Annual Reports in Medicinal Chemistry, Volume 48

1st Edition

Serial Editors: Manoj Desai
Paperback ISBN: 9780124171503
eBook ISBN: 9780124171510
Imprint: Academic Press
Published Date: 8th October 2012
Page Count: 672
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Table of Contents



Personal Essays

Chapter One. Challenges in Drug Discovery at Schering–Plough Research Institute: A Personal Reflection




Chapter Two. My Perspective on Time, Managers—and Scientific Fun

1 Controlling Your Scientific Life: Time Management

2 Foster Innovation with Scientific Fun

3 A Good Manager is a Scientist’s Best Friend


Chapter Three. A Career in Medicinal Chemistry—A Journey in Drug Discovery


1 Early Days in Nucleoside, Nucleotide, and Nucleic Acid Chemistry

2 Antivirals

3 Elastase Inhibitors

4 Substance P Antagonists and the Discovery of Aprepitant and Fosaprepitant

5 Hypoglycemic Agents and the Discovery of Sitagliptin

6 Conclusions


Section 1: Central Nervous System Diseases

Chapter Four. Selective Inhibitors of PDE2, PDE9, and PDE10: Modulators of Activity of the Central Nervous System


1 Introduction

2 Phosphodiesterase (PDE) Structures

3 PDE2 Inhibitors and Dual PDE2 + PDE10 Inhibitors

4 PDE9 Inhibitors

5 PDE10 Inhibitors

6 Conclusions


Chapter Five. Beyond Secretases: Kinase Inhibitors for the Treatment of Alzheimer’s Disease


1 Introduction

2 Inhibitors of Dual-Specificity Kinases

3 Inhibitors of Serine–Threonine Kinases

4 Conclusions


Chapter Six. Orexin Receptor Antagonists in Development for Insomnia and CNS Disorders


1 Introduction

2 Clinical Programs

3 Preclinical Programs

4 Potential Indications Beyond Sleep

5 Concluding Remarks


Section 2: Cardiovascular and Metabolic Diseases

Chapter Seven. Discovery an


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

  • Annual Reports in Medicinal Chemistry provides timely and critical reviews and this volume covers important topics such as drug Discovery, Idiopathic Pulmonary Fibrosis and Neuraminidase Inhibitors


medicinal, pharmaceutical, and organic chemists


No. of pages:
© Academic Press 2013
Academic Press
eBook ISBN:
Paperback ISBN:


"This series is one of the very few annual publications which justify the title of an absolute must for the pharmacologist, chemist, or physician who is interested in the chemistry of drug development." --Enzymeologia

About the Serial Editors

Manoj Desai Serial Editor

Dr. Manoj Desai began his career in the pharmaceutical industry at Pfizer Inc, Central Research Division, Groton, CT (1986-1994) before moving to Chiron Corporation (1994-2003) as Director of medicinal chemistry; he was promoted to Vice President, lead discovery and medicinal chemistry (2000). In October 2003, he was appointed Vice President of medicinal chemistry at Gilead Sciences. At Pfizer, he was responsible for the medicinal chemistry efforts that lead to the discovery of oral Substance P antagonist CP-99994 which became the basis for the discovery of the new anti-emetics. At Chiron he formulated macrobead technology for the synthesis and screening of compound libraries for HTS and built the medicinal chemistry department with focus on kinase inhibitors. At Gilead, he was an active proponent to develop a pharmacoenhancer devoid of antiviral activity to improve the pharmacokinetics of integrase inhibitor elvitegravir. These efforts led to the discovery of Cobicistat which is one of components of StribildTM that was approved by FDA in August 2012 for the treatment of HIV infection. He is co-inventor on patents of Cobicistat (US 8,148,374), StribildTM and Ledipasvir (US 8,273,341; Phase III). Furthermore, his group at Gilead has advanced numerous compounds into clinical development for the treatment of antiviral diseases, cancer and cardiovascular diseases. Dr. Desai obtained Ph.D. in organic chemistry from the M.S. University of Baroda in 1981 working with Dr. Sukh Dev and then carried out post-doctoral fellowships at Purdue University working with Professor Herbert C. Brown (19981-1983) and at Harvard University with Professor Elias J. Corey (1983-1986). During his postdoctoral studies, he worked on natural product isolation, development of asymmetric synthetic methods using organoboranes and total synthesis of complex natural products such as retigeranic acid, -trans bergamotene and ginkgolide B. He has co-authored >60 publications in peer revie

Affiliations and Expertise

Gilead Sciences, Inc., Foster City, CA, USA