Annual Reports in Medicinal Chemistry Annual Reports in Medicinal Chemistry Series

Personal Essay

1. Reflections on Medicinal Chemistry at Merck, West Point

Paul S. Anderson

2. My Path in Seeking New Medicines

Peter R. Bernstein

3. Tales of Drug Discovery

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

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

Harrie J. M. Gijsen and François P. Bischoff

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

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

Kamalesh B. Ruppa, Dalton King and Richard Olson

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

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

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

10. AMPK Activation in Health and Disease

Iyassu K. Sebhat and Robert W. Myers

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

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

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

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

Alaric J. Dyckman

14. Bifunctional Compounds for the Treatment of COPD

Gary Phillips and Michael Salmon

15. Inflammatory Targets for the Treatment of Atherosclerosis

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

Paul F. Richardson

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

Sean P. Brown and Joshua P. Taygerly

18. Notch Pathway Modulators as Anti-Cancer Chemotherapeutics

Vibhavari Sail and M. Kyle Hadden

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

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

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

Pravin S. Shirude and Shahul Hameed

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

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

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

Indira Padmalayam and Mark J. Suto

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

Nuska Tschammer

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

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

Mark C. Noe and Adam M. Gilbert

28. Drug Design Strategies for GPCR Allosteric Modulators

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

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

Campbell M^cInnes

VIII. Trends

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

30. New Chemical Entities Entering Phase III Trials in 2011

Gregory T. Notte

31. To Market, To Market – 2011Joanne Bronson, Murali Dhar, William Ewing and Nils Lonberg

• Timely and critical reviews of important topics in medicinal chemistry