Analogue-based drug discovery

著者

• Fischer, János
• Ganellin, C. R. (C. Robin)
• Rotella, David P.

書誌事項

Analogue-based drug discovery

edited by János Fischer and C. Robin Ganellin

Wiley-VCH, c2006-

• [1]
• 2
• 3

タイトル別名

Analogue based drug discovery

注記

(Analogue-based drug discovery 3) edited by: János Fischer, C. Robin Ganellin, David P. Rotella

Includes bibliographical references and index

内容説明・目次

巻冊次

[1] ISBN 9783527312573

内容説明

The first authoritative overview of past and current strategies for successful drug development by analog generation, this unique resource spans all important drug classes and all major therapeutic fields, including histamine antagonists, ACE inhibitors, beta blockers, opioids, quinolone antibiotics, steroids and anticancer platinum compounds. Of the 19 analog classes presented in detail, 9 are described by the scientists who discoverd them. The book includes a table of the most successful drug analogs as based on the IMS ranking and compares them in terms of chemical structure, mode of action and patentability.

目次

Introduction GENERAL ASPECTS OF ANALOGUE-BASED DRUG DISCOVERY Analogues as a Means of Discovering New Drugs Drug Likeness and Analogue-Based Drug Discovery Privileged Structures and Analog-Based Drug Discovery SELECTED EXAMPLES FROM THE ANALOGUE-BASED DRUG DISCOVERIES Development of Anti-Ulcer H2-Receptor Histamine Antagonists Esomeprazole in the Framework of Proton-Pump Inhibitor Development The Development of a New Proton-Pump Inhibitor: The Case History of Pantoprazole Optimizing the Clinical Pharmacologic Properties of the HMG-CoA Reductase Inhibitors Optimizing Antihypertensive Therapy by Angiotensin Receptor Blockers Optimizing Antihypertensive Therapy by Angiotensin-Converting Enzyme Inhibitors Case Study of Lacidipine in the Research of New Calcium Antagonists Selective Beta-Adrenergic Receptor-Blocking Agents Case Study: "Esmolol Stat" [1] Development of Organic Nitrates for Coronary Heart Disease Development of Opioid Receptor Ligands Stigmines Structural Analogues of Clozapine Quinolone Antibiotics: The Development of Moxifloxacin The Development of Bisphosphonates as Drugs Cisplatin and its Analogs for Cancer Chemotherapy The History of Drospirenone Histamine H1 Blockers: From Relative Failures to Blockbusters Within Series of Analogues Corticosteroids: From Natural Products to Useful Analogues

巻冊次

2 ISBN 9783527325498

内容説明

Born out of a project of the IUPAC's committee on Medicinal Chemistry and Drug Development, this reference addresses past and current strategies for successful drug analog development, extending the previously published volume by nine new analog classes and eight case studies. Like its precursor, this volume also contains a general section discussing universally applicable strategies for analog discovery and development. Spanning a wide range of therapeutic fields and chemical classes, the two volumes together constitute the first systematic approach to drug analog development. Of interest to virtually every researcher working in drug discovery and pharmaceutical chemistry.

目次

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

巻冊次

3 ISBN 9783527330737

内容説明

Most drugs are analogue drugs. There are no general rules how a new drug can be discovered, nevertheless, there are some observations which help to find a new drug, and also an individual story of a drug discovery can initiate and help new discoveries. Volume III is a continuation of the successful book series with new examples of established and recently introduced drugs. The major part of the book is written by key inventors either as a case study or a study of an analogue class. With its wide range across a variety of therapeutic fields and chemical classes, this is of interest to virtually every researcher in drug discovery and pharmaceutical chemistry, and -- together with the previous volumes -- constitutes the first systematic approach to drug analogue development.

目次

PREFACE PART I: General Aspects PIONEER AND ANALOGUE DRUGS Monotarget Drugs Dual-Acting Drugs Multitarget Drugs Summary COMPETITION IN THE PHARMACEUTICAL DRUG DEVELOPMENT Introduction Analogue-Based Drugs: Just Copies? How Often Does Analogue-Based Activity Occur? Insights from the GPCR Patent Space METABOLIC STABILITY AND ANALOGUE-BASED DRUG DISCOVERY Introduction Metabolism-Guided Drug Design Indirect Modulation of Metabolism by Fluorine Substitution Modulation of Low Clearance/Long Half-Life via Metabolism-Guided Design Tactics to Resolve Metabolism Liabilities Due to Non-CYP Enzymes Eliminating RM Liabilities in Drug Design Eliminating Metabolism-Dependent Mutagenicity Eliminating Mechanism-Based Inactivation of CYP Enzymes Identification (and Elimination) of Electrophilic Lead Chemical Matter Mitigating Risks of Idiosyncratic Toxicity via Elimination of RM Formation Case Studies on Elimination of RM Liability in Drug Discovery Concluding Remarks USE OF MACROCYCLES IN DRUG DESIGN EXEMPLIFIED WITH ULIMORELIN, A POTENTIAL GHRELIN AGONIST FOR GASTROINTESTINAL MOTILITY DISORDERS Introduction High-Throughput Screening Results and Hit Selection Macrocycle Structure - Activity Relationships PK - ADME Considerations Structural Studies Preclinical Evaluation Clinical Results and Current Status Summary PART II: Drug Classes THE DISCOVERY OF ANTICANCER DRUGS TARGETING EPIGENETIC ENZYMES Epigenetics DNA Methyltransferases 5-Azacytidine (Azacitidine, Vidaza) and 5-Aza-20-deoxycytidine (Decitabine, Dacogen) Other Nucleoside DNMT Inhibitors Preclinical Zinc-Dependent Histone Deacetylases Suberoylanilide Hydroxamic Acid (SAHA, Vorinostat, Zolinza) FK228 (Depsipeptide, Romidepsin, Istodax) Carboxylic Acid and Benzamide HDAC Inhibitors Prospects for HDAC Inhibitors Epigenetic Drugs - A Slow Start but a Bright Future THIENOPYRIDYL AND DIRECT-ACTING P2Y12 RECEPTOR ANTAGONIST ANTIPLATELET DRUGS Introduction Thienopyridines Direct-Acting P2Y12 Antagonists cyclopropylamino]-5-(propylthio)-3H-[1,2,3]triazolo[4,5-d]pyrimidin- 3-yl]-5-(2-hydroxyethoxy)cyclopentane-1,2-diol Summary SELECTIVE ESTROGEN RECEPTOR MODULATORS Introduction Tamoxifen Raloxifene Summary DISCOVERY OF NONPEPTIDE VASOPRESSIN V2 RECEPTOR ANTAGONISTS Introduction Peptide AVP Agonists and Antagonists Lead Generation Strategies Lead Generation Strategy-2, V2 Receptor Affinity Lead Optimization Reported Nonpeptide Vasopressin V2 Receptor Antagonist Compounds Conclusions THE DEVELOPMENT OF CYSTEINYL LEUKOTRIENE RECEPTOR ANTAGONISTS Introduction Scope of the Drug Discovery Effort on Leukotriene Modulators Synthetic Leukotriene Production and Benefits Derived from this Effort Bioassays and General Drug Discovery Testing Cascade Development of Antagonists - General Approaches Discovery of Zafirlukast Discovery of Montelukast Discovery of Pranlukast Comparative Analysis and Crossover Impact Postmarketing Issues Conclusions PART III: Case Studies THE DISCOVERY OF DABIGATRAN ETEXILATE Introduction Dabigatran Design Story Preclinical Pharmacology Molecular Mechanism of Action of Dabigatran Clinical Studies and Indications Summary THE DISCOVERY OF CITALOPRAM AND ITS REFINEMENT TO ESCITALOPRAM Introduction Discovery of Talopram Discovery of Citalopram Synthesis and Production of Citalopram The Pharmacological Profile of Citalopram Clinical Efficacy of Citalopram Synthesis and Production of Escitalopram The Pharmacological Profile of the Citalopram Enantiomers R-Citalopram's Surprising Inhibition of Escitalopram Binding Site(s) for Escitalopram on the Serotonin Transporter Future Perspectives on the Molecular Basis for Escitalopram?s Interaction with the SERT Clinical Efficacy of Escitalopram Conclusions TAPENTADOL - FROM MORPHINE AND TRAMADOL TO THE DISCOVERY OF TAPENTADOL Introduction The Discovery of Tapentadol The Preclinical and Clinical Profile of Tapentadol Summary NOVEL TAXANES: CABAZITAXEL CASE STUDY Introduction Cabazitaxel Structure - Activity Relationships and Chemical Synthesis Cabazitaxel Preclinical and Clinical Development Summary DISCOVERY OF BOCEPREVIR AND NARLAPREVIR: A CASE STUDY FOR ROLE OF STRUCTURE-BASED DRUG DESIGN A NEW-GENERATION URIC ACID PRODUCTION INHIBITOR: FEBUXOSTAT Introduction Xanthine Oxidoreductase - Target Protein for Gout Treatment Mechanism of XOR Inhibition by Allopurinol Development of Nonpurine Analogue Inhibitor of XOR: Febuxostat Mechanism of XOR Inhibition by Febuxostat Excretion of XOR Inhibitors Results of Clinical Trials of Febuxostat in Patients with Hyperuricemia and Gout Summary Added in proof INDEX

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詳細情報

• NII書誌ID(NCID): BA84998691
• ISBN:
  • 9783527312573
  • 9783527325498
  • 9783527330737
• LCCN: 2006296627
• 出版国コード: gw
• タイトル言語コード: eng
• 本文言語コード: eng
• 出版地: Weinheim
• ページ数/冊数: v.
• 大きさ: 25 cm
• 分類:
  • LCC : RM301.25
  • DC22 : 615.19
• 件名:
  • LCSH : Drug development