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Author Li, Jie Jack
Title Modern Drug Synthesis
Imprint Hoboken : Wiley, 2010
©2010
book jacket
Edition 1st ed
Descript 1 online resource (372 pages)
text txt rdacontent
computer c rdamedia
online resource cr rdacarrier
Series Wiley Series on Drug Synthesis
Wiley Series on Drug Synthesis
Note Intro -- Modern Drug Synthesis -- Contents -- Preface -- Contributors -- I. Infectious Diseases -- Chapter 1. Raltegravir (Isentress): The First-in-Class HIV-1 Integrase Inhibitor -- 1.1 Background -- 1.2 Pharmacology -- 1.3 Structure-Activity Relationship (SAR) -- 1.4 Pharmacokinetics and Drug Metabolism -- 1.5 Efficacy and Safety -- 1.6 Syntheses -- 1.7 References -- Chapter 2. Maraviroc (Selzentry): The First-in-Class CCR5 Antagonist for the Treatment of HIV -- 2.1 Background -- 2.2 Structure-Activity Relationship (SAR) -- 2.3 Pharmacokinetics and Safety -- 2.4 Syntheses -- 2.5 References -- Chapter 3. Darunavir (Prezista): A HIV-1 Protease Inhibitor for Treatment of Multidrug Resistant HIV -- 3.1 Background -- 3.2 Pharmacology -- 3.3 Structure-Activity Relationship (SAR) -- 3.4 Pharmacokinetics and Drug Metabolism -- 3.5 Efficacy and Safety -- 3.6 Syntheses -- 3.7 References -- II. Cancer -- Chapter 4. Decitabine (Dacogen): A DNA Methyltransferase Inhibitor for Cancer -- 4.1 Background -- 4.2 Pharmacology -- 4.3 Structure-Activity Relationship (SAR) -- 4.4 Pharmacokinetics and Drug Metabolism -- 4.5 Efficacy and Safety -- 4.6 Syntheses -- 4.7 References -- Chapter 5. Capecitabine (Xeloda): An Oral Chemotherapy Agent -- 5.1 Background -- 5.2 Pharmacology -- 5.3 Structure-Activity Relationship (SAR) -- 5.4 Pharmacokinetics and Efficacy -- 5.5 Syntheses -- 5.6 References -- Chapter 6. Sorafenib (Nexavar): A Multikinase Inhibitor for Advanced Renal Cell Carcinoma and Unresectable Hepatocellular Carcinoma -- 6.1 Background -- 6.2 Pharmacology -- 6.3 Structure-Activity Relationship (SAR) -- 6.4 Pharmacokinetics and Drug Metabolism -- 6.5 Efficacy and Safety -- 6.6 Syntheses -- 6.7 References -- Chapter 7. Sunitinib (Sutent): An Angiogenesis Inhibitor -- 7.1 Background -- 7.2 Discovery and Development -- 7.3 Syntheses -- 7.3.1 Discovery Route
7.3.2 Process Route -- 7.4 References -- Chapter 8. Bortezomib (Velcade): A First-in-Class Proteasome Inhibitor -- 8.1 Background -- 8.2 Pharmacology -- 8.3 Structure-Activity Relationship (SAR) -- 8.4 Pharmacokinetics and Drug Metabolism -- 8.5 Efficacy and Safety -- 8.6 Syntheses -- 8.7 References -- Chapter 9. Pazopanib (Votrient): A VEGFR Tyrosine Kinase Inhibitor for Cancer -- 9.1 Background -- 9.2 Pharmacology -- 9.3 Structure-Activity Relationship (SAR) -- 9.4 Pharmacokinetics and Drug Metabolism -- 9.5 Efficacy and Safety -- 9.6 Syntheses -- 9.7 Other VEGFR Inhibitors in Development: Vandetanib and Cediranib -- 9.8 References -- III. Cardiovascular and Metabolic Diseases -- Chapter 10. Sitagliptin (Januvia): A Treatment for Type 2 Diabetes -- 10.1 Background -- 10.2 Pharmacology -- 10.3 Structure-Activity Relationship (SAR) -- 10.4 Pharmacokinetics and Drug Metabolism -- 10.5 Efficacy and Safety -- 10.6 Syntheses -- 10.7 References -- Chapter 11. Aliskiren (Tekturna), The First-in-Class Renin Inhibitor for Hypertension -- 11.1 Background -- 11.2 Pharmacology -- 11.3 Structure-Activity Relationship (SAR) -- 11.4 Pharmacokinetics and Drug Metabolism -- 11.5 Efficacy and Safety -- 11.6 Syntheses -- 11.7 References -- Chapter 12. Vernakalant (Kynapid): An Investigational Drug for the Treatment of Atrial Fibrillation -- 12.1 Background -- 12.2 Pharmacology -- 12.3 Structure-Activity Relationship (SAR) -- 12.4 Pharmacokinetics and Drug Metabolism -- 12.5 Efficacy and Safety -- 12.6 Syntheses -- 12.7 References -- Chapter 13. Conivaptan (Vaprisol), Vasopressin Via and V2 Antagonist for Hyponatremia -- 13.1 Background -- 13.2 Pharmacology -- 13.3 Structure-Activity Relationship (SAR) -- 13.4 Pharmacokinetics and Drug Metabolism -- 13.5 Efficacy and Safety -- 13.6 Syntheses -- 13.7 References
Chapter 14. Rivaroxaban (Xarelto): A Factor Xa Inhibitor for the Treatment of Thrombotic Events -- 14.1 Background -- 14.2 Pharmacology -- 14.3 Structure-Activity Relationship (SAR) -- 14.4 Pharmacokinetics and Drug Metabolism -- 14.5 Efficacy and Safety -- 14.6 Syntheses -- 14.7 Compounds in Development: Apixaban and Otamixaban -- 14.8 References -- Chapter 15. Endothelin Antagonists for the Treatment of Pulmonary Arterial Hypertension -- 15.1 Background -- 15.2 Treatment of PAH -- 15.3 Endothelin Antagonists -- 15.4 Synthesis of Bosentan -- 15.5 Synthesis of Sitaxsentan -- 15.6 Synthesis of Ambrisentan -- 15.7 Conclusion -- 15.8 References -- III. Central Nervous System Diseases -- Chapter 16. Varenicline (Chantix), An α4β2 Nicotinic Receptor Partial Agonist for Smoking Cessation -- 16.1 Background -- 16.2 Discovery Chemistry Program -- 16.3 Pharmacology -- 16.4 Pharmacokinetics and Drug Metabolism -- 16.5 Efficacy and Safety -- 16.6 Syntheses -- 16.7 References -- Chapter 17. Donepezil, Rivastigmine, and Galantamine: Cholinesterase Inhibitors for Alzheimer Disease -- 17.1 Background -- 17.2 Pharmacology -- 17.3 Structure-Activity Relationship (SAR) -- 17.4 Pharmacokinetics and Drug Metabolism -- 17.5 Efficacy and Safety -- 17.6 Synthesis of Donepezil -- 17.7 Synthesis of Rivastigmine -- 17.8 Synthesis of Galantamine -- 17.9 References -- Chapter 18. Aprepitant (Emend): A NK1 Receptor Antagonist for the Treatment of Postchemotherapy Emesis -- 18.1 Background -- 18.2 In Vitro Pharmacology and Structure-Activity Relationships -- 18.3 In Vivo Pharmacology -- 18.4 Pharmacokinetics and Drug Metabolism -- 18.5 Efficacy and Safety -- 18.6 Syntheses -- 18.7 References -- Chapter 19. Armodafinil (Nuvigil): A Psychostimulant for the Treatment of Narcolepsy -- 19.1 Background -- 19.2 Pharmacology -- 19.3 Pharmacokinetics and Drug Metabolism
19.4 Efficacy and Safety -- 19.5 Synthesis -- 19.6 References -- V. Miscellaneous -- Chapter 20. Raloxifene (Evista): A Selective Estrogen Receptor Modulator (SERM) -- 20.1 Background -- 20.2 Mechanism of Action -- 20.3 Pharmacokinetics and Drug Metabolism -- 20.4 Efficacy and Safety -- 20.5 Syntheses -- 20.6 References -- Chapter 21. Latanoprost (Xalatan): A Prostanoid FP Agonist for Glaucoma -- 21.1 Background -- 21.2 Syntheses -- 21.3 References -- Index
Following Contemporary Drug Synthesis and The Art of Drug Synthesis (Wiley, 2004 and 2007), two well-received works, is this new book that demystifies the process of modern drug discovery for practitioners and students. An enhanced introduction covers areas such as background, pharmacology, SAR, PK/PD, efficacy, and safety. Focusing on the advantages of process synthesis versus the discovery synthetic route, Modern Drug Synthesis features authoritative coverage by distinguished editors and authors (some chapter authors are the actual inventor of the drug) of twenty different drug molecules
Description based on publisher supplied metadata and other sources
Electronic reproduction. Ann Arbor, Michigan : ProQuest Ebook Central, 2020. Available via World Wide Web. Access may be limited to ProQuest Ebook Central affiliated libraries
Link Print version: Li, Jie Jack Modern Drug Synthesis Hoboken : Wiley,c2010 9780470525838
Subject Drugs -- Design.;Pharmaceutical chemistry.;Electronic books
Electronic books
Alt Author Johnson, Douglas S
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