Analogue-Based Drug Discovery III by Janos Fischer, C. Robin Ganellin, David P. Rotella PDF

By Janos Fischer, C. Robin Ganellin, David P. Rotella

ISBN-10: 3527330739

ISBN-13: 9783527330737

ISBN-10: 352765108X

ISBN-13: 9783527651085

So much medications are analogue medicinal drugs. There aren't any basic ideas how a brand new drug will be came across, however, there are a few observations which aid to discover a brand new drug, and likewise somebody tale of a drug discovery can start up and support new discoveries. quantity III is a continuation of the winning ebook sequence with new examples of tested and lately brought medicines.
the key a part of the publication is written through key inventors both as a case examine or a examine of an analogue type. With its wide variety throughout quite a few healing fields and chemical periods, this is often of curiosity to almost each researcher in drug discovery and pharmaceutical chemistry, and -- including the former volumes -- constitutes the 1st systematic method of drug analogue development.Content:
Chapter 1 Pioneer and Analogue medicinal drugs (pages 1–19): Prof. Dr. Janos Fischer, Prof. Dr. C. Robin Ganellin and Prof. Dr. David P. Rotella
Chapter 2 pageant within the Pharmaceutical Drug improvement (pages 21–35): Christian Tyrchan and Fabrizio Giordanetto
Chapter three Metabolic balance and Analogue?Based Drug Discovery (pages 37–75): Amit S. Kalgutkar and Antonia F. Stepan
Chapter four Use of Macrocycles in Drug layout Exemplified with Ulimorelin, a possible Ghrelin Agonist for Gastrointestinal Motility problems (pages 77–110): Dr. Mark L. Peterson, Dr. Hamid Hoveyda, Dr. Graeme Fraser, Eric Marsault and Rene Gagnon
Chapter five the invention of Anticancer medications concentrating on Epigenetic Enzymes (pages 111–139): A. Ganesan
Chapter 6 Thienopyridyl and Direct?Acting P2Y12 Receptor Antagonist Antiplatelet medications (pages 141–164): Dr. Joseph A. Jakubowski and Atsuhiro Sugidachi
Chapter 7 Selective Estrogen Receptor Modulators (pages 165–185): Amarjit Luniwal, Rachael Jetson and Paul Erhardt
Chapter eight Discovery of Nonpeptide Vasopressin V2 Receptor Antagonists (pages 187–209): Kazumi Kondo and Hidenori Ogawa
Chapter nine the advance of Cysteinyl Leukotriene Receptor Antagonists (pages 211–239): Peter R. Bernstein
Chapter 10 the invention of Dabigatran Etexilate (pages 241–267): Norbert Hauel, Andreas Clemens, Herbert Nar, Henning Priepke, Joanne van Ryn and Wolfgang Wienen
Chapter eleven the invention of Citalopram and Its Refinement to Escitalopram (pages 269–294): Klaus P. Bogeso and Connie Sanchez
Chapter 12 Tapentadol – From Morphine and Tramadol to the invention of Tapentadol (pages 295–318): Helmut Buschmann
Chapter thirteen Novel Taxanes: Cabazitaxel Case research (pages 319–341): Dr. Herve Bouchard, Dr. Dorothee Semiond, Dr. Marie?Laure Risse and Dr. Patricia Vrignaud
Chapter 14 Discovery of Boceprevir and Narlaprevir: A Case research for position of Structure?Based Drug layout (pages 343–363): Srikanth Venkatraman, Andrew Prongay and George F. Njoroge
Chapter 15 A New?Generation Uric Acid construction Inhibitor: Febuxostat (pages 365–376): Ken Okamoto, Shiro Kondo and Takeshi Nishino

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And Elg, M. (2003) The pharmacodynamics and pharmacokinetics of the oral direct thrombin inhibitor ximelagatran and its active metabolite melagatran: a mini-review. Thromb. , 109 (Suppl. 1), S9–S15. , Lewis, J. , and Shet, S. (2005) Hepatic findings in long-term clinical trials of ximelagatran. , 28 (4), 351–370. , and Wienen, W. (2002) Structure-based design of novel potent nonpeptide thrombin inhibitors. J. Med. , 45, 1757–1766. W. I. (2010) Update on antithrombotic therapy. New anticoagulants.

2003) Patinformatics: tasks to tools. , 25 (3), 211–221. W. and Bajorath, J. (2001) Differential Shannon entropy as a sensitive measure of differences in database variability of molecular descriptors. J. Chem. Inform. Comput. , 4, 1060–1066. com/ products/scitegic (accessed December 8, 2011). , and H€ogberg, T. (2010) Conversion of 4-cyanomethyl-pyrazole-3carboxamides into CB1 antagonists with lowered propensity to pass the blood– brain-barrier. Bioorg. Med. Chem. , 20, 453–457. , and Kunos, G.

Pharm. 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 worked as 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. 1 Introduction Granted patents give the right to exclude others from making, using, selling, offering for sale, or importing the claimed invention for a given time period that can vary between countries.

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Analogue-Based Drug Discovery III by Janos Fischer, C. Robin Ganellin, David P. Rotella


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