Chapter 6. The Development of a New Proton-Pump Inhibitor: The Case History of Pantoprazole

  1. Dr. János Fischer2,
  2. Prof. Dr. C. Robin Ganellin3
  1. Jörg Senn-Bilfinger,
  2. Ernst Sturm

Published Online: 22 MAY 2006

DOI: 10.1002/3527608001.ch6

Book Title

Analogue-based Drug Discovery

Analogue-based Drug Discovery

Additional Information

How to Cite

Senn-Bilfinger, J. and Sturm, E. (2006) The Development of a New Proton-Pump Inhibitor: The Case History of Pantoprazole, in Analogue-based Drug Discovery (eds J. Fischer and C. R. Ganellin), Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim, FRG. doi: 10.1002/3527608001.ch6

Editor Information

  1. 2

    Gedeon Richter Ltd., P.O. Box 27, H-1475 Budapest 10, Hungary

  2. 3

    University College London, Department of Chemistry, 20 Gordon Street, London WC1H OAJ, UK

Author Information

  1. Altana Pharma AG, Byk-Gulden-Str. 2, 78467 Konstanz, Germany

Publication History

  1. Published Online: 22 MAY 2006
  2. Published Print: 20 JAN 2006

ISBN Information

Print ISBN: 9783527312573

Online ISBN: 9783527608003

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Keywords:

  • analogue-based drug discovery;
  • new proton-pump inhibitor (PPI);
  • pantoprazole;
  • gastrointestinal research at Byk Gulden;
  • first PPI project candidates;
  • benzimidazole moiety;
  • mechanism of action of PPIs;
  • optimizing pyridine moiety;
  • internal competition with SK&F95601;
  • toxicological problems;
  • benefits

Summary

This chapter contains sections titled:

  • Introduction

  • History of Gastrointestinal Research at Byk Gulden

    • The Antacids and Cytoprotectives Projects and the Set-Up of In-Vivo Ulcer Models

    • Decision to Concentrate on Anti-Secretory Treatments and the Study of Compounds with an Unknown Mechanism of Action

  • Identification of the First PPI Project Candidates

    • Optimizing the Benzimidazole Moiety

    • Impact of the First PPI Project Compounds

  • Elucidation of the Mechanism of Action of PPIs

    • A Surprising Interrelationship Between Stability and Activity

    • Isolation and Identification of the Active Principle of the PPIs

  • Identification of Pantoprazole as a Candidate for Development

    • Optimizing the Pyridine Moiety and the First Synthesis of Pantoprazole

    • Selection Criteria

    • The Selection of Pantoprazole and Internal Competition with SK&F95601

    • Toxicological Problems: Project Development at Risk

    • Benefits of Pantoprazole for the Patient

    • Summary

  • Outlook on Further Developments

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