Main 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.

Contents:

Personal Essay

Reflections on Medicinal Chemistry at Merck, West Point
Paul S. Anderson

My Path in Seeking New Medicines
Peter R. Bernstein

Tales of Drug Discovery
M. Ross Johnson

I. Central Nervous System Diseases

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

Recent Developments in Targeting Neuroinflammation in Disease
Allen T. Hopper, Brian M. Campbell, Henry Kao, Sean A. Pintchovski and Roland G. W. Staal

Secretase Inhibitors and Modulators as a Disease Modifying Approach Against Alzheimer's Disease
Harrie J. M. Gijsen and Francois P. Bischoff

mGluR2 Activators and mGluR5 Blockers Advancing in the Clinic for Major CNS Disorders
Sylvain Celanire, Guillaume Duvey, Sonia Poli and Jean-Philippe Rocher

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

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

Case History: EliquisTM (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

AMPK Activation in Health and Disease
Iyassu K. Sebhat and Robert W. Myers

Type-2 Diabetes and Associated Co-Morbidities as an Inflammatory Syndrome
Juan C. Jaen, Jay P. Powers and Tim Sullivan

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

Recent Advances in the Discovery and Development of Sphingosine-1-Phosphate-1 Receptor Agonists
Alaric J. Dyckman

Bifunctional Compounds for the Treatment of COPD
Gary Phillips and Michael Salmon

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

Nanotechnology Therapeutics in Oncology - Recent Developments and Future Outlook
Paul F. Richardson

Small-Molecule Antagonists of Bcl-2 Family Proteins
Sean P. Brown and Joshua P. Taygerly

Notch Pathway Modulators as Anti-Cancer Chemotherapeutics
Vibhavari Sail and M. Kyle Hadden

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

Recent Advances in the Discovery of Dengue Virus Inhibitors
Jeremy Green, Upul Bandarage, Kate Luisi and Rene Rijnbrand

Non Fluoro-Quinolone Based Inhibitors of Mycobacterial Type II Topoisomerase as Potential Therapeutic Agents for TB
Pravin S. Shirude and Shahul Hameed

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

Antibody-Drug Conjugates for Targeted Cancer Therapy
Victor S. Goldmacher, Thomas Chittenden, Ravi V. J. Chari, Yelena V. Kovtun and John M. Lambert

3D Cell Cultures: Mimicking in Vivo Tissues for Improved Predictability in Drug Discovery
Indira Padmalayam and Mark J. Suto

Virally Encoded G Protein-Coupled Receptors: Overlooked Therapeutic Opportunities?
Nuska Tschammer

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

Targeted Covalent Enzyme Inhibitors
Mark C. Noe and Adam M. Gilbert

Drug Design Strategies for GPCR Allosteric Modulators
P. Jeffrey Conn, Scott D. Kuduk and Dario Doller

Progress in the Development of Non-ATP Competitive Protein Kinase Inhibitors for Oncology
Campbell McInnes

VIII. Trends

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

New Chemical Entities Entering Phase III Trials in 2011
Gregory T. Notte

To Market, To Market - 2011 Joanne Bronson, Murali Dhar, William Ewing and Nils Lonberg