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

disease

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

Hypertension

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

Topoisomerases

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