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Contents I. Central Nervous System Diseases Ii CONTENTS CONTRIBUTORS xi PREFACE xiii CORRIGENDUM xv I. CENTRAL NERVOUS SYSTEM DISEASES Section Editor: David Wustrow, Pfizer Global Research & Development, Ann Arbor, Michigan 1. Neuronal Nicotinic Acetylcholine Receptor Modulators: Recent Advances and Therapeutic Potential 3 Scott R. Breining, Anatoly A. Mazurov and Craig H. Miller, Targacept, Inc., 200 East First Street, Suite 300, Winston-Salem, NC 27101 2. Recent Advances in Selective Serotonergic Agents 17 Wayne E. Childers, Jr. and Albert J. Robichaud, Chemical & Screening Sciences, Wyeth Research, CN 8000, Princeton, NJ 08543 3. BACE Inhibitors for the Treatment of Alzheimer’s Disease 35 Ellen W. Baxter and Allen B. Reitz, Johnson & Johnson Pharmaceutical Research and Development LLC, Spring House, PA 19477-0776 4. Positron Emission Tomography Agents for Central Nervous System Drug Development Applications 49 N. Scott Masona and Chester A. Mathisa,b,c, aDepartments of Radiology, bPharmacology and cPharmaceutical Sciences, University of Pittsburgh, Pittsburgh, PA, 15213, USA II. CARDIOVASCULAR AND METABOLIC DISEASES Section Editor: Andrew Stamford, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, New Jersey 5. Emerging Topics in Atherosclerosis: HDL Raising Therapies 71 Peter J. Sinclair, Merck Research Laboratories, Rahway, NJ 07065, USA v vi Contents 6. Small Molecule Anticoagulant/Antithrombotic Agents 85 Robert M. Scarborough, Anjali Pandey and Xiaoming Zhang, Portola Pharmaceuticals, Inc., 270 East Grand Ave., Suite 22, South San Francisco, CA 94080, USA 7. CB1 Cannabinoid Receptor Antagonists 103 Francis Barth, Sanofi-aventis, 371 rue du Professeur Blayac 34184 Montpellier Cedex 04, France 8. Melanin-Concentrating Hormone as a Therapeutic Target 119 Mark D. McBriar and Timothy J. Kowalski, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033 9. Glycogen Synthase Kinase-3 (GSK-3): A Kinase with Exceptional Therapeutic Potential 135 John W. Benbow, Christopher J. Helal, Daniel W. Kung and Travis T. Wager, Pfizer Global Research and Development, Groton/ New London Laboratories, Pfizer Inc, Eastern Point Road, Groton, Connecticut, USA 06340 10. Inhibitors of Dipeptidyl Peptidase 4 149 Stephen L. Gwaltney, II and Jeffrey A. Stafford, Takeda San Diego, Inc., 10410 Science Center Drive, San Diego, CA 92121 11. Recent Advances in Therapeutic Approaches to Type 2 Diabetes 167 Ramakanth Sarabu and Jefferson Tilley, Hoffmann-La Roche, Inc, Nutley, NJ 07110 III. INFLAMMATORY, PULMONARY, AND GASTROINTESTINAL DISEASES Section Editor: Mark G. Bock, Merck Research Laboratories, West Point, Pennsylvania 12. The TRPV1 Vanilloid Receptor: A Target for Therapeutic Intervention 185 J. Guy Breitenbucher, Sandra R. Chaplan and Nicholas I. Carruthers, Johnson & Johnson Pharmaceutical Research and Development L.L.C. San Diego, CA 92121 13. Leukotriene Biosynthesis Inhibitors 199 Richard W. Friesena and Denis Riendeaub, aDepartments of Medicinal Chemistry and bBiochemistry and Molecular Biology, Merck Frosst Centre for Therapeutic Research, Kirkland, Quebec, Canada H9H 3L1 Contents vii 14. CXCR3 Antagonists 215 Julio C. Medina, Michael G. Johnson and Tassie L. Collins, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA 15. PDE7 Inhibitors: Chemistry and Potential Therapeutic Utilities 227 Fabrice Vergne, Patrick Bernardelli and Eric Chevalier, Pfizer Global Research and Development, Sandwich Laboratories, Sandwich, CT13 9NJ, UK IV. CANCER AND INFECTIOUS DISEASES Section Editor: Jacob J. Plattner, Anacor Pharmaceuticals, Palo Alto, California 16. Inhibitors of Anti-apoptotic Proteins for Cancer Therapy 245 Steven W. Elmorea, Thorsten K. Oostb and Cheol-Min Parka, aGlobal Pharmaceutical Research & Development, Abbott Laboratories, Abbott Park, IL 60064, USA and bGlobal Pharmaceutical Research & Development, Abbott GmbH & Co. KG, Knollstrasse, 67061 Ludwigshafen, Germany 17. AKT Kinase and Hsp90 Inhibitors as Novel Anti-cancer Therapeutics 263 Timothy Machajewski, Xiaodong Lin, A.B. Jefferson and Zhenhai Gao, Chiron Corporation, 4560 Horton Street, Emeryville, CA 94608, USA 18. Novel Strategies in HIV Prevention – Development of Topical Microbicides 277 Brigitte E. Beer and James E. Cummins, Jr., Southern Research Institute, 431 Aviation Way, Frederick, MD 21701, USA 19. New Developments in HIV Therapeutics 291 Terry A. Lylea and Michael D. Millerb, Departments of aMedicinal Chemistry and bAntiviral Research, Merck Research Laboratories, PO Box 4, West Point, PA 19486, USA 20. Antibacterials for the Treatment of Gram Positive Infections 301 James B. McAlpinea and Morimasa Yagisawab, aEcopia BioSciences Inc., 7290 Frederick Banting, Saint Laurent, Que´bec H4S 2A1, Canada and bJapan Antibiotics Research Association, 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan 21. Progress on New Therapeutics for Fungal Nail Infections 323 Stephen J. Bakera, Xiaoying Huib and Howard I. Maibachb, aAnacor Pharmaceuticals, 1060 East Meadow Circle, Palo Alto, CA 94303, USA and bDepartment of Dermatology, Surge Building, Room 110, 90 Medical Center Way, University of California at San Francisco, San Francisco, CA, 94143, USA viii Contents V. TOPICS IN BIOLOGY Section Editor: John P. Overington, Inpharmatica, London, United Kingdom 22. Chemical Tools for Indications Discovery 339 Andrew Hopkins1, Jerry Lanfear1, Christopher Lipinski2 and Lee Beeley1,3, 1Pfizer Global Research and Development, Ramsgate Road, Sandwich, Kent, United Kingdom CT13 9NJ, UK, 2Pfizer Global Research and Development, Eastern Point Road, Groton, Connecticut 06340, USA and 3PharmaMatters, Ramsgate, Kent, UK 23 Structural Genomics and Drug Discovery Aled Edwards1, Judd Berman2 and Michael Sundstrom3, 1Structural Genomics Consortium, University of Toronto, 349 112 College St, Toronto, Ontario, Canada, 2Affinium Pharmaceuticals, 100 University Ave, Toronto, Ontario, Canada and 3Structural Genomics Consortium, University of Oxford, Botnar Research Centre Oxford OX3 7LD UK VI. TOPICS IN DRUG DESIGN AND DISCOVERY Section Editor: Manoj C. Desai, Gilead Sciences Inc., Foster City, California 24. G-Protein Coupled Receptor Inverse Agonists: Identification, Pharmacological Relevance and Functional Assays 373 Bertrand L. Chenard, George D. Maynard, Robbin M. Brodbeck and James E. Krause, Neurogen Corporation, 35 Northeast Industrial Road, Branford, CT 06405, USA 25. The Utility of Metabonomics for Drug Safety Assessment 387 Marielle Delnomdedieu and Richard P. Schneider, Pfizer Global Research and Development, Worldwide Safety Sciences, Metabonomics Laboratory, Eastern Point Road, Groton, CT 06340, USA 26. Computational Prediction of Blood-brain Barrier Permeation 403 David E. Clark, Argenta Discovery Ltd., 8/9 Spire Green Centre, Flex Meadow, Harlow, Essex, CM19 5TR, UK 27. Pharmacogenetics and Drug Development 417 Hans Reiser, Gilead Sciences, 333 Lakeside Drive, Foster City, CA 94404, USA Contents ix VII. TRENDS AND PERSPECTIVES Section Editor: Annette M. Doherty, Pfizer Global Research & Development, Sandwich Laboratories, Sandwich, Kent, United Kingdom. 28. Trends in Pharmaceutical Innovation 431 Esther F. Schmid and Dennis A. Smith, Pfizer Global Research & Development, Sandwich Laboratories, Sandwich, Kent, United Kingdom 29. To Market, To Market—2004 443 Shridhar Hegde and Michelle Schmidt, Pfizer Global Research & Development, St. Louis, Missouri 63017 COMPOUND NAME, CODE NUMBER AND SUBJECT INDEX, 475 VOLUME 40 CUMULATIVE CHAPTER TITLES KEYWORD INDEX, 485 VOLUMES 1–40 CUMULATIVE NCE INTRODUCTION INDEX, 1983–2004 503 CUMULATIVE NCE INTRODUCTION INDEX, 1983–2004, 521 BY INDICATION CONTRIBUTORS Baker Stephen J. 323 Lin Xiaodong 263 Barth Francis 103 Lipinski Christopher 339 Baxter Ellen W. 35 Lyle Terry A. 291 Beeley Lee 339 Machajewski Timothy 263 Beer Brigitte E. 277 Maibach Howard I. 323 Benbow John W. 135 Mason Scott N. 49 Berman Judd 349 Mathis, Chester A. 49 Bernardelli Patrick 227 Maynard George D. 373 Breining Scott R. 3 Mazurov Anatoly A. 3 Breitenbucher Guy J. 185 McAlpine James B. 301 Brodbeck Robbin M. 373 McBriar Mark D. 119 Carruthers Nicholas I. 185 Medina Julio C. 215 Chaplan Sandra R. 185 Miller Craig H. 3 Chenard Bertrand L. 373 Miller Michael D. 291 Chevalier Eric 227 Oost Thorsten K. 245 Childers, Wayne E., Jr. 17 Pandey Anjali 85 Clark David E. 403 Park Cheol-Min 245 Collins Tassie L. 215 Reiser Hans 417 Cummins James E. Jr. 277 Reitz Allen B. 35 Delnomdedieu Marielle 387 Riendeau Denis 199 Edwards Aled 349 Robichaud Albert J. 17 Elmore Steven W. 245 Sarabu Ramakanth 167 Friesen Richard W. 199 Scarborough Robert M. 85 Gao Zhenhai 263 Schmid Esther F. 431 Gwaltney Stephen L., II 149 Schmidt Michelle 443 Hegde Shridhar 443 Schneider Richard P. 387 Helal Christopher J. 135 Sinclair Peter J. 71 Hopkins Andrew 339 Smith Dennis A. 431 Hui Xiaoying 323 Stafford Jeffrey A. 149 Jefferson A.B. 263 Sundstrom Michael 349 Johnson Michael G. 215 Tilley Jefferson 167 Kowalski Timothy J. 119 Vergne Fabrice 227 Krause James E. 373 Wager Travis T. 135 Kung Daniel W 135 Yagisawa Morimasa 301 Lanfear Jerry 339 Zhang Xiaoming 85 xi PREFACE Annual Reports in Medicinal Chemistry continues to focus on providing 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. Volume 40 mostly retains the familiar format of previous volumes, this year with 29 chapters. Sections I–IV are disease-oriented and generally report on
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