Annual Reports in Medicinal Chemistry - 1st Edition - ISBN: 9780128001677, 9780128003725

Annual Reports in Medicinal Chemistry, Volume 49

1st Edition

Series Editors: Manoj Desai
eBook ISBN: 9780128003725
Paperback ISBN: 9780128001677
Imprint: Academic Press
Published Date: 24th September 2014
Page Count: 636
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Table of Contents

  • Preface
  • Personal Essays
    • Chapter One: A Personal Essay: My Experiences in the Pharmaceutical Industry
    • Chapter Two: Adventures in Medicinal Chemistry: A Career in Drug Discovery
      • Acknowledgments
  • Section 1: Central Nervous System Diseases
    • Chapter Three: Natural and Synthetic Neuroactive Steroid Modulators of GABAA and NMDA Receptors
      • Abstract
      • 1 Introduction
      • 2 NAS Modulators of the GABAA Receptor
      • 3 NAS Modulators of the NMDA Receptor
      • 4 Conclusions
    • Chapter Four: Development of LRRK2 Kinase Inhibitors for Parkinson's Disease
      • Abstract
      • 1 Introduction
      • 2 LRRK2 Biology
      • 3 Medicinal Chemistry
      • 4 Preclinical Animal Models
      • 5 Conclusions
    • Chapter Five: Stimulating Neurotrophin Receptors in the Treatment of Neurodegenerative Disorders
      • Abstract
      • 1 Introduction
      • 2 NTs and NT Receptors—Structure and Function
      • 3 Role of NTs and Their Receptors in Neurodegenerative Disorders
      • 4 Pharmacological Activators of NT Receptors
      • 5 Conclusion
  • Section 2: Cardiovascular and Metabolic Diseases
    • Chapter Six: Small-Molecule Modulators of GPR40 (FFA1)
      • Abstract
      • 1 Introduction
      • 2 Recent Discoveries in GPR40 Biology
      • 3 GPR40 Partial Agonists
      • 4 GPR40 Full Agonists
      • 5 Conclusions
    • Chapter Seven: Recent Advances in the Development of P2Y12 Receptor Antagonists as Antiplatelet Agents
      • Abstract
      • 1 Introduction
      • 2 FDA-Approved P2Y12 Receptor Antagonists
      • 3 New P2Y12 Receptor Antagonists
      • 4 Clinical Application
      • 5 Conclusions
    • Chapter Eight: Current Approaches to the Treatment of Atrial Fibrillation
      • Abstract
      • 1 Introduction
      • 2 Atrial-Selective Agents Versus Non-selective Agents
      • 3 Clinical Updates
      • 4 Preclincal Advances
      • 5 Conclusion
  • Section 3: Inflammation/Pulmonary/GI Diseases
    • Chapter Nine: Advances in the Discovery of Small-Molecule IRAK4 Inhibitors
      • Abstract
      • 1 Introduction
      • 2 Rationale for Targeting IRAK4 in Inflammatory Diseases
      • 3 IRAK4 Structure
      • 4 Recent Medicinal Chemistry Efforts
      • 5 Conclusions
    • Chapter Ten: H4 Receptor Antagonists and Their Potential Therapeutic Applications
      • Abstract
      • 1 Introduction
      • 2 Antagonists of the H4 Receptor
      • 3 Role of the Histamine H4 Receptor in Disease Models
      • 4 Clinical Development of H4 Receptor Antagonists
      • 5 Conclusions
    • Chapter Eleven: Urate Crystal Deposition Disease and Gout—New Therapies for an Old Problem
      • Abstract
      • 1 Introduction
      • 2 Therapeutics for Gout by Clinical Manifestation
      • 3 Conclusions
  • Section 4: Oncology
    • Chapter Twelve: p53–MDM2 and MDMX Antagonists
      • Abstract
      • 1 Introduction
      • 2 MDM2 Antagonists
      • 3 MDMX Antagonists
      • 4 Conclusion
    • Chapter Thirteen: Modulators of Atypical Protein Kinase C as Anticancer Agents
      • Abstract
      • 1 Introduction
      • 2 Atypical Protein Kinase C Isoforms
      • 3 Disease Linkage of Atypical PKCs
      • 4 Non-ATP-Binding Site Inhibitors
      • 5 ATP-Binding Site Inhibitors
      • 6 Conclusions
  • Section 5: Infectious Diseases
    • Chapter Fourteen: Advancement of Cell Wall Inhibitors in Mycobacterium tuberculosis
      • Abstract
      • 1 Introduction
      • 2 Cell Wall Inhibitors
      • 3 Conclusions
    • Chapter Fifteen: Nucleosides and Nucleotides for the Treatment of Viral Diseases
      • Abstract
      • 1 Introduction
      • 2 Human Immunodeficiency Virus
      • 3 Hepatitis B Virus
      • 4 Hepatitis C Virus
      • 5 Dengue Virus
      • 6 Conclusion
    • Chapter Sixteen: Advances in Inhibitors of Penicillin-Binding Proteins and β-Lactamases as Antibacterial Agents
      • Abstract
      • 1 Introduction
      • 2 PBP Inhibitors
      • 3 β-Lactamase Inhibitors
      • 4 Conclusions and Outlook
  • Section 6: Topics in Biology
    • Chapter Seventeen: Tumor Microenvironment as Target in Cancer Therapy
      • Abstract
      • 1 Introduction
      • 2 Cancer-Promoting Enzymes and Inhibitors
      • 3 Carbamoylphosphonates: Inhibitors of Extracellular Zinc–Enzymes
      • 4 Conclusions and Outlook
      • Acknowledgments
    • Chapter Eighteen: Novel Screening Paradigms for the Identification of Allosteric Modulators and/or Biased Ligands for Challenging G-Protein-Coupled Receptors
      • Abstract
      • 1 Introduction
      • 2 Allosteric Modulators
      • 3 Biased Ligands
      • 4 Ab Discovery as Novel AMs/BLs
      • 5 Conclusions
    • Chapter Nineteen: Mer Receptor Tyrosine Kinase: Therapeutic Opportunities in Oncology, Virology, and Cardiovascular Indications
      • Abstract
      • 1 Introduction
      • 2 Mer Biological Function and Therapeutic Opportunities
      • 3 Small Molecule Mer Inhibitors
      • 4 Future Directions and Conclusions
  • Section 7: Topics in Drug Design and Discovery
    • Chapter Twenty: Disease-Modifying Agents for the Treatment of Cystic Fibrosis
      • Abstract
      • 1 Introduction
      • 2 Treating Class I Defects
      • 3 Treating Class II Defects (Correctors)
      • 4 Treating Class III Defects (Potentiators)
      • 5 Compounds with Dual Activity
      • 6 Conclusions
    • Chapter Twenty-One: Advancements in Stapled Peptide Drug Discovery & Development
      • Abstract
      • 1 Introduction
      • 2 Beneficial Effects Attributed to the Hydrocarbon Staple
      • 3 Drug Discovery: Preclinical Research
      • 4 Drug Development and P53 Reactivation
      • 5 Concluding Remarks
    • Chapter Twenty-Two: Cytochrome P450 Enzyme Metabolites in Lead Discovery and Development
      • Abstract
      • 1 Introduction
      • 2 Identification of CYP-Modified Natural Products as Drug Leads
      • 3 Identification of Pharmacologically Active Metabolites of Known Drugs
      • 4 Future Directions and Conclusions
      • Acknowledgments
  • Section 8: Case Histories and NCEs
    • Chapter Twenty-Three: Case History: ForxigaTM (Dapagliflozin), a Potent Selective SGLT2 Inhibitor for Treatment of Diabetes
      • Abstract
      • 1 Introduction
      • 2 Renal Recovery of Glucose
      • 3 O-Glucoside SGLT2 Inhibitors
      • 4 C-Aryl Glucoside SGLT2 Inhibitors
      • 5 Synthesis of Dapagliflozin
      • 6 Preclinical Profiling Studies with Dapagliflozin
      • 7 Clinical Studies with Dapagliflozin
      • 8 Conclusion
    • Chapter Twenty-Four: Case History: Kalydeco® (VX-770, Ivacaftor), a CFTR Potentiator for the Treatment of Patients with Cystic Fibrosis and the G551D-CFTR Mutation
      • Abstract
      • 1 Introduction
      • 2 CFTR as a Drug Discovery Target
      • 3 The Discovery of CFTR Potentiators
      • 4 Medicinal Chemistry Efforts Culminating in Ivacaftor
      • 5 Preclinical Properties of Ivacaftor
      • 6 Formulation Development
      • 7 Clinical Studies
      • 8 Conclusion
    • Chapter Twenty-Five: Case History: Xeljanz™ (Tofacitinib Citrate), a First-in-Class Janus Kinase Inhibitor for the Treatment of Rheumatoid Arthritis
      • Abstract
      • 1 Introduction
      • 2 Rationale for Targeting the JAK Enzymes
      • 3 Medicinal Chemistry Efforts Culminating in the Identification of Tofacitinib15
      • 4 Selectivity and Pharmacology of Tofacitinib
      • 5 Preclinical Properties of Tofacitinib
      • 6 Clinical Properties of Tofacitinib
      • 7 Conclusions
      • Acknowledgments
    • Chapter Twenty-Six: New Chemical Entities Entering Phase III Trials in 2013
      • Abstract
    • Chapter Twenty-Seven: To Market, To Market—2013
      • Abstract
      • Overview
      • 1 Acotiamide (Dyspepsia)11–17
      • 2 Ado-Trastuzumab Emtansine (Anticancer)18–22
      • 3 Afatinib (Anticancer)23–29
      • 4 Canagliflozin (Antidiabetic)30–42
      • 5 Cetilistat (Antiobesity)43–52
      • 6 Cobicistat (Antiviral, Pharmacokinetic Enhancer)53–59
      • 7 Dabrafenib (Anticancer)60–65
      • 8 Dimethyl Fumarate (Multiple Sclerosis)66–80
      • 9 Dolutegravir (Antiviral)81–91
      • 10 Efinaconazole (Antifungal)92–98
      • 11 Elvitegravir (Antiviral)99–108
      • 12 Ibrutinib (Anticancer)109–114
      • 13 Istradefylline (Parkinson's Disease)115–122
      • 14 Lixisenatide (Antidiabetic)123–131
      • 15 Macitentan (Antihypertensive)132–138
      • 16 Metreleptin (Lipodystrophy)139–150
      • 17 Mipomersen (Antihypercholesteremic)151–158
      • 18 Obinutuzumab (Anticancer)159–164
      • 19 Olodaterol (Chronic Obstructive Pulmonary Disease)165–174
      • 20 Ospemifene (Dyspareunia)175–181
      • 21 Pomalidomide (Anticancer)182–195
      • 22 Riociguat (Pulmonary Hypertension)196–203
      • 23 Saroglitazar (Antidiabetic)204–212
      • 24 Simeprevir (Antiviral)214–223
      • 25 Sofosbuvir (Antiviral)224–235
      • 26 Trametinib (Anticancer)236–242
      • 27 Vortioxetine (Antidepressant)243–252
  • Keyword Index, Volume 49
  • Cumulative Chapter Titles Keyword Index, Volume 1 – 49
  • Cumulative NCE Introduction Index, 1983–2013
  • Cumulative NCE Introduction Index, 1983–2013 (By Indication)

Description

Annual Reports in Medicinal Chemistry provides timely and critical reviews of important topics in medicinal chemistry with an emphasis on emerging topics in the biological sciences that are expected to provide the basis for entirely new future therapies.

Key Features

  • Reviews on hot topics of interest in small molecule drug discovery heavily pursued by industrial research organizations
  • Provides preclinical information in the context of chemical structures
  • Knowledgeable section editors who evaluate invited reviews for scientific rigor

Readership

Ideally suited for chemists engaged in multidisciplinary teams for drug discovery including medicinal chemists and others involved in chemical biology and bio-organic disciplines and computational chemistry


Details

No. of pages:
636
Language:
English
Copyright:
© Academic Press 2014
Published:
Imprint:
Academic Press
eBook ISBN:
9780128003725
Paperback ISBN:
9780128001677

About the Series Editors

Manoj Desai Series Editor

Dr. Manoj Desai began his career in the pharmaceutical industry at Pfizer Inc, Central Research Division, Groton, CT (1986-1994) before moving to Chiron Corporation (1994-2003) as Director of medicinal chemistry; he was promoted to Vice President, lead discovery and medicinal chemistry (2000). In October 2003, he was appointed Vice President of medicinal chemistry at Gilead Sciences. At Pfizer, he was responsible for the medicinal chemistry efforts that lead to the discovery of oral Substance P antagonist CP-99994 which became the basis for the discovery of the new anti-emetics. At Chiron he formulated macrobead technology for the synthesis and screening of compound libraries for HTS and built the medicinal chemistry department with focus on kinase inhibitors. At Gilead, he was an active proponent to develop a pharmacoenhancer devoid of antiviral activity to improve the pharmacokinetics of integrase inhibitor elvitegravir. These efforts led to the discovery of Cobicistat which is one of components of StribildTM that was approved by FDA in August 2012 for the treatment of HIV infection. He is co-inventor on patents of Cobicistat (US 8,148,374), StribildTM and Ledipasvir (US 8,273,341; Phase III). Furthermore, his group at Gilead has advanced numerous compounds into clinical development for the treatment of antiviral diseases, cancer and cardiovascular diseases.

Dr. Desai obtained Ph.D. in organic chemistry from the M.S. University of Baroda in 1981 working with Dr. Sukh Dev and then carried out post-doctoral fellowships at Purdue University working with Professor Herbert C. Brown (19981-1983) and at Harvard University with Professor Elias J. Corey (1983-1986). During his postdoctoral studies, he worked on natural product isolation, development of asymmetric synthetic methods using organoboranes and total synthesis of complex natural products such as retigeranic acid, -trans bergamotene and ginkgolide B.

He has co-authored >60 publications in peer reviewed journals and is an inventor on >25 issued patents. Furthermore, Dr. Desai is Editor-in-Chief for Annual Reports in Medicinal chemistry (2012-current), and have co-edited Comprehensive Medicinal Chemistry II (volume 7). In 2013, he co-edited book titled “Successful Strategies for the Discovery of Antiviral Drugs”.

Affiliations and Expertise

Gilead Sciences, Inc., Foster City, CA, USA