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Informationen zum Autor Xianhai Huang, PhD , is a Principal Scientist at Merck Research Laboratories. Dr. Huang is the inventor or co-inventor on more than forty patents and patent applications. As a mentor in the Schering-Plough chemistry postdoctoral program, Dr. Huang and his group discovered novel synthetic applications of (diacetoxyiodo) benzene and successfully applied the methodology to the total synthesis of psymberin, an antitumor natural product. Robert G. Aslanian, PhD , is an adjunct professor of chemistry at William Paterson University and was formerly a Senior Director of Medicinal Chemistry with the Schering-Plough Research Institute and Merck Research Laboratories. Dr. Aslanian has over twenty-five years of experience in the pharmaceutical industry. He is co-inventor on thirty-eight U.S. patents and coauthor on sixty-seven scientific articles and reviews. Klappentext Learn why some drug discovery and development efforts succeed . . . and others failWritten by international experts in drug discovery and development, this book sets forth carefully researched and analyzed case studies of both successful and failed drug discovery and development efforts, enabling medicinal chemists and pharmaceutical scientists to learn from actual examples. Each case study focuses on a particular drug and therapeutic target, guiding readers through the drug discovery and development process, including drug design rationale, structure-activity relationships, pharmacology, drug metabolism, biology, and clinical studies.Case Studies in Modern Drug Discovery and Development begins with an introductory chapter that puts into perspective the underlying issues facing the pharmaceutical industry and provides insight into future research opportunities. Next, there are fourteen detailed case studies, examining:* All phases of drug discovery and development from initial idea to commercialization* Some of today's most important and life-saving medications* Drugs designed for different therapeutic areas such as cardiovascular disease, infection, inflammation, cancer, metabolic syndrome, and allergies* Examples of prodrugs and inhaled drugs* Reasons why certain drugs failed to advance to market despite major research investmentsEach chapter ends with a list of references leading to the primary literature. There are also plenty of tables and illustrations to help readers fully understand key concepts, processes, and technologies.Improving the success rate of the drug discovery and development process is paramount to the pharmaceutical industry. With this book as their guide, readers can learn from both successful and unsuccessful efforts in order to apply tested and proven science and technologies that increase the probability of success for new drug discovery and development projects. Zusammenfassung Using case studies of successful drug discoveries and launches, this book helps master the necessary knowledge of the drug discovery process. It includes pharmacology, drug metabolism, biology, drug development, and clinical studies. The introduction provides an overview of process, principles, and technologies and each chapter contains case studies that focus on one therapeutic target. It also offers stories from patients who have used the drugs covered as a way to illustrate the impact medicinal chemistry has on real life. Inhaltsverzeichnis Preface xv Contributors xvii Chapter 1 Introduction: Drug Discovery in Difficult Times 1 Malcolm MacCoss Chapter 2 Discovery and Development of The DPP-4 Inhibitor Januvia ® (SITA-GLIPTIN) 10 Emma R. Parmee, Ranabir SinhaRoy, Feng Xu, Jeffrey C. Givand, and Lawrence A. Rosen 2.1 Introduction 10 2.2 DPP-4 Inhibition as a Therapy for Type 2 Diabetes: Identification of Key Determinants for Efficacy and Safety 10 2.2.1 Incretin-Based Therapy for T2DM...
