Comprehensive accounts of pharmaceutical research and development : from discovery to late-stage process development

書誌事項

Comprehensive accounts of pharmaceutical research and development : from discovery to late-stage process development

Ahmed F. Abdel-Magid, Jaan Pesti, Rajappa Vaidyanathan, editor[s] ; sponsored by the ACS Division of Organic Chemistry

(ACS symposium series, 1239, 1240)

American Chemical Society , Distributed in print by Oxford University Press, c2016

  • v. 1
  • v. 2

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注記

Includes bibliographical references and indexes

内容説明・目次

巻冊次

v. 1 ISBN 9780841231894

内容説明

Until the latter part of the 19th century, the majority of known drugs were either herbs or extracts of active ingredients from botanical sources. At this point, the world witnessed two major cornerstone achievements that laid the foundation of modern drug discovery and development: the emergence of pharmacology as a contemporary science through the work of Schmiedeberg (considered by many as the father of modern pharmacology) at the University of Strasbourg, and Woehler's landmark synthesis of urea from ammonium cyanate (the first synthesis of an 'organic' molecule from an 'inorganic' source) which heralded the birth of modern organic chemistry. Drug discovery has evolved from relying on luck, accident and serendipity to a complex endeavor that is at the interface of several disciplines (e.g. pharmacology, biology, chemistry), and is built on the understanding of mechanisms and causes of diseases. This book is produced to celebrate the evolution of drug discovery and development. It will prove useful to synthetic organic chemists in both pharmaceutical industry and in academia, and can serve as a teaching tool to students who want to learn and understand the processes and challenges of drug discovery and development with real examples from top pharmaceutical companies. The chapters contain citations of a large number of valuable selected references to the primary literature. The book highlights the tireless efforts of discovery and process chemists, and their roles in the advancement of drug discovery and development. The chapters presented in this book are written by a selected group of outstanding, very accomplished medicinal and process chemists with noted experiences and diverse backgrounds, representing some of the top pharmaceutical companies. The chapters highlight examples of emerging concepts, new developments and challenges arising in the discovery of new drug candidates and the development of new practical synthetic chemistry processes to produce these drug candidates on large scale. The discovery of each drug or drug candidate is presented by the discovery chemist(s) and the process chemist(s) who developed the drug. These writing teams describe the drug's development to give the reader a complete story of drug discovery and development.

目次

Preface 1. Discovery and Chemical Development of Suvorexant - A Dual Orexin Antagonist for Sleep Disorder 2. Discovery of Novel Protein Fucosylation Inhibitors and Development of a Manufacturing Process To Prepare Inhibitor 6,6,6-Trifluorofucose 3. Development of Hsp90 Inhibitors for the Treatment of HER-2 Positive Solid Cancers 4. Discovery of the Novel Oxadiazole-Containing 5-Lipoxygenase Activating Protein (FLAP) Inhibitor BI 665915 5. Development of an Efficient Asymmetric Synthesis of the Chiral Quaternary 5-Lipoxygenase Activating Protein Inhibitor 6. The Discovery and Process Chemistry Development of GDC-0084, a Brain Penetrating Inhibitor of PI3K and mTOR 7. Discovery and Development of Doravirine: An Investigational Next Generation Non-Nucleside Reverse Transcriptase Inhibitor (NNRTI) for the Treatment of HIV 8. The Discovery of Dacomitinib, a Potent Irreversible EGFR Inhibitor 9. Early and Late Stage Process Development for the Manufacture of Dacomitinib 10. Discovery and Development of the Natural Product Derivative SPI-1865 as a Gamma Secretase Modulator for Alzheimer's Disease: Part I 11. Discovery and Development of the Natural Product Derivative SPI-1865 as a Gamma Secretase Modulator for Alzheimer's Disease 12. Telaprevir: From Drug Discovery to the Manufacture of Drug Substance Editors' Biographies Indexes
巻冊次

v. 2 ISBN 9780841231917

内容説明

Until the latter part of the 19th century, the majority of known drugs were either herbs or extracts of active ingredients from botanical sources. At this point, the world witnessed two major cornerstone achievements that laid the foundation of modern drug discovery and development: the emergence of pharmacology as a contemporary science through the work of Schmiedeberg (considered by many as the father of modern pharmacology) at the University of Strasbourg, and Woehler's landmark synthesis of urea from ammonium cyanate (the first synthesis of an 'organic' molecule from an 'inorganic' source) which heralded the birth of modern organic chemistry. Drug discovery has evolved from relying on luck, accident and serendipity to a complex endeavor that is at the interface of several disciplines (e.g. pharmacology, biology, chemistry), and is built on the understanding of mechanisms and causes of diseases. This book is produced to celebrate the evolution of drug discovery and development. It will prove useful to synthetic organic chemists in both pharmaceutical industry and in academia, and can serve as a teaching tool to students who want to learn and understand the processes and challenges of drug discovery and development with real examples from top pharmaceutical companies. The chapters contain citations of a large number of valuable selected references to the primary literature. The book highlights the tireless efforts of discovery and process chemists, and their roles in the advancement of drug discovery and development. The chapters presented in this book are written by a selected group of outstanding, very accomplished medicinal and process chemists with noted experiences and diverse backgrounds, representing some of the top pharmaceutical companies. The chapters highlight examples of emerging concepts, new developments and challenges arising in the discovery of new drug candidates and the development of new practical synthetic chemistry processes to produce these drug candidates on large scale. The discovery of each drug or drug candidate is presented by the discovery chemist(s) and the process chemist(s) who developed the drug. These writing teams describe the drug's development to give the reader a complete story of drug discovery and development.

目次

Preface 1. Synthesis of a Potent NAE Inhibitor: Pevonedistat 2. Process Development and GMP Production of a Potent NEDD8-Activating Enzyme (NAE) Inhibitor: Pevonedistat 3. The Discovery and Synthesis of the CGRP Receptor Antagonist MK-3207 4. Design and Enabling Development of Hydroxyethylamine-Derived BACE1 Inhibitor 5. Identification and Optimization of a Series of Non-Steroidal Trifluoromethylcarbinol Glucocorticoid Receptor Agonists 6. Development of an Asymmetric Route for Large-Scale Synthesis of a Glucocorticoid Agonist 7. The Medicinal Chemistry and Commercial Manufacturing Behind the Discovery and Development of the Hedgehog Inhibitor Vismodegib 8. Discovery and Process Development of Class I PI3K and Class I PI3K/mTOR Inhibitors GDC-0941 and GDC-0980 9. The Development and Manufacture of Azacitidine, Decitabine, and Cladribine: Stereoselective Ribonucleoside Drug Synthesis Using the Vorbruggen Glycosylation Editors' Biographies Indexes

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