Modern Drug Synthesis

InhaltsangabePreface. Contributors. I. Infectious Diseases. Chapter 1. Raltegravir (Isentress), The First-in-class HIV-1 Integrase Inhibitor (Julianne A. Hunt). 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 (David Price). 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 (Arun K. Ghosh and Cuthbert D. Martyr). 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 (Jennifer A. Van Camp). 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 (R. Jason Herr). 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 Multi-kinase Inhibitor for Advanced Renal Cell Carcinoma and Unresectable Hepatocellular Carcinoma (Shuanghua Hu). 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 (Martin Pettersson). 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 (Benjamin S. Greener and David S. Millan). 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 (Ji Zhang and Jie Jack Li). 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 (Scott D. Edmondson, Feng Xu, and Joseph D. Armstrong III). 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 (Victor J. Cee). 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 (David L. Gray). 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 V1a and V2 Antagonist for Hyponatremia (Brian A. Lanman). 13.1 Background. 13.2 Pharmacology. 13.3 Structure-Activity Relationship (SAR). 13.4 Pharmacokinetics and Dr

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