Annual Reports in Medicinal Chemistry: Volume 47

Klappentext 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. Zusammenfassung Provides critical reviews of important topics in medicinal chemistry together with an emphasis on topics in the biological sciences! which are expected to provide the basis for entirely new future therapies. Inhaltsverzeichnis 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 François P. Bischoff mGluR2 Activators and mGluR5 Blockers Advancing in the Clinic for Major CNS Disorders Sylvain Célanire, 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 ...

Zusammenfassung
Provides critical reviews of important topics in medicinal chemistry together with an emphasis on topics in the biological sciences, which are expected to provide the basis for entirely new future therapies.

Inhalt

Personal Essay

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

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2. My Path in Seeking New Medicines*Peter R. Bernstein

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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: 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

   ---

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

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

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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

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24. 3D Cell Cultures: Mimicking in Vivo Tissues for Improved Predictability in Drug Discovery*Indira Padmalayam and Mark J. Suto

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

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26. Recent Advances in Wnt/b-Catenin Pathway Small Molecule Inhibitors*Daniel D. Holsworth and Stefan Krauss

    • ** VII. Topics in Drug Design …