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Annual Reports in Medicinal Chemistry

Series Editor:
  • John Macor, Neuroscience Discovery Chemistry, Bristol-Myers Squibb, USA

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.

Audience
medicinal, pharmaceutical, and organic chemists

Paperback, 472 Pages

Published: October 2012

Imprint: Academic Press

ISBN: 978-0-12-396492-2

Reviews

  • 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

Contents

  • Personal Essay

    1. Reflections on Medicinal Chemistry at Merck, West Point

      2. Paul S. Anderson

    2. My Path in Seeking New Medicines

      3. Peter R. Bernstein

    3. Tales of Drug Discovery

      4. M. Ross Johnson

      I. Central Nervous System Diseases

      Section Editor: Albert J. Robichaud; Sage Therapeutics, Inc. Cambridge, Massachusetts

    4. Recent Developments in Targeting Neuroinflammation in Disease

      5. Allen T. Hopper, Brian M. Campbell, Henry Kao, Sean A. Pintchovski and Roland G. W. Staal

    5. Secretase Inhibitors and Modulators as a Disease Modifying Approach Against Alzheimer’s Disease

      6. Harrie J. M. Gijsen and François P. Bischoff

    6. mGluR2 Activators and mGluR5 Blockers Advancing in the Clinic for Major CNS Disorders

      7. Sylvain Célanire, Guillaume Duvey, Sonia Poli and Jean-Philippe Rocher

    7. NMDA Antagonists of GluN2B Subtype and Modulators of GluN2A, GluN2C and GluN2D Subtypes - Recent Results and Developments

      8. Kamalesh B. Ruppa, Dalton King and Richard Olson

    8. Recent Advances in the Development of PET and SPECT Tracers for Brain Imaging

      9. Lei Zhang and Anabella Villalobos

      II. Cardiovascular and Metabolic Diseases

      Section Editor: Andy Stamford, Merck Research Laboratories, Kenilworth, New Jersey

    9. Case History: Eliquis TM (Apixaban), a Potent and Selective Inhibitor of Coagulation Factor Xa for the Prevention and Treatment of Thrombotic Diseases

      10. Donald J. P. Pinto, Pancras C. Wong, Robert M. Knabb and Ruth R. R. Wexler

    10. AMPK Activation in Health and Disease

      11. Iyassu K. Sebhat and Robert W. Myers

    11. Type-2 Diabetes and Associated Co-Morbidities as an Inflammatory Syndrome

      12. Juan C. Jaen, Jay P. Powers and Tim Sullivan

    12. Beyond PPARs & Metformin: New Insulin Sensitizers for the Treatment of Type 2 Diabetes

      13. Philip A. Carpino and David Hepworth

      III. Inflammatory Pulmonary and Gastrointestinal Diseases

      Section Editor: David S. Weinstein, Bristol-Myers Squibb R&D, Princeton, New Jersey

    13. Recent Advances in the Discovery and Development of Sphingosine-1-Phosphate-1 Receptor Agonists

      14. Alaric J. Dyckman

    14. Bifunctional Compounds for the Treatment of COPD

      15. Gary Phillips and Michael Salmon

    15. Inflammatory Targets for the Treatment of Atherosclerosis

      16. Robert O. Hughes, Alessandra Bartolozzi and Hidenori Takahashi

      IV. Oncology

      Section Editor: Shelli R. McAlpine, School of Chemistry, University of New South Wales, Sydney, Australia

    16. Nanotechnology Therapeutics in Oncology - Recent Developments and Future Outlook

      17. Paul F. Richardson

    17. Small-Molecule Antagonists of Bcl-2 Family Proteins

      18. Sean P. Brown and Joshua P. Taygerly

    18. Notch Pathway Modulators as Anti-Cancer Chemotherapeutics

      19. Vibhavari Sail and M. Kyle Hadden

    19. Anaplastic Lymphoma Kinase (ALK) Inhibitors for the Treatment of ALK-Positive Cancers

      20. Kazutomo Kinoshita, Nobuhiro Oikawa and Takuo Tsukuda

      V. Infectious Diseases

      Section Editor: John Primeau, Westford, Massachusetts

    20. Recent Advances in the Discovery of Dengue Virus Inhibitors

      21. Jeremy Green, Upul Bandarage, Kate Luisi and Rene Rijnbrand

    21. Non Fluoro-Quinolone Based Inhibitors of Mycobacterial Type II Topoisomerase as Potential Therapeutic Agents for TB

      22. Pravin S. Shirude and Shahul Hameed

    22. HCV Inhibition Mediated through the Nonstructural Protein 5A (NS5A) Replication Complex

      23. Robert Hamatake, Andrew Maynard and Wieslaw M. Kazmierski

      VI. Topics in Biology

      Section Editor: John Lowe, JL3Pharma LLC, Stonington, Connecticut

    23. Antibody-Drug Conjugates for Targeted Cancer Therapy

      24. Victor S. Goldmacher, Thomas Chittenden, Ravi V. J. Chari, Yelena V. Kovtun and John M. Lambert

    24. 3D Cell Cultures: Mimicking in Vivo Tissues for Improved Predictability in Drug Discovery

      25. Indira Padmalayam and Mark J. Suto

    25. Virally Encoded G Protein-Coupled Receptors: Overlooked Therapeutic Opportunities?

      26. Nuska Tschammer

    26. Recent Advances in Wnt/b-Catenin Pathway Small Molecule Inhibitors

      27. Daniel D. Holsworth and Stefan Krauss

      VII. Topics in Drug Design and Discovery

      Section Editor: Peter R. Bernstein, PhaRmaB LLC, Rose Valley, Pennsylvania

    27. Targeted Covalent Enzyme Inhibitors

      28. Mark C. Noe and Adam M. Gilbert

    28. Drug Design Strategies for GPCR Allosteric Modulators

      29. P. Jeffrey Conn, Scott D. Kuduk and Darío Doller

    29. Progress in the Development of Non-ATP Competitive Protein Kinase Inhibitors for Oncology

      30. Campbell M c Innes

      VIII. Trends

      Section Editor: Joanne Bronson, Bristol-Myers Squibb, Wallingford, Connecticut

    30. New Chemical Entities Entering Phase III Trials in 2011

      31. Gregory T. Notte

    31. To Market, To Market - 2011

       Joanne Bronson, Murali Dhar, William Ewing and Nils Lonberg

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