Annual Reports in Medicinal Chemistry - 1st Edition - ISBN: 9780123743442, 9780080921877

Annual Reports in Medicinal Chemistry, Volume 43

1st Edition

Series Editors: John Macor
eBook ISBN: 9780080921877
Paperback ISBN: 9780123743442
Imprint: Academic Press
Published Date: 20th October 2008
Page Count: 584
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Table of Contents

  • Preface
  • Part I: Central Nervous System Diseases
    • Chapter 1: Recent Advances in Corticotropin-Releasing Factor Receptor Antagonists
      • Publisher Summary
      • 1 INTRODUCTION
      • 2 NON-PEPTIDE SMALL MOLECULE CRF-R1 ANTAGONISTS
      • 3 THERAPEUTIC INDICATIONS
      • 4 CLINICAL FINDINGS WITH CRF-R1 ANTAGONISTS
      • 5 SUMMARY
    • Chapter 2: Recent Advances on the 5-HT5A, 5-HT6 and 5-HT7 Receptors
      • Publisher Summary
      • 1 INTRODUCTION
      • 2 THE 5-HT5A RECEPTOR
      • 3 THE 5-HT6 RECEPTOR
      • 4 THE 5-HT7 RECEPTOR
      • 5 CONCLUSIONS
    • Chapter 3: Recent Advances in Voltage-Gated Sodium Channel Blockers: Therapeutic Potential as Drug Targets in the CNS
      • Publisher Summary
      • 1 INTRODUCTION
      • 2 SODIUM CHANNELS AND THERAPEUTIC OPPORTUNITIES
      • 3 ASSAYS
      • 4 CNS AND PNS SODIUM CHANNEL SUBTYPES AND THEIR MODULATORS
      • 5 ADDITIONAL STRUCTURES
      • 6 RECENT CLINICAL DATA
      • 7 CONCLUSION AND FUTURE PERSPECTIVES
    • Chapter 4: Medication Development for the Treatment of Substance Abuse
      • Publisher Summary
      • 1 INTRODUCTION
      • 2 THE ADDICTIVE STATE
      • 3 BEHAVIORAL PHARMACOLOGY MODELS OF ADDICTION
      • 4 PARTIAL AGONIST APPROACH TO MEDICATION DEVELOPMENT
      • 5 OPIOIDS
      • 6 COCAINE
      • 7 STIMULANTS: METHAMPHETAMINE
      • 8 CONCLUSION
  • Part II: Cardiovascular and Metabolic Diseases
    • Chapter 5: GPR40 (FFAR1) Modulators
      • Publisher Summary
      • 1 INTRODUCTION
      • 2 BIOLOGY OF GPR40
      • 3 ARYLPROPIONIC ACIDS
      • 4 LONG CHAIN ALKYL ACID DERIVATIVES
      • 5 ACID ISOSTERES
      • 6 CONCLUSION
    • Chapter 6: Rho-Kinase Inhibitors for Cardiovascular Disease
      • Publisher Summary
      • 1 INTRODUCTION
      • 2 PRECLINICAL STUDIES
      • 3 CLINICAL STUDIES
      • 4 STRUCTURE
      • 5 MEDICINAL CHEMISTRY PROGRESS
      • 6 CONCLUSION
      • 7 RECENT DEVELOPMENTS
    • Chapter 7: LXR Agonists for the Treatment of Atherosclerosis: Recent Highlights
      • Publisher Summary
      • 1 INTRODUCTION
      • 2 LXR AND ATHEROSCLEROSIS
      • 3 LXR SUBTYPE SELECTIVITY
      • 4 CLINICAL CANDIDATE WAY-252623
      • 5 CONCLUSION
    • Chapter 8: Glucagon Receptor Antagonists for Type II Diabetes
      • Publisher Summary
      • 1 INTRODUCTION
      • 2 GLUCAGON RECEPTOR ANTAGONISTS
      • 3 CONCLUSION
  • Part III: Inflammation/Pulmonary/GI
    • Chapter 9: Advances Toward Dissociated Non-Steroidal Glucocorticoid Receptor Agonists
      • Publisher Summary
      • 1 INTRODUCTION
      • 2 FLUOROCORTIVAZOL ANALOGS
      • 3 HYDROXY-TRIFLUOROMETHYL-PHENYL-PENTANOIC (HTPP) ARYL AMIDES
      • 4 DIHYDRO-1H-BENZOPYRANO[3,4-f]QUINOLINES (DBQ)
      • 5 ADDITIONAL FUSED CYCLIC CORES
      • 6 SULFONAMIDE-LINKED SCAFFOLDS
      • 7 CONCLUSION
    • Chapter 10: Advances in the Discovery of IκB Kinase Inhibitors
      • Publisher Summary
      • 1 INTRODUCTION
      • 2 BIOCHEMISTRY OF IκB KINASE INHIBITION
      • 3 IKK-2 PHARMACOLOGY
      • 4 IKK TOXICOLOGY
      • 5 CLINICAL TRIALS
      • 6 RECENT IKK-2 INHIBITORS
      • 7 CONCLUSIONS
    • Chapter 11: Protease Inhibitors for the Potential Treatment of Chronic Obstructive Pulmonary Disease and Asthma
      • Publisher Summary
      • 1 INTRODUCTION
      • 2 SERINE PROTEASE INHIBITORS
      • 3 CYSTEINE PROTEASE INHIBITORS
      • 4 MATRIX METALLOPROTEINASES INHIBITORS
      • 5 CONCLUSIONS
  • Part IV: Oncology
    • Chapter 12: mTOR Inhibitors in Oncology
      • Publisher Summary
      • 1 INTRODUCTION
      • 2 MECHANISM OF mTOR INHIBITION
      • 3 RAPAMYCIN ANALOGS IN THE CLINIC
      • 4 PRE-CLINICAL RAPAMYCIN ANALOGS
      • 5 ATP COMPETITIVE mTOR INHIBITORS
      • 6 OTHER mTOR INHIBITORS
      • 7 CONCLUSION
    • Chapter 13: Oncology Drug Targets in the Sphingomyelin-Signaling Pathway
      • Publisher Summary
      • 1 INTRODUCTION
      • 2 THERAPEUTIC TARGETS
      • 3 TREATMENT MODALITIES
      • 4 OPPORTUNITY AND THREAT
      • 5 DISCUSSION AND CONCLUSIONS
  • Part V: Infectious Diseases
    • Chapter 14: Inhibitors of Respiratory Syncytial Virus
      • Publisher Summary
      • 1 INTRODUCTION
      • 2 FUSION INHIBITORS
      • 3 N-PROTEIN INTERACTING COMPOUNDS
      • 4 OTHER MECHANISMS
      • 5 ANTISENSE COMPOUNDS AND siRNA
      • 6 FUTURE PROSPECTS
    • Chapter 15: Recent Developments in β-Lactamases and Inhibitors
      • Publisher Summary
      • 1 INTRODUCTION
      • 2 COMBINATION OF INHIBITORS WITH ANTIBIOTICS
      • 3 β-LACTAMASES
      • 4 INHIBITORS BASED ON CRYSTAL STRUCTURES OF β-LACTAMASES
      • 5 BROAD-SPECTRUM INHIBITORS
      • 6 6-METHYLIDENE PENEMS
      • 7 CONCLUSION
    • Chapter 16: Recent Development in the Treatment of Clostridium difficile Associated Disease (CDAD)
      • Publisher Summary
      • 1 INTRODUCTION
      • 2 ROLE OF TOXINS IN CDAD
      • 3 REVIEW ON CURRENT TREATMENTS
      • 4 AGENTS IN DEVELOPMENT
      • 5 CONCLUSIONS
    • Chapter 17: Recent Advances in the Discovery of Hybrid Antibacterial Agents
      • Publisher Summary
      • 1 INTRODUCTION
      • 2 NOVEL HYBRID/DUAL-ACTION ANTIBACTERIAL AGENTS
      • 3 CONCLUSIONS
  • Part VI: Topics in Biology
    • Chapter 18: Recent Renaissance of Prostaglandin Research
      • Publisher Summary
      • 1 INTRODUCTION
      • 2 SELECTIVE PROSTANOID AGONISTS AND ANTAGONISTS
      • 3 RECENT NOVEL PROSTANOID STRUCTURE DESIGN AND ACTIVITY
      • 4 CURRENT RESEARCH AIMED AT PROSTANOID-DERIVED THERAPEUTICS
      • 5 CONCLUSION
    • Chapter 19: Human Exposure and Dose Projections
      • Publisher Summary
      • 1 INTRODUCTION
      • 2 THEORETICAL FRAMEWORK AND APPROACHES
      • 3 DATA ANALYSIS AND APPLICATIONS
      • 4 CONCLUSION AND FUTURE DIRECTIONS
    • Chapter 20: Modeling Networks of Glycolysis, Overall Energy Metabolism and Drug Metabolism under a Systems Biology Approach
      • Publisher Summary
      • 1 INTRODUCTION
      • 2 CHANGING ARCHITECTURE IN NEWER METABOLIC MODELS
      • 3 ANALYSIS OF METABOLIC NETWORK CONTROL DISTRIBUTION IN DRUG DISCOVERY AND DISEASE
      • 4 MODELING METABOLISM WITHIN THE BRAIN
      • 5 MODELING BRAIN METABOLIC NETWORKS
      • 6 CAN STABLE ISOTOPE METHODS PROVIDE NEW INSIGHTS INTO OPEN QUESTIONS IN BRAIN METABOLIC REGULATION AND NEUROLOGICAL DISORDERS?
      • 7 FUTURE DIRECTIONS IN METABOLIC MODELING
      • 8 CONCLUSION
  • Part VII: Topics in Drug Design and Discovery
    • Chapter 21: Contrasting the Gastrointestinal Tracts of Mammals: Factors that Influence Absorption
      • Publisher Summary
      • 1 INTRODUCTION
      • 2 OVERVIEW OF THE ALIMENTARY CANAL
      • 3 SITES OF AND BARRIERS TO ABSORPTION
      • 4 DIMENSIONS OF REGIONS OF THE GASTROINTESTINAL TRACT
      • 5 SURFACE AREAS OF THE GASTROINTESTINAL TRACT
      • 6 TRANSIT TIMES
      • 7 NATURE OF LUMINAL CONTENTS
      • 8 BILE AND BILE SALTS
      • 9 CONCLUSIONS ABOUT ABSORPTION
      • ACKNOWLEDGEMENTS
    • Chapter 22: The Emerging Utility of Co-Crystals in Drug Discovery and Development
      • Publisher Summary
      • 1 INTRODUCTION
      • 2 FUNDAMENTALS OF CO-CRYSTALS: NOMENCLATURE AND INTERACTIONS
      • 3 A BRIEF HISTORY OF CO-CRYSTALS
      • 4 THE PREPARATION AND CHARACTERIZATION OF CO-CRYSTALS
      • 5 APPLICATIONS OF CO-CRYSTALS IN DRUG FORMULATION
      • 6 OPTICAL RESOLUTION BY CO-CRYSTAL FORMATION
      • 7 CO-CRYSTALS AND TOXICITY
      • 8 SUMMARY
    • Chapter 23: Pregnane X Receptor: Prediction and Attenuation of Human CYP3A4 Enzyme Induction and Drug–Drug Interactions
      • Publisher Summary
      • 1 INTRODUCTION
      • 2 PREGNANE X RECEPTOR
      • 3 CRYSTAL STRUCTURE AND MOLECULAR MODELING OF PXR
      • 4 SUMMARY
    • Chapter 24: Formulation in Drug Discovery
      • Publisher Summary
      • 1 INTRODUCTION
      • 2 EARLY CONSIDERATIONS OF A NEW CHEMICAL ENTITY
      • 3 SOLUBILITY THEORY
      • 4 FORMULATION
      • 5 CONCLUSION
  • Part VIII: Trends and Perspectives
    • Chapter 25: To Market, To Market — 2007
      • Publisher Summary
      • 1 INTRODUCTION
      • 2 ALISKIREN (ANTIHYPERTENSIVE) [3–8]
      • 3 AMBRISENTAN (PULMONARY ARTERIAL HYPERTENSION) [9–13]
      • 4 ARFORMOTEROL (COPD) [14–17]
      • 5 CLEVUDINE (HEPATITIS B) [18–21]
      • 6 ECULIZUMAB (HEMOGLOBINURIA) [22–24]
      • 7 FLUTICASONE FUROATE (ANTIALLERGY) [25–27]
      • 8 GARENOXACIN (ANTI-INFECTIVE) [28–32]
      • 9 IMIDAFENACIN (OVERACTIVE BLADDER) [33–37]
      • 10 IXABEPILONE (ANTICANCER) [38–42]
      • 11 LAPATINIB (ANTICANCER) [43–47]
      • 12 LISDEXAMFETAMINE (ADHD) [48–51]
      • 13 MARAVIROC (ANTI-INFECTIVE-HIV) [52–55]
      • 14 NILOTINIB (ANTICANCER — CML) [56–59]
      • 15 PALIPERIDONE (ANTIPSYCHOTIC) [60–63]
      • 16 RALTEGRAVIR (ANTI-INFECTIVE-HIV) [64–67]
      • 17 RETAPAMULIN (ANTI-INFECTIVE) [68–71]
      • 18 RUFINAMIDE (ANTICONVULSANT) [72–75]
      • 19 TEMSIROLIMUS (ANTICANCER) [76–80]
      • 20 TRABECTEDIN (ANTICANCER) [81–86]
      • 21 VILDAGLIPTIN (ANTIDIABETIC) [87–92]
  • Compound Name, Code Number and Subject Index, Volume 43
  • Cumulative Chapter Titles Keyword Index, Volume 1–43
  • Cumulative Nce Introduction Index, 1983–2007
  • Cumulative Nce Introduction Index, 1983–2007 (By Indication)

Description

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

Key Features

  • covers findings related to cardiovascular, inflammation, and pulmonary diseases

  • examines issues in oncology, from mTor inhibitors to drug targets

  • incorporates up-to-date information on drug design and discovery, including delivery to market

Readership

medicinal, pharmaceutical, and organic chemists


Details

No. of pages:
584
Language:
English
Copyright:
© Academic Press 2008
Published:
Imprint:
Academic Press
eBook ISBN:
9780080921877
Paperback ISBN:
9780123743442

About the Series Editors

John Macor Series Editor

Affiliations and Expertise

Neuroscience Discovery Chemistry, Bristol-Myers Squibb, USA