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Annual Reports in Medicinal Chemistry - 1st Edition - ISBN: 9780123747662, 9780080912141

Annual Reports in Medicinal Chemistry, Volume 44

1st Edition

Series Editor: John Macor
Paperback ISBN: 9780123747662
eBook ISBN: 9780080912141
Imprint: Academic Press
Published Date: 26th October 2009
Page Count: 736
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Table of Contents

1 Recent advances in the discovery of GSK-3 inhibitors and a

perspective on their utility for the treatment of Alzheimer’s


Robert G. Gentles, Shuanghua Hu,

and. Gene Dubowchik

2 Advances in the Development of Nitric Oxide Synthase Inhibitors

Shawn Maddaford, Subhash

Annendi, Jailall Remnauth, and

Suman Rakhit

3 Small Molecule Protein–Protein Interaction Inhibitors as

Therapeutic Agents for Neurodegenerative Diseases: Current

Progress and Future Hurdles

Simon Haydar and Warren Hirst

4 Case History: Chantix (varenicline tartrate) a Nicotinic Partial

Agonist Aid to Smoking Cessation

Jotham W. Coe, Hans Rollema and

Brian T. O’Neill

5 Case History on Tekturna® /Rasilez® (Aliskiren), a Highly

Efficacious Direct Oral Renin Inhibitor as a New Therapy for


Juergen Maibaum and David Feldman

6 Advances in Vasopressin Receptor Agonists and Antagonists Thomas Ryckmans

7 The Emergence of GPR119 Agonists as Anti-diabetic Agents Robert Jones

8 Non-peptide Ligands for the Gonadotropin Receptors Nicole van Straten, Marco Timmers

9 Recent Advances in Coagulation Serine Protease Inhibitors

Mimi Quan and Joanne Smallheer

10 Advances in the Discovery of Anti-Inflammatory FMS Inhibitors Mark Player and Carl Manthey

11 Recent Advances in the Discovery of CB2 Selective Agonists Jayant Thatte, Sangdon Han, and Rob Jones

12 Advances in the Discovery of Small Molecule JAK3 Inhibitors Stephen Wrobleski

13 Recent Advances in Adenosine Receptor (AR) Ligands in

Pulmonary Diseases

Jeff Zablocki and Rao Kalla

14 Recent Progress in the Development of Small Molecule Inhibitors

of Insulin-like Growth Factor Receptor (IGF-1R) Kinase Dinesh Vyas and Mark Wittman

15 Case History: Discovery of Ixabepilone (IXEMPRA[TM]), a First-inclass

Epothilone Analogue for Treatment of Metastatic Breast Cancer

Robert M. Borzilleri and Gregory D.

16 Hedgehog Signaling Pathway Inhibitors as Cancer Therapeutics Stefan Peuker and Karen Miller-Moslin

17 Emerging Therapies Based on Inhibitors of Phosphatidyl-Inositol-

3-Kinases (PI3Ks)

John M. Nuss, Amy Lew Tsuhako

and Neel K. Anand Exelixis

18 Anti-infective Activity of Artemisinin and its Semi-synthetic

Derivatives John G. D'Angelo

19 Recent Advances in the Inhibition of Bacterial Type II


Greg Bisacchi & Jacques Dumas

20 Progress Towards the Discovery and Development of Specifically

Targeted Inhibitors of Hepatitis C Virus

Nicholas A. Meanwell John F.

Kadow and Paul M. Scol

21 Inhibitors of Nuclear Hormone Receptor/Steroid Receptor

Coactivator Interactions

Terry Moore, John Katzenellenbogen

22 Safety Testing of Drug Metabolites Tom Thompson

23 A Path to Innovation: Gene Knockouts Model New Drug Action Brian Zambrowicz

24 Discovery of Novel Positron Emission Tomography (PET) Tracers Dennis McCarthy

25 The Use of Isotopically Labeled Compounds in Drug Discovery (Chad) Charles S. Elmore

26 Mechanism based inhibition of CYP3A4 and other cytochromes P450 Bernard Murray

27 Nonclinical Toxicogenomics in the Pharmaceutical Environment Bruce D. Car

28 To Market, To Market 2008 Shridhar Hegde and Michelle Schmidt



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.

Key Features

  • Covers findings related to cardiovascular, inflammation, and pulmonary diseases

    * Examines issues in oncology, from mTor inhibitors to drug targets

    * Incorporates up-to-date information on drug design and discovery, including delivery to market


medicinal, pharmaceutical, and organic chemists


No. of pages:
© Academic Press 2009
26th October 2009
Academic Press
Paperback ISBN:
eBook ISBN:

Ratings and Reviews

About the Series Editor

John Macor

Affiliations and Expertise

Neuroscience Discovery Chemistry, Bristol-Myers Squibb, USA