venkatraman, Andrew Prongay and George F. NjorogeChapter 15 A New?Generation Uric Acid Production Inhibitor: Febuxostat (pages 365–376): Ken Okamoto, Shiro Kondo and Takeshi Nishino Most Drugs Are Analogue Drugs. There Are No General Rules How A New Drug Can Be Discovered, Nevertheless, There Are Some Observations Which Help To Find A New Drug, And Also An Individual Story Of A Drug Discovery Can Initiate And Help New Discoveries. Volume Iii Is A Continuation Of The Successful Book Series With New Examples Of Established And Recently Introduced Drugs. The Major Part Of The Book Is Written By Key Inventors Either As A Case Study Or A Study Of An Analogue Class. With Its Wide Range Across A Variety Of Therapeutic Fields And Chemical Classes, This Is Of Interest To Virtu General Aspects. Pioneer And Analogue Drugs / Janos Fischer, C Robin Ganellin, David P Rotella -- Competition In The Pharmaceutical Drug Development / Christian Tyrchan, Fabrizio Giordanetto -- Metabolic Stability And Analogue-based Drug Discovery / Amit S Kalgutkar, Antonia F Stepan -- Use Of Macrocycles In Drug Design Exemplified With Ulimorelin, A Potential Ghrelin Agonist For Gastrointestinal Motility Disorders / Mark L Peterson, Hamid Hoveyda, Graeme Fraser, Eric Marsault, Rene Gagnon -- Drug Classes. The Discovery Of Anticancer Drugs Targeting Epigenetic Enzymes / A Ganesan -- Thienopyridyl And Direct-acting P2y Receptor Antagonist Antiplatelet Drugs / Joseph A Jakubowski, Atsuhiro Sugidachi -- Selective Estrogen Receptor Modulators / Amarjit Luniwal, Rachael Jetson, Paul Erhardt -- Discovery Of Nonpeptide Vasopressin V2 Receptor Antagonists / Kazumi Kondo, Hidenori Ogawa -- The Development Of Cysteinyl Leukotriene Receptor Antagonists / Peter R Bernstein -- Case Studies. The Discovery Of Dabigatran Etexilate / Norbert Hauel, Andreas Clemens, Herbert Nar, Henning Priepke, Joanne Van Ryn, Wolfgang Wienen -- The Discovery Of Citalopram And Its Refinement To Escitalopram / Klaus P Bogeso, Connie Sanchez -- Tapentadol : From Morphine And Tramadol To The Discovery Of Tapentadol / Helmut Buschmann -- Novel Taxanes: Cabazitaxel Case Study / Herve Bouchard, Dorothee Semiond, Marie-laure Risse, Patricia Vrignaud -- Discovery Of Boceprevir And Narlaprevir: A Case Study For Role Of Structure-based Drug Design / Srikanth Venkatraman, Andrew Prongay, George F Njoroge -- A New-generation Uric Acid Production Inhibitor: Febuxostat / Ken Okamoto, Shiro Kondo, Takeshi Nishino. Edited By Ja�1nos Fischer, C. Robin Ganellin, David P. Rotella. Includes Bibliographical References And Index. Mode Of Access: World Wide Web. Most drugs are analogue drugs. There are no general rules how a new drug can be discovered, nevertheless, there are some observations which help to find a new drug, and also an individual story of a drug discovery can initiate and help new discoveries. Volume 1 is the first authoritative overview of past and current strategies for successful drug development by analog generation, this unique resource spans all important drug classes and all major therapeutic fields, including histamine antagonists, ACE inhibitors, beta blockers, opioids, quinolone antibiotics, steroids and anticancer platinum compounds. Of the 19 analog classes presented in detail, 9 are described by the scientists who discoverd them. The book includes a table of the most successful drug analogs as based on the IMS ranking and compares them in terms of chemical structure, mode of action and patentability. Volume 2 was born out of a project of the IUPAC's committee on Medicinal Chemistry and Drug Development, this reference addresses past and current strategies for successful drug analog development, extending the previously published volume by nine new analog classes and eight case studies. Like its precursor, this volume also contains a general section discussing universally applicable strategies for analog discovery and development. Spanning a wide range of therapeutic fields and chemical classes, the two volumes together constitute the first systematic approach to drug analog development. Of interest to virtually every researcher working in drug discovery and pharmaceutical chemistry. Volume 3 is a continuation of the successful book series with new examples of established and recently introduced drugs. The major part of the book is written by key inventors either as a case study or a study of an analogue class. 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