Modern Drug Synthesis

Informationen zum Autor JIE JACK LI is a chemist at Bristol-Myers Squibb Company in Wallingford, Connecticut. He is the coauthor of various books, including Palladium in Heterocyclic Chemistry, Name Reactions: A Collection of Detailed Reaction Mechanisms and Synthetic Applications, Name Reactions in Heterocyclic Chemistry, Contemporary Drug Synthesis, The Art of Drug Synthesis, Name Reactions for Functional Group Transformations, Name Reactions for Homologations, Parts 1 and 2, and Name Reactions for Carbocyclic Ring Formations. DOUGLAS JOHNSON is a medicinal chemist and project leader at Pfizer in Groton, Connecticut. He is a coauthor on more than forty publications and patents, including the books The Art of Drug Synthesis and Contemporary Drug Synthesis. Klappentext The all-inclusive book on the cutting-edge science driving the medicinal chemistry of the latest drugs The successor to the editors' two highly acclaimed works on drug synthesis, Contemporary Drug Synthesis and The Art of Drug Synthesis , this book provides refocused and extensive new coverage detailing how chemistry, biology, and pharmacokinetics integrate to spearhead successful medical findings. Modern Drug Synthesis carries on the mission of delivering the most up-to-date developments unfolding in this rapidly evolving field by placing a stronger emphasis on medicinal chemistry and pharmacology, in addition to drug synthesis. Other highlights include: Chapters are logically divided into categories such as background of disease area, pharmacology, SAR (structure-activity relationships), pharmacokinetics and drug metabolism, efficacy and safety, and synthesis Expert analysis of the pros and cons of different synthetic routes A step-by-step breakdown of today's drug discovery process for professionals and students Supporting case studies in each chapter Modern Drug Synthesis shows that whether drug synthesis is in early development or the process stage, the ability to design elegant and economical synthetic routes is often a major factor making a drug a commercial winner. Easy to follow and stacked with valuable information on the present and future direction of medicinal chemistry, Modern Drug Synthesis is the one guide that paints a clear and complete picture of this complex subject. Zusammenfassung 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. Inhaltsverzeichnis Preface xi Contributors xiii I. Infectious Diseases 1 Chapter 1. Raltegravir (Isentress), The First-in-class HIV-1 Integrase Inhibitor 3 Julianne A. Hunt 1.1 Background 3 1.2 Pharmacology 5 1.3 Structure-Activity Relationship (SAR) 6 1.4 Pharmacokinetics and Drug Metabolism 8 1.5 Efficacy and Safety 9 1.6 Syntheses 10 1.7 References 13 Chapter 2. Maraviroc (Selzentry), The First-in-class CCR5 Antagonist for the Treatment of HIV 17 David Price 2.1 Background 17 2.2 Structure-Activity Relationship (SAR) 19 2.3 Pharmacokinetics and Safety 21 2.4 Syntheses 22 2.5 References 27 Chapter 3. Darunavir (Prezista), A HIV-1 Protease Inhibitor for Treatment of Multidrug Resistant HIV 29 Arun K. Ghosh and Cuthbert D. Martyr 3.1 Background 29 3.2 Pharmacology 32 3.3 Structure-Activity Relationship (SAR) 32 3.4 Pharmacokinetics and Drug Metabolism 33 3.5 Efficacy and Safety 33 3.6 Syntheses 34 3.7 References 42 II. Cancer 45 Chapt...

Sommario

Preface.
 
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

Relazione

"All chapters are very well written, and the used schemes and tables are conveniently arranged. The information and explanations given are strengthened by well-chosen examples and so the reader can easily follow the discussion. The comprehensive referenced literature placed at the end of each chapter enables further reading, and a detailed keyword index in combination with a logically structured Table of Content allows fast access to the topic of interest." ( ChemMedChem , 2010)

Dettagli sul prodotto

• Autori: Johnson, Douglas S. Johnson, Li, Jie Jack Li, Jie Jack (Bristol Myers Squibb Company Li, Jie Jack Johnson Li, JJ Li, LI JIE JACK JOHNSON DOUGLAS S
• Con la collaborazione di: Ji Jack Li (Editore), Jie Jack Li (Editore), Douglas S. Johnson (Editore), Johnson Douglas S. (Editore), Jie J. Li (Editore), Jie Jack Li (Editore), Li Jie Jack (Editore), S Johnson (Editore), S Johnson (Editore)
• Editore: Wiley, John and Sons Ltd
• Lingue: Inglese
• Formato: Copertina rigida
• Pubblicazione: 27.08.2010
• EAN: 9780470525838
• ISBN: 978-0-470-52583-8
• Pagine: 376
• Serie: Wiley Series on Drug Synthesis; Wiley Series on Drug Synthesis
• Categorie: Scienze naturali, medicina, informatica, tecnica > Chimica > Chimica organica; Chemie, Organische Chemie, ORGANIC CHEMISTRY, chemistry, Pharmaceutical & Medicinal Chemistry, Pharmazeutische u. Medizinische Chemie, Arzneimitteldesign