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”.

• A Personal Essay: My Experiences in the Pharmaceutical IndustryAdventures in Medicinal Chemistry - A Career in Drug DiscoveryNatural and Synthetic Neuroactive Steroid (NAS) Modulators of GABAA and NMDA ReceptorsDevelopment of LRRK2 Kinase Inhibitors for Parkinson’s DiseaseStimulating Neurotrophin Receptors in the Treatment of Neurodegenerative DisordersSmall Molecule Modulators of GPR40 (FFA1)Recent Advances in the Development of P2Y12 Receptor Antagonists as Antiplatelet AgentsCurrent Approaches to the Treatment of Atrial FibrillationAdvances in the Discovery of Small Molecule IRAK4 InhibitorsH4 Receptor Antagonists and Their Potential Therapeutic ApplicationsUrate Crystal Deposition Disease and Gout - New Therapies for an Old Problemp53 - MDM2 and MDMX AntagonistsModulators of Atypical Protein Kinase C as Anticancer AgentsAdvancement of Cell Wall Inhibitors in Mycobacterium TuberculosisNucleosides and Nucleotides for the Treatment of Viral DiseasesAdvances in Inhibitors of Penicillin Binding Proteins and β-lactamases as Antibacterial AgentsTumor Microenvironment as Target in Cancer TherapyNovel Screening Paradigms for the Identification of Allosteric Modulators and /or Biased Ligands for Challenging G-Protein-Coupled Receptors (GPCRs)Mer Tyrosine Kinase Receptor: Therapeutic Opportunities in Oncology, Virology and Cardiovascular IndicationsDisease Modifying Agents for the Treatment of Cystic FibrosisAdvancements in Stapled Peptide Drug Discovery and DevelopmentCytochrome P450 Enzyme Metabolites in Lead Discovery and DevelopmentCase History: ForxigaTM (Dapagliflozin), a Potent Selective SGLT2 Inhibitor for Treatment of DiabetesCase History: Kalydeco® (VX-770, Ivacaftor), a CFTR Potentiator for the Treatment of Patients with Cystic Fibrosis and the G551D-CFTR MutationCase History: XeljanzTM (Tofacitinib Citrate), A First-In-Class Janus Kinase (JAK) Inhibitor for the Treatment of Rheumatoid ArthritisNew Chemical Entities Entering Phase III Trials in 2013To Market, To Market – 2013