Analogue-based Drug Discovery II (PDF)

PART I GENERAL ASPECTS Optimizing Drug Therapy by Analogues Standalone Drugs Application of Molecular Modeling in Analogue-Based Drug Discovery Issues for the Patenting of Analogues PART II ANALOGUE CLASSES Dipeptidyl Peptidase IV Inhibitors for the Treatment of Type 2 Diabetes Phosphodiesterase 5 Inhibitors to Treat Erectile Dysfunction Rifamycins, Antibacterial Antibiotics and Their New Applications Monoterpenoid Indole Alkaloids, CNS Anticancer Drugs Anthracyclines, Optimizing Anticancer Analogues Paclitaxel and Epothilone Analogues, Anticancer Drugs Selective Serotonin Reuptake Inhibitors for the Treatment of Depression Muscarinic Receptor Antagonists in the Treatment of COPD beta-Adrenoceptor Agonists and Asthma PART III CASE HISTORIES Liraglutide, a GLP-1 Analogue to Treat Diabetes Eplerenone: Selective Aldosterone Antagonist Clevudine, to Treat Hepatitis B Viral Infection Rilpivirine, a Non-nucleoside Reverse Transcriptase Inhibitor to Treat HIV-1 Tipranavir, a Non-Peptidic Protease Inhibitor for Multi-drug Resistant HIV Lapatinib, an Anticancer Kinase Inhibitor Dasatinib, a Kinase Inhibitor to Treat Chronic Myelogenous Leukemia Venlafaxine and Desvenlafaxine, Selective Norepinephrine and Serotonin Reuptake Inhibitors to Treat Major Depressive Disorder

János Fischer is a Senior Research Scientist at Richter Plc., Budapest, Hungary. He received his MSc and PhD degrees in organic chemistry from the Eotvos University of Budapest under Professor A. Kucsman. Between 1976 and 1978, he was a Humboldt Fellow at the University of Bonn under Professor W. Steglich. He has worked at Richter Plc. since 1981 where he participated in the research and development of leading cardiovascular drugs in Hungary. His main interest is analogue based drug discovery. He is the author of some 100 patents and scientific publications. In 2004, he was elected as a Titular member of the Chemistry and Human Health Division of IUPAC. He received an honorary professorship at the Technical University of Budapest.

C. Robin Ganellin studied Chemistry at London University, receiving a PhD in 1958 under Professor Michael Dewar, and was a Research Associate at MIT with Arthur Cope in 1960. He then joined Smith Kline & French Laboratories in the UK and was one of the co inventors of the revolutionary drug, cimetidine (also known as Tagamet). In 1986, he was made a Fellow of the Royal Society and appointed to the SK&F Chair of Medicinal Chemistry at University College London, where he is now Professor Emeritus of Medicinal Chemistry. Professor Ganellin is co inventor of over 160 patents and has authored over 260 scientific publications. He was President of the Medicinal Chemistry Section of the IUPAC and is Chairman of the IUPAC Subcommittee on Medicinal Chemistry and Drug Development.

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