Edited by Janos
Fischer and C.
Wiley-VCH, 2006 [ISBN 3-527-31257-9]
The first authoritative overview of past and current strategies for
successful drug development by molecular modification of known leads.
This unique resource spans the important drug classes in most major
Analogue-based drug discovery is discussed among others,
for beta blockers, ACE inhibitors, steroids, opiates, stigmines, proton
pump inhibitors, platinum anti-cancer compounds and anti-infective quinolones.
Statistically, every second drug is an analogue, and their
market value amounts to two thirds of all drugs. Analogues are the most
successful way of inventing a new drug and they provide the required
improvements in drug therapy.
Case studies, by the respective inventors on selected
commercially successful drug analogues provide prime advice for new
drug development projects based on analogue modification.
The book includes a table of the most successful drug
analogues as based on the IMS ranking and compares them in terms of
chemical structure, mode of action, launch year and patent priority.
GENERAL ASPECTS OF ANALOGUE-BASED DRUG DISCOVERY
- Analogues as Means of Discovering New Drugs
- Drug Likeness and Analogue-Based Drug Discovery
- Privileged Structures and Analogue-based Drug Discovery
SELECTED EXAMPLES FROM THE ANALOGUE-BASED DRUG DISCOVERY
- Development of Anti-ulcer H2-Receptor Histamine Antagonists
- Case History Omeprazole-Esomeprazole
- Case History of Pantoprazole
- Optimizing the Clinical Pharmacologic Properties of the HMG-CoA Reductase
- Optimizing antihypertensive Therapy by Angiotensin Receptor Blockers
- Optimizing Antihypertensive Therapy by Angiotensin-Converting Entyme
- Case Study of Lacidinpine in the Research of New Calcium Antagonists
- Selective Beta-Adrenergic Receptor blocking Agents
- Case Study: "Esmolol Stat"
- Development of Organic Nitrates for Coronary Heart Disease
- Development of Opioid Receptor Ligands
- Structural Analogues of Clozapine
- Quinolone antibiotics - The Development of Moxifloxiacin
- The Development of Bisphosphonates as Drugs
- Cisplatin and Its Analogues for Cancer Chemotherapy
- The History of Drospirenone
- Histamine H1 Blockers; from Relative Failures to Blockbusters within
Series of Anaologues
- Corticosteroids: form Natural Products to Useful Analogues
TABLE OF ANALOGUES
(classified according to chemical analogy, mode of action, therapeutic
area and patent priority)
Approx 600 pages. Hardcover
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