• PART I. INTRODUCTION Polypharmacology in Drug Discovery PART II. SELECTIVITY OF MARKTETED DRUGS Kinase Inhibitors New Indications for Marketed Drugs Discovery Technologies of New Indications PART III. FIXED-DOSE COMBINATIONS The Growing Market of Fixed-Dose Combinations PART IV. UNSELECTIVE DRUGS IN DRUG DISCOVERY The Growing Importance of Individualising Drugs Drug Discovery Strategies for the Generation of Multi-Target Ligands against Neglected Tropical Diseases Designing-In Approach The Linker Approach (Drug-Conjugates) Merged Multiple Ligands Pharmacophore Generation of Multiple Ligands Cellular Assays PART V. THERAPEUTIC AREAS FOR DESIGNED MULTIPLE LIGANDS 5HT Transporter-Based Multiple Ligands for Depression Multiple Ligands Targeting the Angiotensin System for Hypertension PPAR-Based Multiple Ligands for Metabolic Disease Antibiotics Multiple Ligands in Cancer Therapy Multiple Ligands in Neurodegenerative Diseases.
• (source: Nielsen Book Data)9783527674411 20180618

The book provides a current overview and comprehensive compilation for medicinal chemists that discusses the effects of aiming for multiple targets on the entire drug development process. The result is a broad survey of current and future strategies for drug selectivity in medicinal chemistry with theoretical but also practical aspects. Different strategies are presented and evaluated, such as various design approaches, merged multiple ligands, discovery technologies and a broad range of successful examples of unselective drugs taken from all major disease areas. With its wide-ranging view of an emerging new paradigm in drug development, this handbook is of prime importance for every medicinal and pharmaceutical chemist.
(source: Nielsen Book Data)9783527674411 20180618

• Intro; Green Techniques for Organic Synthesis and Medicinal Chemistry; Contents; List of Contributors; Foreword; Preface; Part I General Topics in Green Chemistry; 1 Green Chemistry Metrics; 1.1 Business Case; 1.2 Historical Context; 1.3 Metrics, Awards, and Barriers; 1.3.1 Mass-Based Metrics; 1.3.2 Life-Cycle Assessment; 1.3.3 Green Analytical Chemistry (GAC); 1.3.4 Awards; 1.3.5 Barriers; 1.4 Metrics Unification Via Green Aspiration Level; 1.4.1 Standardizing Metrics; 1.4.2 Defining Analysis Starting Points; 1.4.3 Considering Drug Manufacturing Complexity; 1.4.4 Green Aspiration Level (GAL).

• 1.4.5 Relative Process Greenness (RPG)1.5 Green Scorecard; 1.6 Supply Chain; 1.7 Outlook and Opportunities; 1.7.1 Industry-Wide Adaption; 1.7.2 Integration with LCA; 1.7.3 Application of GAL to Supply Chain; 1.7.4 Transformation-Typeâ#x80; #x93; Based GAL; 1.7.5 Opportunities for Government; References; 2 Green Solvents; 2.1 Introduction; 2.1.1 The Need for Greener Alternatives for Chlorinated Solvents; 2.1.2 The Need for Greener Alternatives for Dipolar Aprotic Solvents; 2.1.3 Scope; 2.2 Solvent Selection Guides and Tools; 2.3 Greener Molecular Solvents; 2.3.1 Carbonates; 2.3.2 -Valerolactone.

• 2.3.3 Dimethylisosorbide2.3.4 Butanol; 2.3.5 Ethyl Lactate and Lactic Acid; 2.3.6 Glycerol and Glycerol Derivatives; 2.3.7 Cyrene; 2.3.8 2-Methyl Tetrahydrofuran; 2.3.9 Cyclopentyl Methyl Ether; 2.4 Opportunities, Challenges, and Future Developments; References; 3 Green Analytical Chemistry; 3.1 Introduction; 3.1.1 Analytical Method Assessment; 3.1.2 Case Studies; 3.2 Sample Preparation; 3.2.1 Sample Preparation Focusing on Liquid Approaches; 3.2.2 Sample Preparation Using Solid Supports; 3.3 Techniques and Methods; 3.3.1 Liquid Chromatography; 3.3.2 Gas Chromatography.

• 3.3.3 Supercritical Fluid Chromatography3.3.4 Spectroscopy; 3.4 Process Analytical Technology; 3.5 Biopharmaceutical Analysis; 3.5.1 Biopharmaceutical Sample Preparation; 3.5.2 Chromatographic and Electrophoretic Separation; 3.5.3 PAT for Biopharmaceuticals; 3.6 Conclusions; Acknowledgments; References; 4 Green Engineering; 4.1 Introduction: Green Engineering Misconceptions and Realizations; 4.2 12 Principles of Green Engineering; 4.3 Green Chemistry Metrics Applied to Engineering; 4.3.1 Maleic Anhydride Production Example; 4.3.2 Level 1 Green Chemistry Metrics.

• 4.3.3 Level 2 Green Chemistry Metrics4.3.4 Level 3 Green Chemistry Metrics; 4.4 Use of Green Solvents in the Chemical Industry; 4.4.1 Waste Prevention; 4.4.2 Inherently Non-Hazardous; 4.4.3 Renewable Rather Than Depleting; 4.4.4 Design for Commercial After-Life; 4.4.5 Separation and Purification to Minimize Energy Consumption and Materials Use; 4.4.6 Integration and Interconnectivity with Available Energy and Materials Flows; 4.4.7 Conserve Complexity; 4.5 Presidential Green Chemistry Awards; 4.6 Opportunities and Outlook; References; 5 Greening of Consumer Cleaning Products.

An updated overview of the rapidly developing field of green techniques for organic synthesis and medicinal chemistry Green chemistry remains a high priority in modern organic synthesis and pharmaceutical R&D, with important environmental and economic implications. This book presents comprehensive coverage of green chemistry techniques for organic and medicinal chemistry applications, summarizing the available new technologies, analyzing each technique s features and green chemistry characteristics, and providing examples to demonstrate applications for green organic synthesis and medicinal chemistry. The extensively revised edition of Green Techniques for Organic Synthesis and Medicinal Chemistry includes 7 entirely new chapters on topics including green chemistry and innovation, green chemistry metrics, green chemistry and biological drugs, and the business case for green chemistry in the generic pharmaceutical industry. It is divided into 4 parts. The first part introduces readers to the concepts of green chemistry and green engineering, global environmental regulations, green analytical chemistry, green solvents, and green chemistry metrics. The other three sections cover green catalysis, green synthetic techniques, and green techniques and strategies in the pharmaceutical industry. Includes more than 30% new and updated material plus seven brand new chapters Edited by highly regarded experts in the field (Berkeley Cue is one of the fathers of Green Chemistry in Pharma) with backgrounds in academia and industry Brings together a team of international authors from academia, industry, government agencies, and consultancies (including John Warner, one of the founders of the field of Green Chemistry) Green Techniques for Organic Synthesis and Medicinal Chemistry, Second Edition is an essential resource on green chemistry technologies for academic researchers, R&D professionals, and students working in organic chemistry and medicinal chemistry.
(source: Nielsen Book Data)9781119288169 20180618

• Introduction to Hazardous Reagent Substitution in the Pharmaceutical Industry-- Recyclability of Reagents-- Recoverable Polymer-supported DMAP Derivatives-- Synthesis of Atorvastatin-- Synthesis of Raloxifene-- Synthesis of Montelukast-- Development of a Safe, Scalable, Azide-free Synthesis of 1-Aryl-1H-tetrazoles Using Diformylhydrazine-- New Directions from Academia.
• (source: Nielsen Book Data)9781782623847 20180213

In recent years, a significant amount of progress has been made using green chemistry in the synthesis of synthetically useful compounds and molecules by replacing hazardous chemicals with greener alternatives. However, there is still room for improvement, especially in the pharmaceutical sector where new drugs are being formulated. This book examines green approaches to overcoming hazardous organic transformations. Summarizing recent developments, the book features a detailed description of some of the high impact active pharmaceutical ingredients that have been developed considering green chemistry approaches. It explores the design, engineering and process development and the calculations to account for waste. The book includes strategies to further advance green approaches in the development of generic pharmaceutical industries and features novel, innovative approaches that promote waste-free organic synthesis. This book is of interest to industrialists working in pharmaceuticals and researchers working in green chemistry.
(source: Nielsen Book Data)9781782623847 20180213

• Historical perspective and overview of drug discovery
• Drug discovery: hit and lead identification
• Lead optimization: drug-target interactions and the pharmacophore
• Lead optimization: properties optimized and medicinal chemistry strategies
• The process of developing a drug from an optimized lead
• Receptors, ion channels, and transporters as drug targets
• Enzymes as drug targets
• Protein-protein interactions and lipid structure interactions as drug targets
• DNA and RNA as drug targets
• Anti-cancer drugs
• Antiviral and antifungal agents
• Antibacterial and antiparasitic drugs
• Drugs acting on the central nervous system.

"Volume 18, entitled Metallo-Drugs: Development and Action of Anticancer Agents of the series Metal Ions in Life Sciences centers on biological, medicinal inorganic chemistry. The serendipitous discovery of the antitumor activity of cis-diamminodichloroplatinum(II) (cisplatin) by Barnett Rosenberg in the 1960s is a landmark in metallodrug-based chemotherapy. The success of cisplatin in the clinic, followed by oxaliplatin and carboplatin, along with their drawbacks relating mainly to resistance development and severe toxicity, initiated research on polynuclear platinum complexes and on Pt(IV) complexes as prodrugs. Furthermore, the indicated shortcomings led to the exploration of other transition and main group metal ions, among them Ru(II/III), Au(I/III), Ti(IV), V(IV/V), and Ga(III) including also the essential metal ions Fe(II/III), Cu(I/II), and Zn(II). Ionic as well as covalent and non-covalent interactions between structurally very different complexes and biomolecules like nucleic acids, proteins, and carbohydrates are studied and discussed with regard to their possible anticancer actions. Hence, MILS-18 summarizes the research at the forefront of medicinal inorganic chemistry, including studies on the next-generation, tailor-made anticancer drugs. All this and more is treated in an authoritative and timely manner in the 17 stimulating chapters of this book, written by 39 internationally recognized experts from 10 nations (from the US via Europe to China and Australia). The impact of this vibrant research area is manifested by more than 2700 references, nearly 150 illustrations (more than half in color) and several comprehensive tables. Metallo-Drugs: Development and Action of Anticancer Agents is an essential resource for scientists working in the wide range from enzymology, material sciences, analytical, organic, and inorganic biochemistry all the way through to medicine including the clinic ... not forgetting that it also provides excellent information for teaching"--Provided by publisher.

• 1. Introduction of Mid-Size Drugs and Peptidomimetics.- 2. Chloroalkene Dipeptide Isosteres as Peptidomimetics.- 3. Conformational-restricted Cyclic Peptides.- 4. Peptidomimetics that Mimic Secondary Structures of Peptides.- 5.Peptidomimetics that Mimic Tertiary Structures of Peptides.- 6. Conjugated Compounds Involving Peptides.- 7. Summary and Future Perspectives of Researches on Mid-Size Drugs.
• (source: Nielsen Book Data)9789811076909 20180430

This brief describes studies conducted by the authors on mid-size drugs utilizing peptides and peptidomimetics, and on the development of anti-HIV agents. Peptides are important biological molecules and have various physiological actions. Peptide-based drug discovery may help bring about the development of useful medicines that are highly safe and show potent pharmacological effects in small doses. Recently, it has been shown that there is an important drug-like space in the mid-sized region between low- and high-molecular-weight compounds. Thus, mid-size drugs such as peptide compounds are being focused on. To date, several peptidomimetics that mimic primary, secondary, and tertiary structures of peptides have been developed to maintain and improve biological activities and actions of peptides. In this book, the features and advantages of mid-size drugs are described in detail. In addition, the merits of utilizing peptidomimetics in the development of mid-size drugs are referred to. Understanding such peptide-derived mid-size drugs will lead to a comprehensive expansion of medicinal chemistry.
(source: Nielsen Book Data)9789811076909 20180430

• Pharmacotherapy, Toxicodynamics and Regulatory Science-Divergent Objectives Nonclinical Pharmacokinetics - a primer Routes - with considerations for species specificity Delivery Systems Regimens Fundamentals of Nonclinical Formulation Excipients and Vehicles: Tolerance and toxicity Appendices.
• (source: Nielsen Book Data)9781466502536 20171218

If we will ever achieve Paul Ehrlich's "magic bullet, " that is, a molecule which goes with high selectivity to the therapeutic target site, does what it needs to do, and is subsequently cleared from the body, the practice of safety assessment will have to change. Nonclinical Drug Administration: Formulations, Routes and Regimens for Solving Drug Delivery Problems in Animal Model Systems seeks to address a trio of objectives that, though separate, are linked and central to biomedical science and, ultimately, medicine. Rather seeing these as separate "silos, " those working in nonclinical safety assessment will have to view these three in an integrated manner and to regularly and thoughtfully incorporate new information and technology. The trio of objectives this book explores are: first, to present how to deliver more of a drug product systemically to facilitate the regulatory need for evaluating safety and efficacy in animal species (at elevated exposure levels) prior to advancing the drug to human testing; second is to achieve better tolerance to therapeutics administration in test animals and humans which achieves objectives 1 and 3; and third, to explore ways to improve on therapeutic target receptor delivery performance, therefore improving both clinical pharmacodynamics bioavailability and specificity. The book's ten chapters assemble the basic concepts, principles and hypotheses involved in quantitative receptor and chronological organism interaction dynamics central to the successful development of new therapeutics which depend on systemic administration to achieve desired therapeutic goals and in so doing avoid outcomes which limit, marginalize, or preclude the therapeutic use of so many molecules.
(source: Nielsen Book Data)9781466502536 20171218
The concept of the perfect medicine as a molecule that goes with high selectivity to the therapeutic target site, does what it needs to do, and is subsequently cleared from the body is especially relevant now. Much of the current costs and post-market safety concerns arise from the inability to achieve adequate concentrations and selectivity in the due course of actually delivering the active drug. Providing an integrated approach, this book presents ways of achieving the desired adequate and selective delivery using the currently available technology in three tool sets: route, regimen, and formulation.
(source: Nielsen Book Data)9781466502598 20171218

• Intro; Title Page; Copyright Page; Contents; Chapter 1 Introduction; 1.1 The Original Definition of Privileged Structures; 1.2 The Role of Privileged Structures in the Drug Discovery Process; 1.3 The Loose Definitions of â#x80; #x9C; Privileged Structuresâ#x80; #x9D; ; 1.4 Synthesis and Biological Activities of Carbocyclic and Heterocyclic Privileged Structures; 1.4.1 Synthesis and Biological Activities of Three- and Four-Membered Ring Privileged Structures; 1.4.2 Synthesis and Biological Activities of Five-Membered Ring Privileged Structures

• 1.4.3 Synthesis and Biological Activities of Six-Membered Ring Privileged Structures1.4.4 Synthesis and Biological Activities of Bicyclic 5/5 and 6/5 Ring Privileged Structures; 1.4.5 Synthesis and Biological Activities of Bicyclic 6/6 and 6/7 Ring Privileged Structures; 1.4.6 Synthesis and Biological Activities of Tricyclic and Tetracyclic Ring Privileged Structures; 1.5 Combinatorial Libraries of â#x80; #x9C; Privileged Structuresâ#x80; #x9D; ; 1.6 Scope of this Monograph; References; Chapter 2 Benzodiazepines; 2.1 Introduction; 2.2 Marketed BDZ Drugs; 2.2.1 1,4-Benzodiazepine Marketed Drugs

• 2.2.2 1,5-Benzodiazepine Marketed Drugs2.2.3 Linearly Fused BDZ Marketed Drugs; 2.2.4 Angularly Fused-1,4-Benzodiazepine Marketed Drugs; 2.3 Medicinal Chemistry Case Studies; 2.3.1 Cardiovascular Applications; 2.3.2 Central Nervous System Applications; 2.3.3 Gastrointestinal Applications; 2.3.4 Infectious Diseases Applications; 2.3.5 Inflammation Applications; 2.3.6 Metabolic Diseases Applications; 2.3.7 Oncology Applications; 2.4 Synthesis of BDZs; 2.4.1 Condensation of o-Phenylenediamines to 1,5-Benzodiazepines; 2.4.1.1 Condensation of o-Phenylenediamines with Ketones

• 2.4.1.2 Condensation of o-Phenylenediamines with α, β-Unsaturated Ketones2.4.1.3 Condensation of o-Phenylenediamines with Alkynes; 2.4.2 Reductive Condensation of α-Substituted Nitrobenzenes with Ketones and α, β-Unsaturated Ketones; 2.4.3 Intramolecular Cyclizations to 1,4-Benzodiazepines; 2.4.3.1 Intramolecular Cyclizationsâ#x80; #x94; Path A; 2.4.3.2 Intramolecular Cyclizationsâ#x80; #x94; Path B; 2.4.3.3 Intramolecular Cyclizationsâ#x80; #x94; Path C; 2.4.3.4 Intramolecular Cyclizationsâ#x80; #x94; Path D; 2.4.3.5 Intramolecular Cyclizationsâ#x80; #x94; Path E; 2.4.3.6 Intramolecular Cyclizationsâ#x80; #x94; Path F

• 2.4.3.7 Intramolecular Cyclizationsâ#x80; #x94; Path G2.4.3.8 Intramolecular Cyclizationsâ#x80; #x94; Path H; 2.4.4 Ugi Multicomponent Synthesis; 2.4.5 Elaboration of 1,4-Benzodiazepines; 2.4.6 Pyrrolo[2,1-c]benzodiazepines; 2.4.7 Fused BDZ Ring Systems; 2.4.8 Solid-Phase Synthesis of BDZs; References; Chapter 3 1,4-Dihydropyridines; 3.1 Introduction; 3.2 Marketed 1,4-Dihyropyridine Drugs; 3.3 Medicinal Chemistry Case Studies; 3.3.1 Cardiovascular Applications; 3.3.2 Central Nervous System Applications; 3.3.3 Infectious Diseases Applications; 3.3.4 Inflammation Applications

• 3.3.5 Menâ#x80; #x99; s and Womenâ#x80; #x99; s Health Issues Applications

A comprehensive guide to privileged structures and their application in the discovery of new drugs The use of privileged structures is a viable strategy in the discovery of new medicines at the lead optimization stages of the drug discovery process. Privileged Structures in Drug Discovery offers a comprehensive text that reviews privileged structures from the point of view of medicinal chemistry and contains the synthetic routes to these structures. In this text, the author a noted expert in the field includes an historical perspective on the topic, presents a practical compendium to privileged structures, and offers an informed perspective on the future direction for the field. The book describes the up-to-date and state-of-the-art methods of organic synthesis that describe the use of privileged structures that are of most interest. Chapters included information on benzodiazepines, 1,4-dihydropyridines, biaryls, 4-(hetero)arylpiperidines, spiropiperidines, 2-aminopyrimidines, 2-aminothiazoles, 2-(hetero)arylindoles, tetrahydroisoquinolines, 2,2-dimethylbenzopyrans, hydroxamates, and bicyclic pyridines containing ring-junction nitrogen as privileged scaffolds in medicinal chemistry. Numerous, illustrative case studies document the current use of the privileged structures in the discovery of drugs. This important volume: Describes the drug compounds that have successfully made it to the marketplace and the chemistry associated with them Offers the experience from an author who has worked in many therapeutic areas of medicinal chemistry Details many of the recent developments in organic chemistry that prepare target molecules Includes a wealth of medicinal chemistry case studies that clearly illustrate the use of privileged structures Designed for use by industrial medicinal chemists and process chemists, academic organic and medicinal chemists, as well as chemistry students and faculty, Privileged Structures in Drug Discovery offers a current guide to organic synthesis methods to access the privileged structures of interest, and contains medicinal chemistry case studies that document their application.
(source: Nielsen Book Data)9781118145661 20180618

• PART I: GENERAL ASPECTS Small molecule drugs and biologics Patenting antibodies PART II: DRUG CLASSES Androgen Antagonists Kinase Inhibitors PART III: CASE HISTORIES Blinatumomab Ceritinib Daratumumab Obeticholic acid Obinutuzumab Omarigliptin Opicapone Osimertinib Pitolisant Safinamide Trifluridine and Tipiracilhydrochloride.
• (source: Nielsen Book Data)9783527808663 20180618

With its focus on drugs so recently introduced that they have yet to be found in any other textbooks or general references, the information and insight found here makes this a genuinely unique handbook and reference. Following the successful approach of the previous volumes in the series, inventors and primary developers of successful drugs from both industry and academia tell the story of the drug's discovery and describe the sometimes twisted route from the first drug candidate molecule to the final marketed drug. The 11 case studies selected describe recent drugs ranging across many therapeutic fields and provide a representative cross-section of present-day drug developments. Backed by plenty of data and chemical information, the insight and experience of today?s top drug creators makes this one of the most useful training manuals that a junior medicinal chemist may hope to find. The International Union of Pure and Applied Chemistry has endorsed and sponsored this project because of its high educational merit.
(source: Nielsen Book Data)9783527808663 20180618

• Cover; Preface; Contents; Chapter 1 Introduction; 1.1 Introduction; References; Chapter 2 Transition Metals in Greener Pharmaceutical Chemistry; 2.1 Transition Metals in Greener Pharmaceutical Chemistry; References; Chapter 3 Sustainable Synthesis of Pharmaceuticals Using Alternative Techniques: Microwave, Sonochemistry and Mechanochemistry; 3.1 Introduction; 3.2 Metrics; 3.3 Microwave; 3.4 Sonochemistry; 3.5 Mechanochemistry; 3.6 Conclusion; Acknowledgements; References; Chapter 4 Carbonylation Reactions in the Synthesis of Pharmaceutically Active Compounds; 4.1 Introduction.

• 4.2 Hydroalkoxycarbonylation of Alkenes4.3 Carbonylation of Aryl/Alkenyl Halides; 4.3.1 Aminocarbonylation Reactions; 4.3.2 Alkoxy-and Hydroxycarbonylations; 4.3.3 Carbonylative Coupling Reactions; 4.3.4 The Use of CO Equivalents; 4.3.5 Industrial Applications; 4.4 Oxidative Carbonylation Reactions; 4.5 Conclusion and Outlook; Acknowledgements; References; Chapter 5 Applications of Catalytic Hydroformylation in the Synthesis of Biologically Relevant Synthons and Drugs; 5.1 Introduction; 5.2 Hydroformylation Catalysts-A Historical Perspective.

• 5.3 Hydroformylation with Alternative Catalytic Systems5.4 Catalytic Hydroformylation in the Synthesis of Biologically Active Molecules: Selected Examples; 5.4.1 Enantioselective and Diastereoselective Hydroformylation in Drug Synthesis; 5.5 Conclusion and Future Perspective; Acknowledgements; References; Chapter 6 Transfer Hydrogenation with Non-toxic Metals for Drug Synthesis; 6.1 Introduction; 6.2 Transfer Hydrogenation; 6.2.1 Mechanistic Overview of Transfer Hydrogenation of Ketones; 6.2.2 Transfer Hydrogenation with Cheap Metals.

• 6.2.3 Asymmetric Transfer Hydrogenation in the Synthesis of Bioactive Molecules6.3 Borrowing Hydrogen Methodology; 6.4 Conclusion; Acknowledgements; References; Chapter 7 Green Metal-catalysed Synthesis of Pharmaceutically Useful Asymmetric Epoxides and Sulfoxides; 7.1 Epoxidation and Sulfoxidation: Introduction; 7.2 Asymmetric Transition Metal-catalysed Epoxidation of Olefins; 7.2.1 The Katsuki-Sharpless Asymmetric Epoxidation of Allylic Alcohols; 7.2.2 The Jacobsen-Katsuki Epoxidation with M(salen) Complexes; 7.2.3 M(bis-hydroxamic acid)-catalysed Epoxidations.

• 7.2.4 M(aminopyridine)-catalysed Epoxidations7.3 Transition Metal-catalysed Asymmetric Sulfoxidation; 7.3.1 Asymmetric Sulfoxidation with Sharpless-type Catalysts; 7.3.2 Asymmetric Sulfoxidation with Jacobsen-Katsuki-type Catalysts; 7.3.3 Asymmetric Sulfoxidation with M(bis-hydroxamic) Catalysts; 7.3.4 Catalytic ASO Processes Using Environmentally Sustainable O2 as TO; 7.3.5 Catalytic ASO Processes Using Environmentally Sustainable H2O2 as TO; 7.3.6 M(salen), M(salan) and M(salalen) Sulfoxidation with H2O2 as TO; 7.4 Conclusion; References.

There is a growing interest in the development of sustainable processes for the synthesis of pharmaceuticals and this book bridges the divide between industrial examples and the fundamental chemistry. It explains the basic principles of using transition metal catalysis with several green approaches for the synthesis of pharmaceuticals. The topic is an important one for green chemistry and the chapters in this book on hydroformylation, green oxidation and olefin metathesis will also be of interest to both medicinal and organic chemists. Written by leading experts in the field, it provides a valuable and easy tool for scientists and industrialists who require information regarding this topic.

This book compiles reliable protocols for preparation of intermediates for carbohydrate synthesis or other substances and methods performed at the bench, which can be expected to be useful in the glycosciences. To ensure reproducibility, the experimental part involved is verified by an independent checker by repeating the protocol or using the method. Regardless of whether the method has previously been published, the protocol must be reliable and expected to be of wide use in the carbohydrate field.
(source: Nielsen Book Data)9781498726924 20171218

• Volume 1: General Perspective - The Future of Drug Discovery Volume 2: Drug Discovery Technologies Volume 3: In Silico Drug Discovery Tools Volume 4: Experimental ADME and Toxicology Volume 5: Cancer, Immunology and Inflammation, and Infectious Disease Volume 6: CNS, Pain, Metabolic Syndrome, Urology, Gastrointestinal and Cardiovascular Volume 7: Biologics Medicine Volume 8: Case Histories in Recent Drug Discovery.
• (source: Nielsen Book Data)9780128032008 20170724

Comprehensive Medicinal Chemistry III, Third Edition provides a contemporary and forward looking critical analysis and summary of recent developments, emerging trends, and recently identified new areas where medicinal chemistry is having an impact. The discipline of medicinal chemistry continues to evolve as it adapts to new opportunities and strives to solve new challenges. These include drug targeting, biomolecular therapeutics, development of chemical biology tools, data collection and analysis, in silico models as predictors for biological properties, identification and validation of new targets, approaches to quantify target engagement, new methods for synthesis of drug candidates such as green chemistry, development of novel scaffolds for drug discovery, and the role of regulatory agencies in drug discovery.
(source: Nielsen Book Data)9780128032008 20170724

• Introduction: Hydrogel as useful carrier for drug delivery systems: an overview. Synthesis of protein-based hydrogels as drug delivery devices. Synthesis of polysaccharide-based hydrogels as drug delivery devices. Synthetic hydrogels as drug delivery devices. Nanocomposite hydrogels: Synthesis and characterization. pH-sensitive drug-delivery hydrogels: synthesis and applications. Thermo-sensitive drug-delivery hydrogels: synthesis and applications. Enzyme-responsive hydrogels: synthesis and applications. Nanocomposites hydrogels as electro and magneto-responsive devices. Multi-responsive drug delivery hydrogels. Mucoadhesive Hydrogels: a valuable strategy for the prolonged-delivery of drugs. Hydrogel as carrier for large-molecule delivery. DNA delivery vectors for gene-therapy. Synthesis and application of molecularly imprinted hydrogels for specific release of the therapeutics.
• (source: Nielsen Book Data)9781498749022 20171218

The book deals with the synthesis and characterization of hydrogels specifically used as drug delivery systems. Each chapter includes the most recent updates about the different starting materials employed-whether natural and synthetic-and the improvement, such as modifications of synthetic approach and polymerization technique, of their physicochemical and biological properties to synthetize high performing carriers for specific uses, i.e. stimuli-responsive materials, molecularly imprinted polymers, mucoadhesive materials, carrier for the delivery of high molecular weight drugs, and gene-delivery.
(source: Nielsen Book Data)9781498749022 20171218

This third volume in a four-volume set offers new theories and applications for the diagnosis and treatment of mental disorders. Having laid the groundwork in the first two volumes, the authors now embark on significant, real-life scenarios that apply their philosophy to mental disorder treatments. The goal of the project is to take the industry toward sustainability, not just in terms of the chemical engineering used to create medicines, but also environmentally, economically, and personally. Their unique approach uses a more holistic and philosophically cohesive method for treating mental disorders, making the industry "greener" and the patient healthier. The four volumes in "The Greening of Pharmaceutical Engineering" are: * Volume 1: Practice, Analysis, and Methodology * Volume 2: Theories and Solutions * Volume 3: Applications for Mental Disorder Treatments * Volume 4: Applications for Physical Disorder Treatments This ground-breaking set of books is a unique and state-of-the-art study that only appears here, within these pages. A fascinating study for the engineer, scientist, and pharmacist working in the pharmaceutical industry and interested in sustainability, it is also a valuable textbook for students and faculty studying these subjects.
(source: Nielsen Book Data)9781119183815 20170807

• 1. Introduction
• 2. A model for humanity and human behavior
• 3. Chemical drugs for mental health disorder
• 4. Psychological grounding
• 5. Drivers of mental ailments and natural remedy
• 6. Schizophrenia as a tangible expression of mental disorder
• 7. The myopic mindset of self-destruction
• 8. Optimization of lifestyle
• 9. Conclusions.

• Bioanalytical concepts for environmental toxicology.- In vitro - in vivo endocrine disruptors.- In vitro - in vivo Genotoxicity.- In vitro - in vivo Carcinogenicity.- In vitro - in vivo Modeling.- Key factor Metabolism.- Biosensing.- Effect directed analysis (EDA).
• (source: Nielsen Book Data)9783319459066 20171211

This book review series presents current trends in modern biotechnology. The aim is to cover all aspects of this interdisciplinary technology where knowledge, methods and expertise are required from chemistry, biochemistry, microbiology, genetics, chemical engineering and computer science.Volumes are organized topically and provide a comprehensive discussion of developments in the respective field over the past 3-5 years. The series also discusses new discoveries and applications. Special volumes are dedicated to selected topics which focus on new biotechnological products and new processes for their synthesis and purification.In general, special volumes are edited by well-known guest editors. The series editor and publisher will however always be pleased to receive suggestions and supplementary information. Manuscripts are accepted in English.
(source: Nielsen Book Data)9783319459066 20171211

Despite considerable technological advances, the pharmaceutical industry is experiencing a severe innovation deficit, especially in the discovery of new drugs. Innovative Approaches in Drug Discovery: Ethnopharmacology, Systems Biology and Holistic Targeting provides a critical review and analysis of health, disease and medicine, and explores possible reasons behind the present crisis in drug discovery. The authors illustrate the benefits of systems biology and pharmacogenomics approaches, and advocate the expansion from disease-centric discovery to person-centric therapeutics involving holistic, multi-target, whole systems approaches. This book lays a path for reigniting pharmaceutical innovation through a disciplined reemergence of pharmacognosy, embracing open innovation models and collaborative, trusted public-private partnerships. With unprecedented advances made in the development of biomedically-relevant tools and technologies, the need is great and the time is now for a renewed commitment towards expanding the repertoire of medicines.ïŽ By incorporating real-life examples and state-of-the-art reviews, this book provides valuable insights into the discovery and development strategies for professionals, academicians, and students in the pharmaceutical sciences.

• Preface ix Companion Website Directions xii 1. Introduction: Basic Concepts 1 1.1 Introduction 1 1.2 Drugs and drug nomenclature 3 1.3 Law of mass action 4 1.4 Ionization 9 1.5 Partition coefficients 12 1.6 Further reading 14 2. Drug Administration and Distribution 15 2.1 Introduction 15 2.2 Drug transfer across biological membranes 16 2.3 Drug administration 22 2.4 Drug distribution 31 2.5 Plasma protein binding 38 2.6 Further reading 43 2.7 References 43 3. Drug Metabolism and Excretion 45 3.1 Introduction 45 3.2 Metabolism 46 3.3 Excretion 58 3.4 Further reading 69 3.5 References 69 4. Single compartment Pharmacokinetic Models 71 4.1 Introduction 72 4.2 Systemic clearance 74 4.3 Intravenous administration 76 4.4 Absorption 79 4.5 Infusions 87 4.6 Multiple doses 90 4.7 Non linear kinetics 94 4.8 Relationship between dose, and onset and duration of effect 98 4.9 Limitations of single compartment models 99 4.10 Further reading 100 4.11 References 100 5. Multiple compartment and Non compartment Pharmacokinetic Models 102 5.1 Multiple compartment models 102 5.2 Non compartmental models 117 5.3 Population pharmacokinetics 121 5.4 Curve fitting and the choice of most appropriate model 122 5.5 Further reading 124 5.6 References 124 6. Kinetics of Metabolism and Excretion 126 6.1 Introduction 126 6.2 Metabolite kinetics 127 6.3 Renal excretion 137 6.4 Excretion in faeces 142 6.5 Further reading 143 6.6 References 144 7. Clearance, Protein Binding and Physiological Modelling 145 7.1 Introduction 145 7.2 Clearance 146 7.3 Physiological modelling 158 7.4 Further reading 161 7.5 References 161 8. Quantitative Pharmacological Relationships 162 8.1 Pharmacokinetics and pharmacodynamics 162 8.2 Concentration effect relationships (dose response curves) 163 8.3 Time dependent models 169 8.4 PK PD modelling 173 8.5 Further reading 177 8.6 References 177 9. Pharmacokinetics of Large Molecules 178 9.1 Introduction 178 9.2 Pharmacokinetics 179 9.3 Plasma kinetics and pharmacodynamics 184 9.4 Examples of particular interest 185 9.5 Further reading 191 9.6 References 191 10. Pharmacogenetics and Pharmacogenomics 192 10.1 Introduction 192 10.2 Methods for the study of pharmacogenetics 193 10.3 N Acetyltransferase 194 10.4 Plasma cholinesterase 197 10.5 Cytochrome P450 polymorphisms 199 10.6 Alcohol dehydrogenase and acetaldehyde dehydrogenase 202 10.7 Thiopurine methyltransferase 202 10.8 Phase 2 enzymes 202 10.9 Transporters 204 10.10 Ethnicity 206 10.11 Pharmacodynamic differences 206 10.12 Personalized medicine 208 10.13 Further reading 209 10.14 References 209 11. Additional Factors Affecting Plasma Concentrations 211 11.1 Introduction 211 11.2 Pharmaceutical factors 213 11.3 Sex 214 11.4 Pregnancy 218 11.5 Weight and obesity 220 11.6 Food, diet and nutrition 225 11.7 Time of day 226 11.8 Posture and exercise 228 11.9 Further reading 231 11.10 References 231 12. Effects of Age and Disease on Drug Disposition 233 12.1 Introduction 233 12.2 Age and development 234 12.3 Effects of disease on drug disposition 242 12.4 Assessing pharmacokinetics in special populations 256 12.5 Further reading 257 12.6 References 258 13. Drug Interactions and Toxicity 260 13.1 Introduction 260 13.2 Drug interactions 261 13.3 Toxicity 273 13.4 Further reading 282 13.5 References 282 14. Perspectives and Prospects: Reflections on the Past, Present and Future of Drug Disposition and Pharmacokinetics 284 14.1 Drug disposition and fate 284 14.2 Pharmacodynamics 286 14.3 Quantification of drugs and pharmacokinetics 286 14.4 The future 289 14.5 Postscript 291 14.6 Further reading 292 14.7 References 292 Appendices 1 Mathematical Concepts and the Trapezoidal Method 293 2 Dye Models to Teach Pharmacokinetics 300 3 Curve Fitting 303 4 Pharmacokinetic Simulations 307 Index 312.
• (source: Nielsen Book Data)9781119261049 20170403

The application of knowledge of drug disposition, and skills in pharmacokinetics, are crucial to the development of new drugs and to a better understanding of how to achieve maximum benefit from existing ones. The book takes the reader from basic concepts to a point where those who wish to will be able to perform pharmacokinetic calculations and be ready to read more advanced texts and research papers. The book will be of benefit to students of medicine, pharmacy, pharmacology, biomedical sciences and veterinary science, including those who have elected to study the topic in more detail, such as via electives and special study modules. It will be of benefit to those involved in drug discovery and development, pharmaceutical and medicinal chemists, as well as budding toxicologists and forensic scientists who require the appropriate knowledge to interpret their findings and as an introductory text for clinical pharmacologists. Early chapters describe the basic principles of the topic while the later ones illustrate the application of those principles to modern approaches to drug development and clinical use. Full colour illustrations facilitate the learning experience and supporting material for course leaders and students can be found on the Companion Web Site.
(source: Nielsen Book Data)9781119261049 20170403

• Drug Administration and Distribution
• Drug Metabolism and Excretion
• Single-compartment Pharmacokinetic Models
• Multiple-compartment and Non-compartment Pharmacokinetic Models
• Kinetics of Metabolism and Excretion
• Clearance, Protein Binding and Physiological Modelling
• Quantitative Pharmacological Relationships
• Pharmacokinetics of Large Molecules
• Pharmacogenetics and Pharmacogenomics
• Additional Factors Affecting Plasma Concentrations
• Effects of Age and Disease on Drug Disposition
• Drug Interactions and Toxicity
• Perspectives and Prospects
• Appendix 1: Mathematical Concepts and the Trapezoidal Method
• Appendix 2: Dye Models to Teach Pharmacokinetics
• Appendix 3: Curve Fitting
• Appendix 4: Pharmacokinetic Simulations.

"The application of knowledge of drug disposition, and skills in pharmacokinetics, are crucial to the development of new drugs and to a better understanding of how to achieve maximum benefit from existing ones. The book takes the reader from basic concepts to a point where those who wish to will be able to perform pharmacokinetic calculations and be ready to read more advanced texts and research papers. The book will be of benefit to students of medicine, pharmacy, pharmacology, biomedical sciences and veterinary science, including those who have elected to study the topic in more detail, such as via electives and special study modules. It will be of benefit to those involved in drug discovery and development, pharmaceutical and medicinal chemists, as well as budding toxicologists and forensic scientists who require the appropriate knowledge to interpret their findings and as an introductory text for clinical pharmacologists. Early chapters describe the basic principles of the topic while the later ones illustrate the application of those principles to modern approaches to drug development and clinical use. Full colour illustrations facilitate the learning experience and supporting material for course leaders and students can be found on the Companion Web Site"-- Provided by publisher.
"The book takes the reader from basic concepts to a point where those who wish to will be able to perform pharmacokinetic calculations and be ready to read more advanced texts and research papers"-- Provided by publisher.

• PART A DRUG TARGETS - STRUCTURE AND FUNCTION-- PART B PHARMACODYNAMICS AND PHARMACOKINETICS-- PART C DRUG DISCOVERY, DESIGN, AND DEVELOPMENT-- PART D TOOLS OF THE TRADE-- PART E SELECTED TOPICS IN MEDICINAL CHEMISTRY-- APPENDICES.
• (source: Nielsen Book Data)9780198749691 20180409

For many people, taking some form of medication is part of everyday life, whether for mild or severe illness, acute or chronic disease, to target infection or to relieve pain. However for most it remains a mystery as to what happens once the drug has been taken into the body: how do the drugs actually work? Furthermore, by what processes are new drugs discovered and brought to market? An Introduction to Medicinal Chemistry, sixth edition, provides an accessible and comprehensive account of this fascinating multidisciplinary field. Assuming little prior knowledge, the text is ideal for those studying the subject for the first time. Part one of the book introduces the principles of drug action via targets such as receptors and enzymes. The book goes on to explore how drugs work at the molecular level (pharmacodynamics), and the processes involved in ensuring a drug meets its target (pharmacokinetics). Further sections cover the processes by which drugs are discovered and designed, and what has to happen before a drug can be made available to the public. The book concludes with a selection of current topics in medicinal chemistry, and a discussion of various key drug groups. The subject is brought to life throughout by engaging case studies highlighting particular drugs and the stories behind their discovery and development. The Online Resource Centre features: For students: * Multiple Choice Questions to support self-directed learning * Web articles describing recent developments in the field and further information on topics covered in the book * Journal Club to encourage students to critically analyse the research literature * Molecular Modelling Exercises, with new exercises in Chem3D * New assignments to help students develop data analysis and problem solving skills For registered adopters of the book: * A test bank of additional multiple-choice questions, with links to relevant sections in the book * Answers to end-of-chapter questions. * Figures from the book, ready to download. * Power Point slides to accompany every chapter in the book.
(source: Nielsen Book Data)9780198749691 20180409