Annual Reports in Medicinal Chemistry

Annual Reports in Medicinal Chemistry

1st Edition - October 12, 2011

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  • Editor: John Macor
  • Paperback ISBN: 9780123860095
  • eBook ISBN: 9780123860248

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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.

Readership

medicinal, pharmaceutical, and organic chemists

Table of Contents

  • Contributors

    Preface

    Chapter 1: Progress in the Medicinal Chemistry of Group III Metabotropic Glutamate Receptors

    1. Introduction

    2. Group III Orthosteric Ligands

    3. mGlu4 Receptor Allosteric Ligands

    4. mGlu6 Receptor Ligands

    5. mGlu7 Receptor Ligands

    6. mGlu8 Receptor Ligands

    7. Conclusions

    Chapter 2: Recent Advances Toward Pain Therapeutics

    1. Introduction

    2. Sodium Channel Blockers

    3. NGF/TrkA Pathway Interference

    4. FAAH Inhibitors

    5. Conclusions

    Chapter 3: Central Modulation of Circadian Rhythm via CK1 Inhibition for Psychiatric Indications

    1. Introduction

    2. Description of Circadian Clock

    3. CK1 Inhibitors

    4. Preclinical Animal Models

    5. Conclusions

    Chapter 4: Recent Progress in the Discovery of Kv7 Modulators

    1. Introduction

    2. Kv7.1 Channels

    3. Kv7.2–Kv7.5 Channels

    4. Conclusion

    Chapter 5: Bile Acid Receptor Modulators in Metabolic Diseases

    1. Introduction

    2. FXR Agonists

    3. TGR5 Agonists

    4. FXR/TGR5 Dual Agonists

    5. Clinical Studies and Outlook

    Chapter 6: Recent Advances in Mineralocorticoid Receptor Antagonists

    1. Introduction

    2. Aldosterone and MR Biology

    3. RAAS Pathway, MR Antagonists versus ACE, ARB Therapy

    4. Structural Features of the Ligand Binding Domain of MR

    5. Current Medicinal Chemistry Efforts

    6. Conclusions

    Chapter 7: SGLT2 Inhibitors for Type 2 Diabetes

    1. Introduction

    2. SGLT2 Physiology

    3. Clinical Trials

    4. SGLT2 Inhibitors

    5. Conclusion

    Chapter 8: Recent Advances in the Discovery and Development of CRTh2 Antagonists

    1. Introduction

    2. CRTh2 Antagonists

    3. Conclusions

    Chapter 9: Developments and Advances in Gastrointestinal Prokinetic Agents

    1. Introduction

    2. Key Clinical Developments

    3. Recent Medicinal Chemistry Developments

    4. Conclusions

    Chapter 10: Targeting Th17 and Treg Signaling Pathways in Autoimmunity

    1. Introduction

    2. Current Targets and Molecules in Development

    3. Conclusions

    Chapter 11: Advances in the Discovery of C5a Receptor Antagonists

    1. Introduction

    2. Peptide and Large Molecule Agents

    3. Macromolecules

    4. Small Molecule Agents

    5. Clinical Update

    6. Marketed Agents

    7. Conclusion

    Chapter 12: Inhibition of Translation Initiation as a Novel Paradigm for Cancer Therapy

    1. Introduction

    2. State of the Art

    3. Conclusions

    Chapter 13: The Discovery and Development of Smac Mimetics—Small-Molecule Antagonists of the Inhibitor of Apoptosis Proteins

    1. Introduction

    2. Organization of Inhibitor of Apoptosis Proteins

    3. Smac, XIAP, and Caspase-9: Structure and Mechanism

    4. Structure–Activity Relationships of Smac Mimetics

    5. Bivalency and Smac Mimetic Function

    6. Recently Described Smac Mimetics

    7. Preclinical and Clinical Evaluation

    8. Conclusion

    Chapter 14: Case History

    1. Introduction

    2. Halichondrin B

    3. Eribulin Drug Discovery Program

    4. From Discovery to Development

    5. Conclusion

    Chapter 15: Emerging New Therapeutics Against Key Gram-Negative Pathogens

    1. Introduction

    2. New Compounds from Known Classes

    3. Novel Compound Classes

    4. Conclusion

    Chapter 16: Hepatitis C Virus—Progress Toward Inhibiting the Nonenzymatic Viral Proteins

    1. Introduction

    2. HCV core (Capsid) Protein Inhibitors

    3. HCV Entry Inhibitors

    4. HCV p7 Inhibitors

    5. HCV NS4A Inhibitors

    6. HCV NS4B Inhibitors

    7. HCV NS5A Inhibitors

    8. HCV IRES Inhibitors

    9. Conclusion

    Chapter 17: The Emergence of Small-Molecule Inhibitors of Capsid Assembly as Potential Antiviral Therapeutics

    1. Introduction

    2. Capsid Assembly Inhibitors

    3. CA Inhibition via Host Factor Modulation

    4. Conclusion

    Chapter 18: Molecular Mechanism of Action (MMoA) in Drug Discovery

    1. Introduction-Molecular Mechanism of Action

    2. Molecular Descriptors

    3. Metric, Biochemical Efficiency

    4. Strategies for an Optimal MMoA

    5. Chemistry of Binding Kinetics

    6. Conclusions

    Chapter 19: Aryl Hydrocarbon Receptor (AhR) Activation

    1. Introduction

    2. Overview of the AhR

    3. Effects on Immune Cell Function

    4. Therapeutic Effects in Animal Models of Human Diseases

    5. Conclusion

    Chapter 20: Peptidyl Prolyl Isomerase Inhibitors

    1. Introduction

    2. Categories of Peptidyl Prolyl Isomerases

    3. Small-Molecule Inhibitors

    4. Macrocyclic Inhibitors

    5. Conclusion

    Chapter 21: MicroRNAs—Basic Biology and Therapeutic Potential

    1. Introduction

    2. MicroRNAs in Human Disease

    3. MicroRNAs as Potential Therapeutics

    4. Conclusion

    Chapter 22: Induced Pluripotent Stem Cells as Human Disease Models

    1. Introduction

    2. iPSC Technology

    3. iPSC Derivation and Production

    4. Differentiation—Problems and Promise

    5. Leads for Drug Discovery and Development

    6. Stem Cell Modulators

    7. Predictive Toxicology with iPSC

    8. In Vitro Clinical Trial

    9. Personalized Medicine: Patient Profiling for Optimal Drug Efficacy

    10. Conclusion and the Role of Small Molecule Chemistry

    Chapter 23: The Future of Drug Repositioning

    1. Introduction

    2. Perspectives of Drug Repositioning

    3. New Strategies Toward Drug Repositioning

    4. Case Studies of Drug Repositioning Strategies

    5. Future Directions of Drug Repositioning

    6. Conclusion

    Chapter 24: Deuterium in Drug Discovery and Development

    1. Introduction

    2. Deuterium Background

    3. Deuterium Safety and Pharmacology

    4. Deuterium-Containing Drugs

    5. Deuterated Drugs as Clinical Agents

    6. Patentability of Deuterated Drugs

    7. Conclusions

    Chapter 25: Drug-Induced Phospholipidosis

    1. Introduction

    2. Evolving Regulatory and Industry Views

    3. Screening Methods

    4. Examples of Project Responses to Finding PLD

    5. Conclusion

    Chapter 26: To Market, To Market—2010

    1. Alcaftadine (0.25%) (Ophthalmologic, Allergic Conjunctivitis)

    2. Alogliptin (Antidiabetic)

    3. Bilastine (Antiallergy)

    4. Cabazitaxel (Anticancer)

    5. Ceftaroline Fosamil (Antibacterial)

    6. Corifollitropin Alfa (Infertility)

    7. Dalfampridine (Multiple Sclerosis)

    8. Denosumab (Osteoporosis and Metastatic Bone Disease)

    9. Diquafosol (Ophthalmologic, Dry Eye)

    10. Ecallantide (Angioedema, Hereditary)

    11. Eribulin Mesylate (Anticancer)

    12. Fingolimod Hydrochloride (Multiple Sclerosis)

    13. Laninamivir Octanoate (Antiviral)

    14. Lurasidone (Antipsychotic)

    15. Mifamurtide (Anticancer)

    16. Peramivir (Antiviral)

    17. Roflumilast (Chronic Obstructive Pulmonary Disorder)

    18. Romidepsin (Anticancer)

    19. Sipuleucel-T (Anticancer)

    20. Tesamorelin Acetate (HIV Lipodystrophy)

    21. Ticagrelor (Antithrombotic)

    22. Vernakalant (Antiarrhythmic)

    23. Vinflunine Ditartrate (Anticancer)

    24. Zucapsaicin (Analgesic)

    Keyword Index, Volume 46

    Cumulative Chapter Titles Keyword Index, Volume 1–46

    Cumulative Nce introduction index, 1983–2010

    Cumulative NCE Introduction Index, 1983–2010 (by indication)

Product details

  • No. of pages: 624
  • Language: English
  • Copyright: © Academic Press 2011
  • Published: October 12, 2011
  • Imprint: Academic Press
  • Paperback ISBN: 9780123860095
  • eBook ISBN: 9780123860248

About the Series Editor

John Macor

Affiliations and Expertise

Neuroscience Discovery Chemistry, Bristol-Myers Squibb, USA

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