Annual Reports in Medicinal Chemistry: Volume 49

ISBN-13: 9780128001677 / Angielski / Miękka / 2014 / 636 str.

Manoj C. Desai

Opis

Annual Reports in Medicinal Chemistry provides timely and critical reviews of important topics in medicinal chemistry with an emphasis on emerging topics in the biological sciences that are expected to provide the basis for entirely new future therapies.

• Reviews on hot topics of interest in small molecule drug discovery heavily pursued by industrial research organizations
• Provides preclinical information in the context of chemical structures
• Knowledgeable section editors who evaluate invited reviews for scientific rigor

Spis treści

1. A Personal Essay: My Experiences in the Pharmaceutical Industry
2. Adventures in Medicinal Chemistry - A Career in Drug Discovery
3. Natural and Synthetic Neuroactive Steroid (NAS) Modulators of GABA_A and NMDA Receptors
4. Development of LRRK2 Kinase Inhibitors for Parkinson's Disease
5. Stimulating Neurotrophin Receptors in the Treatment of Neurodegenerative Disorders
6. Small Molecule Modulators of GPR40 (FFA1)
7. Recent Advances in the Development of P2Y₁₂ Receptor Antagonists as Antiplatelet Agents
8. Current Approaches to the Treatment of Atrial Fibrillation
9. Advances in the Discovery of Small Molecule IRAK4 Inhibitors
10. H₄ Receptor Antagonists and Their Potential Therapeutic Applications
11. Urate Crystal Deposition Disease and Gout - New Therapies for an Old Problem
12. p53 - MDM2 and MDMX Antagonists
13. Modulators of Atypical Protein Kinase C as Anticancer Agents
14. Advancement of Cell Wall Inhibitors in Mycobacterium Tuberculosis
15. Nucleosides and Nucleotides for the Treatment of Viral Diseases
16. Advances in Inhibitors of Penicillin Binding Proteins and ß-lactamases as Antibacterial Agents
17. Tumor Microenvironment as Target in Cancer Therapy
18. Novel Screening Paradigms for the Identification of Allosteric Modulators and /or Biased Ligands for Challenging G-Protein-Coupled Receptors (GPCRs)
19. Mer Tyrosine Kinase Receptor: Therapeutic Opportunities in Oncology, Virology and Cardiovascular Indications
20. Disease Modifying Agents for the Treatment of Cystic Fibrosis
21. Advancements in Stapled Peptide Drug Discovery and Development
22. Cytochrome P450 Enzyme Metabolites in Lead Discovery and Development
23. Case History: Forxiga^TM (Dapagliflozin), a Potent Selective SGLT2 Inhibitor for Treatment of Diabetes
24. Case History: Kalydeco® (VX-770, Ivacaftor), a CFTR Potentiator for the Treatment of Patients with Cystic Fibrosis and the G551D-CFTR Mutation
25. Case History: Xeljanz^TM (Tofacitinib Citrate), A First-In-Class Janus Kinase (JAK) Inhibitor for the Treatment of Rheumatoid Arthritis
26. New Chemical Entities Entering Phase III Trials in 2013
27. To Market, To Market - 2013

O autorze

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”.