Analogue-Based Drug Discovery III - download pdf or read online

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

ISBN-10: 3527330739

ISBN-13: 9783527330737

ISBN-10: 352765108X

ISBN-13: 9783527651085

Such a lot medications are analogue medicines. There are not any basic principles how a brand new drug may be stumbled on, however, there are a few observations which support to discover a brand new drug, and likewise anyone tale of a drug discovery can start up and aid new discoveries. quantity III is a continuation of the winning publication sequence with new examples of verified and lately brought medications.
the main a part of the e-book is written via key inventors both as a case learn or a research of an analogue type. With its wide selection 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 festival 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 issues (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 focusing 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 learn 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 creation Inhibitor: Febuxostat (pages 365–376): Ken Okamoto, Shiro Kondo and Takeshi Nishino

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J. (1985) Substituted fused imidazole compounds as aromatase inhibitors. European Patent Application EP 165904A2. F. (1985) Imidazo[1,5-a] pyridines: a new class of thromboxane A2 synthetase inhibitors. J. Med. , 28, 164. , and Dukes, M. (1994) Arimidex: a potent and selective fourth-generation aromatase inhibitor. Breast Cancer Res. , 30, 103–111. N. (2006) A partial view of the quest for Arimidex, a potent, selective inhibitor of aromatase, in Smith and Williams’ Introduction to the Principles of Drug Design and Action, 4th edn, CRC Press, Boca Raton, FL, pp.

Lancet, 2 (7251), 311–314. C. (1964) A new adrenergic beta-receptor antagonist. Lancet, 1 (7342), 1080–1081. , and Le Count, D. (1973) A new type of cardioselective adrenoceptive blocking drug. Br. J. , 48, 3408. , and Friderichs, E. (1978) Studies of chemical structure and analgetic activity of phenyl substituted aminomethylcyclohexanoles. , 28 (I), 107–113. , and Friderichs, F. (2001) 1-Phenyl-3dimethylaminopropane compounds with a pharmacological effect. EP 693 475. Schmutz, J. and Eichenberger, E.

3 Multitarget Drugs discovery of citalopram and its refinement to escitalopram is discussed in Chapter 11. H N CH3 O F3C fluoxetine 30 NC CH3 O N CH3 F citalopram 31 N CH3 O H3C diphenhydramine (lead for fluoxetine) 32 H3C CH3 O NHCH3 talopram (lead for citalopram) 33 Summary: Pioneer multitarget nonselective serotonin/norepinephrine reuptake inhibitor antidepressant drug: imipramine. First (but unsuccessful) selective serotonin reuptake inhibitor: zimelidine. First selective serotonin reuptake inhibitors: fluoxetine and citalopram.

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


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