Drug Synthesis Book Set

Jie Jack Li is an Associate Professor of chemistry at the University of San Francisco. Previously, he was a chemist at Bristol-Myers Squibb Company. He has authored or edited several books published by Wiley, including Drug Discovery: Practices, Processes, and Perspectives, Heterocyclic Chemistry in Drug Discovery, Name Reactions in Heterocyclic Chemistry, Name Reactions for Functional Group Transformations, Contemporary Drug Synthesis, The Art of Drug Synthesis, and Modern Drug Synthesis. Douglas Johnson is an Associate Research Fellow and head of Chemical Biology in the Neuroscience Medicinal Chemistry group at Pfizer Worldwide Research and Development. He is a co-author on more than 70 publications and patents and is a co-author of the book Contemporary Drug Synthesis and is an editor of The Art of Drug Synthesis, and Modern Drug Synthesis (all published by Wiley).

Contemporary Drug Synthesis Preface v Trade Names and Their Corresponding USANs xi Acronyms and Abbreviations xiii Chapter 1. Antithrombotics: Ticlopidine (Ticlid) and Clopidogrel (Plavix) 1 Chapter 2. Anti-inflammatory Cyclooxygenase-2 Selective Inhibitors: Celecoxib (Celebrex) and Rofecoxib (Vioxx) 11 Chapter 3. H+/K+ -ATPase Inhibitors: Esomeprazole (Nexium) 21 Chapter 4. Protein-tyrosine Kinase Inhibitors: Imatnib (Gleevec) and Gefitinib (Iressa) 29 Chapter 5. Non-sedating Antihistamines 39 Chapter 6. Cosmeceuticals: Istretinoin (Accutane), Tazarotene (Tazorac), Minoxidil (Rogaine), and Finasteride (Propecia) 55 Chapter 7. Antibacterials: Ciprofloxacin (Cipro) and Linezolid (Zyvox) 75 Chapter 8. Atypical Antupsychotics 89 Chapter 9. Atovastatin Calcium (Lipitor) 113 Chapter 10. Antidepressants 125 Chapter 11. Anti-obesity: Orlistat (Xenical) 149 Chapter 12. Triptans for Migrane 161 Chapter 13. PDE 5 Inhibitors for Erectile Dysfunction: Sildenafil (Viagra), Vardenafil (Levitra), and Tadalafil (Cialis) 189 Chapter 14. Antiasthmatics 201 Index 214 The Art of Drug Synthesis 1 THE ROLE OF MEDICINAL CHEMISTRY IN DRUG DISCOVERY 1 John A. Lowe, III 2 PROCESS RESEARCH: HOW MUCH? HOW SOON? 11 Neal G. Anderson 3 AROMATASE INHIBITORS FOR BREAST CANCER: EXEMESTANE (AROMASIN), ANASTROZOLE (ARIMIDEX), AND LETROZOLE (FEMARA) 31 Jie Jack Li 4 QUINOLONE ANTIBIOTICS: LEVOFLOXACIN (LEVAQUIN), MOXIFLOXACIN (AVELOX), GEMIFLOXACIN (FACTIVE), AND GARENOXACIN (T-3811) 39 Chris Limberakis 5 TRIAZOLE ANTIFUNGALS: ITRACONAZOLE (SPORANOX), FLUCONAZOLE (DIFLUCAN), VORICONAZOLE (VFEND), AND FOSFLUCONAZOLE (PRODIF) 71 Andrew S. Bell 6 NON-NUCLEOSIDE HIV REVERSE TRANSCRIPTASE INHIBITORS 83 Arthur Harms 7 NEURAMINIDASE INHIBITORS FOR INFLUENZA: OSELTAMIVIR PHOSPHATE (TAMIFLU) AND ZANAMIVIR (RELENZA) 95 Douglas S. Johnson and Jie Jack Li 8 PEROXISOME PROLIFERATOR-ACTIVATED RECEPTOR (PPAR) AGONISTS FOR TYPE 2 DIABETES 117 Jin Li 9 ANGIOTENSIN AT1 ANTAGONISTS FOR HYPERTENSION 129 Larry Yet 10 LEADING ACE INHIBITORS FOR HYPERTENSION 143 Victor J. Cee and Edward J. Olhava 11 DIHYDROPYRIDINE CALCIUM CHANNEL BLOCKERS FOR HYPERTENSION 159 Daniel P. Christen 12 SECOND-GENERATION HMG-CoA REDUCTASE INHIBITORS 169 Jeffrey A. Pfefferkorn 13 CHOLESTEROL ABSORPTION INHIBITORS: EZETIMIBE (ZETIA) 183 Stuart B. Rosenblum 14 DUAL SELECTIVE SEROTONIN AND NOREPINEPHRINE REUPTAKE INHIBITORS (SSNRIs) FOR DEPRESSION 199 Marta Pineiro-Nunez 15 GABAA RECEPTOR AGONISTS FOR INSOMNIA: ZOLPIDEM (AMBIEN), ZALEPLON (SONATA), ESZOPICLONE (ESTORRA, LUNESTA), AND INDIPLON 215 Peter R. Guzzo 16 Alpha2Delta LIGANDS: NEURONTIN (GABAPENTIN) AND LYRICA (PREGABALIN) 225 Po-Wai Yuen 17 APPROVED TREATMENTS FOR ATTENTION DEFICIT HYPERACTIVITY DISORDER: AMPHETAMINE (ADDERALL), METHYLPHENIDATE (RITALIN), AND ATOMOXETINE (STRATERRA) 241 David L. Gray References 257 Index 261 Modern Drug Synthesis Preface xi Contributors xiii I. Infectious Diseases 1 Chapter 1. Raltegravir (Isentress), The First-in-class HIV-1 Integrase Inhibitor 3 Julianne A. Hunt Chapter 2. Maraviroc (Selzentry), The First-in-class CCR5 Antagonist for the Treatment of HIV 17 David Price Chapter 3. Darunavir (Prezista), A HIV-1 Protease Inhibitor for Treatment of Multidrug Resistant HIV 29 Arun K. Ghosh and Cuthbert D. Martyr II. Cancer 45 Chapter 4. Decitabine (Dacogen), A DNA Methyltransferase Inhibitor for Cancer 47 Jennifer A. Van Camp Chapter 5. Capecitabine (Xeloda), An Oral Chemotherapy Agent 57 R. Jason Herr Chapter 6. Sorafenib (Nexavar), A Multi-kinase Inhibitor for Advanced Renal Cell Carcinoma and Unresectable Hepatocellular Carcinoma 73 Shuanghua Hu Chapter 7. Sunitinib (Sutent), An Angiogenesis Inhibitor 87 Martin Pettersson Chapter 8. Bortezomib (Velcade), A First-in-class Proteasome Inhibitor 99 Benjamin S. Greener and David S. Millan Chapter 9. Pazopanib (Votrient), A VEGFR Tyrosine Kinase Inhibitor for Cancer 111 Ji Zha