János Fischer & C. Robin Ganellin 
Analogue-based Drug Discovery II [PDF ebook] 

Traditionelle und brandneue Strategien für die Entwicklung von Analogwirkstoffen stehen im Mittelpunkt dieses Bandes, der seinen Vorgänger deutlich erweitert: Neun Klassen von Analoga kommen hinzu, dazu acht Fallstudien aus einer breiten Palette von Substanzklassen und therapeutischen Einsatzgebieten.

Innehållsförteckning

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

Om författaren

János Fischer is a Senior Research Scientist at Richter Plc., Budapest, Hungary. He received his MSc and Ph D 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 Ph D 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.