Introduction.

List of Contributors.

Abbreviations.

PART I: GENERAL ASPECTS OF ANALOGUE-BASED DRUG DISCOVERY.

1. Analogues as a Means of Discovering New Drugs.

2. Drug Likeness and Analogue-Based Drug Discovery.

3. Privileged Structures and Analog-Based Drug Discovery.

PART II: SELECTED EXAMPLES FROM THE ANALOGUE-BASED DRUG DISCOVERIES.

1. Development of Anti-Ulcer H2-Receptor Histamine Antagonists.

2. Esomeprazole in the Framework of Proton-Pump Inhibitor Development.

3. The Development of a New Proton-Pump Inhibitor: The Case History of Pantoprazole.

4. Optimizing the Clinical Pharmacologic Properties of the HMG-CoA Reductase Inhibitors.

5. Optimizing Antihypertensive Therapy by Angiotensin Receptor Blockers.

6. Optimizing Antihypertensive Therapy by Angiotensin-Converting Enzyme Inhibitors.

7. Case Study of Lacidipine in the Research of New Calcium Antagonists.

8. Selective Beta-Adrenergic Receptor-Blocking Agents.

9. Case Study: "Esmolol Stat".

10. Development of Organic Nitrates for Coronary Heart Disease.

11. Development of Opioid Receptor Ligands.

12. Stigmines.

13. Structural Analogues of Clozapine.

14. Quinolone Antibiotics: The Development of Moxifloxacin.

15. The Development of Bisphosphonates as Drugs.

16. Cisplatin and its Analogs for Cancer Chemotherapy.

17. The History of Drospirenone.

18. Histamine H1 Blockers: From Relative Failures to Blockbusters Within Series of Analogues.

19. Corticosteroids: From Natural Products to Useful Analogues.

PART III: TABLE OF SELECTED ANALOGUE CLASSES.

Index.