Annual Reports in Medicinal Chemistry

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 reviewed journals and is an inventor on >25 issued patents. Furthermore, Dr. Desai is Editor-in-Chief for Annual Reports in Medicinal chemistry (2012-current), and have co-edited Comprehensive Medicinal Chemistry II (volume 7). In 2013, he co-edited book titled “Successful Strategies for the Discovery of Antiviral Drugs”.

Challenges in Drug Discovery at Schering-Plough Research Institute: A Personal Reflection
My Perspective on Time, Managers—and Scientific Fun
A Career in Medicinal Chemistry - A Journey in Drug Discovery
Selective Inhibitors of PDE2, PDE9 and PDE10 - Modulators of Activity of the Central Nervous System
Beyond Secretases: Kinases Inhibitors for the Treatment of Alzheimer’s Disease
Orexin Receptor Antagonists in Development for Insomnia and CNS Disorders
Discovery and Development of Prolylcarboxypeptidase (PRCP) Inhibitors for Cardiometabolic Disorders
Molecular Targeting of Imaging and Drug Delivery Probes in Atherosclerosis
Oral GLP-1 Modulators for the Treatment of Diabetes
Recent Advances in the Discovery and Development of CCR1 Antagonists
Emerging Targets for the Treatment of Idiopathic Pulmonary Fibrosis
Targeting the Nuclear Hormone Receptor RORgt for the Treatment of Autoimmune and Inflammatory Disorders
Recent Advances in Small-Molecule Modulation of Epigenetic Targets: Discovery and Development of Histone Methyltransferase- and Bromodomain Inhibitors
Inhibition of Ubiquitin Proteasome System Enzymes for Anticancer Therapy
Targeting Protein–Protein Interactions to Treat Cancer?Recent Progress and Future Directions
Recent Progress in the Discovery of Neuraminidase Inhibitors as Anti-influenza Agents
Novel Therapeutics in Discovery and Development for Treatment of Chronic HBV Infection
Special Challenges to the Rational Design of Antibacterial Agents
Recent Advances in Small Molecule Target Identification Methods
Neuroinflammation in Mood Disorders: Mechanisms and Drug Targets
Inhibitors of hERG Channel Trafficking—A Cryptic Mechanism For QT Prolongation
Recent Progress in Small-Molecule Agents Against Age-Related Macular Degeneration
Synthetic Macrocycles in Small-Molecule Drug Discovery
Glossary of Terms Used in Medicinal Chemistry Part II (IUPAC Recommendations 2011)
Case History: XalkoriTM (Crizotinib), a Potent and Selective Dual Inhibitor of MET and ALK for Cancer Treatment
Case History: Vemurafenib, a Potent, Selective, and First-in-Class Inhibitor of Mutant BRAF for the Treatment of Metastatic Melanoma
New Chemical Entities Entering Phase III Trials in 2012 28. To Market, to Market—2012