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Annual Reports in Medicinal Chemistry - 1st Edition - ISBN: 9780123860095, 9780123860248

Annual Reports in Medicinal Chemistry, Volume 46

1st Edition

Series Editor: John Macor
Paperback ISBN: 9780123860095
eBook ISBN: 9780123860248
Imprint: Academic Press
Published Date: 24th October 2011
Page Count: 624
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Table of Contents



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)


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.


medicinal, pharmaceutical, and organic chemists


No. of pages:
© Academic Press 2011
24th October 2011
Academic Press
Paperback ISBN:
eBook ISBN:


This series is one of the very few annual publications which justify the title of an absolute must for the pharmacologist, chemist, or physician who is interested in the chemistry of drug development." - ENZYMOLOGIA

Ratings and Reviews

About the Series Editor

John Macor

Affiliations and Expertise

Neuroscience Discovery Chemistry, Bristol-Myers Squibb, USA