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Keeping up-to-date with the latest technologies in lead optimisation can be time consuming so SMi Conferences has done the hard work for you with our latest international conference.

From Hit-to-Lead: Optimising Drug development takes place on the 19th & 20th September 2001 at the Hatton, London and will make sure your fully informed of the recent developments and strategies in lead optimisation that have lead to revolutionary advances throughout science and industry. You will also discover more about the integration of predictive biology into drug discovery and design as well as the commercial issues in lead generation and optimisation. This will include the increasing pressures upon the pharmaceutical industry to meet the productivity challenge.

Our speakers at this conference are leaders in the fields of lead discovery, lead optimisation and pharmaceutical development and will offer an insight into the importance of lead optimisation within drug discovery to help you benefit financially.

The conference will of course also be an ideal opportunity for you to network with a focused, appropriate audience and gain up to date information regarding the future of drug discovery.

Build on the information gained at the conference with our one-day post-conference workshop:

Man & Machine in Harmony: Addressing the People Factors in Drug Discovery

Conference programme

8:30 Registration and Coffee

9:00 Chairman's Opening Remarks

Dr Alan Wilson

Dr Alan Wilson, Head & Senior Director, Drug Metabolism & Toxicology, Lexicon Genetics

9:10 RECENT DEVELOPMENTS IN LEAD OPTIMISATION

Dr Neerja Bhatnagar

Dr Neerja Bhatnagar, Research Head, Medicinal Chemistry, Aventis

  • Advances in technology
  • Mechanism based library design
  • From target family directed library to target specific dedicated library
  • Results
  • 9:40 STREAMLINING DRUG DISCOVERY

    Dr Sian Griffiths

    Dr Sian Griffiths, Manager, Technical Marketing, Pharmacopeia

  • Collaborative drug discovery
  • From target to lead optimisation
  • Generating leads using uHTS
  • Combinatorial chemistry: ECLIPSTM
  • Predictive tools for lead optimisation
  • 10:20 STRATEGIC DEVELOPMENTS IN LEAD OPTIMISATION

    Dr Daniel Schirlin

    Dr Daniel Schirlin, Head, Global Chemistry, Aventis

  • Innovations in lead technology
  • High-throughput technologies: for synthesis and screening
  • Strategies and predictive models
  • Parameters critical to clinical success
  • 11:00 Morning Coffee

    11:20 DRUG DISCOVERY STRATEGIES

    Dr John Montana

    Dr John Montana, Director, NCE Research, Celltech

  • Effective application of parallel synthesis
  • Benefits of working in gene families
  • Efficient use of early DMPK in research
  • Applications of CADD and SBDD
  • Triaging these activities to reduce timelines
  • 12:00 PHARMACEUTICAL PROFILING

    Dr Edward Kerns

    Dr Edward Kerns, Principal Research Scientist, Chemical Sciences, Wyeth-Ayerst Research

  • Complementary nature of compound properties and activity
  • Value of early pharmaceutical property assessment
  • Primary pharmaceutical profile panel: implementation and application
  • Building favourable pharmaceutical properties
  • Selecting advantageous HTS hits and leads
  • General case studies of drug discovery impact
  • 12:40 Networking Lunch

    13:40 R & D PROJECT MANAGEMENT

    Guy Malchi

    Guy Malchi, Operations Manager, TEFEN

  • Reducing time to market using Goals Orientated Project Management (GoPM)
  • Role of project management in pharmaceutical R & D projects
  • GoPM methodology overview
  • Assess current PM & control practices
  • Creating a GoPM control centre
  • Measuring R & D productivity
  • 14:20 THE CHALLENGES OF VIRTUAL SCREENING

    Dr Ulrich Dauer

    Dr Ulrich Dauer, Chief Executive Officer, 4SC AG

  • Making predictive methods applicable to huge datasets
  • Hardware trends
  • Interplay between virtual and medicinal chemistry
  • Access to novel structures
  • The limits of HTS
  • Shortcuts on the way: the development candidates
  • 15:00 LEAD DISCOVERY AND GENERATION

    Dr Paul England

    Dr Paul England, Senior Scientific Fellow, Aurora Biosciences

  • Critical issues in assay development
  • Investing in screening to improve target validation
  • Integrating assay technology
  • Streamlining lead optimisation through assay development
  • Potential for pharmaceutical applications
  • 15:40 Afternoon Tea

    16:00 BIOPHARMACEUTICAL PROPERTY PREDICTIONS

    Dr Pieter Stouten

    Dr Pieter Stouten, Head, Molecular Modelling & Design, Discovery Research Oncology, Pharmacia

  • Early contributions from property predictions
  • Solubility prediction, a key factor
  • The need for in-house model development
  • The “globality” of computer models
  • Property predictions in combinatorial library design
  • The importance of the type and quality of experimental data
  • 16:30 THE DESIGN AND DEVELOPMENT OF EXPLORATORY COMBINATORIAL LIBRARIES

    Dr Eddy Littler

    Dr Eddy Littler, Director, Biology & Molecular Sciences & Lead Discovery Manager, Medivir AB

  • Selection of tractable targets
  • Library design HTS versus focused library sets
  • Technology solutions
  • Use of combinatorial chemistry to accelerate drug discovery
  • 17:00 Chairman's Closing Remarks and Close of Day One

    8:30 Re-registration and Coffee

    9:00 Chairman's Opening Remarks

    Dr Nicholas Dean

    Dr Nicholas Dean, Vice President, Functional Genomics, ISIS Pharmaceuticals

    9:10 LIBRARY DESIGN AND SYNTHESIS

    Dr Michael Lawless

    Dr Michael Lawless, Senior Project Manager, Tripos

  • Effecting lead development through design and synthesis
  • Using topomeric shape and feature searches to guide synthesis
  • Generating virtual libraries: ChemSpaceTM technology
  • Combinatorial libraries: shape and feature searching
  • Identifying the best compounds to synthesise
  • Improving the efficiency of lead optimisation
  • 9:40 UTILISING TECHNOLOGY TO ACCELERATE THE PACE OF DRUG DISCOVERY

    Dr John Hurst

    Dr John Hurst, Vice President and Chief Technology Officer, ChemNavigator

  • In silico technology: an information intensive business
  • Lead exploration: the importance of making quality decisions
  • In silico screening technologies
  • Technology for streamlining screening applications
  • Reducing development times: mapping and predicting biological processes with simulation tools
  • The key to future success in discovery and development
  • 10:20 UTILISING ORIGEN ECL TECHNOLOGY IN THE HIT TO LEAD PROCESS

    Katrina Drayton

    Katrina Drayton, Senior Research Scientist, AstraZeneca

  • Hit to Lead process mapping
  • Whole cell functional assays
  • Comparison of Origen, FMAT and ELISA approaches
  • Efficiency gains and cost reductions
  • Generic assay formats
  • Future opportunities
  • 11:00 Morning Coffee

    11:20 APPICATION OF FLUORESCENCE TECHNOLOGY TO IN-VITRO ADME ASSAYS

    Lawrence Cohen

    Lawrence Cohen, Associate Scientist, Candidate Enhancement, Pfizer

  • Comparison between drug and fluorogenic probes
  • Application of fluorescence technology in early ADME
  • Furthering lead optimisation
  • 12:00 IN SILICO HIGH-THROUGHPUT SCREENING

    Dr Trevor Howe

    Dr Trevor Howe, Scientific Expert, Computational Chemist, Novartis

  • Measuring the impact of in silico techniques
  • Optimising lead selection
  • High-throughput process development
  • What are the benefits of in silico technology?
  • The key to optimal HTS
  • Building a screening collection
  • 12:40 Networking Lunch

    13:40 LEAD GENERATION: FROM HERE TO THERE

    Chris Holmes

    Chris Holmes, Principal, World Class International

  • The challenges faced for drug discovery
  • Providing the optimum mindset for drug discovery
  • Extracting maximum value from genomic information
  • Integrating informative data to find leads
  • Quality output vs high-throughput
  • Tackling the challenges for lead generation
  • 14:20 FROM GENOMICS TO BREAKTHROUGH DRUGS

    Dr Doug Livingston

    Dr Doug Livingston, Vice President, Chemistry and New Technology, Structural GenomiX

  • Primary applications of X-ray crystallography
  • Methods of structurally annotating the genome
  • Applying genomics-based platforms to lead optimisation - selecting drug candidates
  • The potential of genomic applications in medicinal chemistry
  • Improving the quality of lead compounds and clinical candidates
  • 15:00 RAPID & HIGH THROUGH PUT GENE FUNCTIONALISATION IN TISSUE CULTURE & ANIMALS

    Dr Nicholas Dean

    Dr Nicholas Dean, Vice President, Functional Genomics, ISIS Pharmaceuticals

  • Genomic information and the challenges facing the pharmaceutical industry
  • Utilising gene functionalisation to develop new & specific drug classes
  • Lead optimisation and target validation: value of antisense technology
  • Future developments & technologies
  • 15:40 Afternoon Tea

    16:00 GENOMICS-BASED DRUG DESIGN

    Dr Philip Dean

    Dr Philip Dean, Chief Scientific Officer, De Novo Pharmaceuticals

  • Utilising the human genome sequence for lead generation
  • The in silico problem for drug discovery
  • The provision of possible targets
  • Finding structurally related binding sites
  • Determining how selectivity in drug design can be approached
  • Computational methods for structure generation
  • 16:30 STRATEGIES FOR LEAD COMPOUND TRIAGE

    Dr Joseph Rininger

    Dr Joseph Rininger, Senior Research Scientist, Curagen

  • GeneCallingTM technology: creating gene expression profiles
  • Pharmacogenomics profiles denoting drug response
  • How to efficiently triage lead compounds
  • Characterising marker genes
  • Elucidation of alternate indications
  • Utilising technology to determine risk among lead drug candidates
  • 17:00 Chairman's Closing Remarks and Close of Conference

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    Workshops

    Man & Machine in Harmony
    Workshop

    Man & Machine in Harmony

    None
    21st July 2001
    , None

    The Hatton, at etc. venues

    51/53 Hatton Garden
    London EC1N 8HN
    United Kingdom

    The Hatton, at etc. venues

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    WHAT IS CPD?

    CPD stands for Continuing Professional Development’. It is essentially a philosophy, which maintains that in order to be effective, learning should be organised and structured. The most common definition is:

    ‘A commitment to structured skills and knowledge enhancement for Personal or Professional competence’

    CPD is a common requirement of individual membership with professional bodies and Institutes. Increasingly, employers also expect their staff to undertake regular CPD activities.

    Undertaken over a period of time, CPD ensures that educational qualifications do not become obsolete, and allows for best practice and professional standards to be upheld.

    CPD can be undertaken through a variety of learning activities including instructor led training courses, seminars and conferences, e:learning modules or structured reading.

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    There are approximately 470 institutes in the UK across all industry sectors, with a collective membership of circa 4 million professionals, and they all expect their members to undertake CPD.

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    CPD Schemes often run over the period of a year and the institutes generally provide online tools for their members to record and reflect on their CPD activities.

    TYPICAL CPD SCHEMES AND RECORDING OF CPD (CPD points and hours)

    Professional bodies and Institutes CPD schemes are either structured as ‘Input’ or ‘Output’ based.

    ‘Input’ based schemes list a precise number of CPD hours that individuals must achieve within a given time period. These schemes can also use different ‘currencies’ such as points, merits, units or credits, where an individual must accumulate the number required. These currencies are usually based on time i.e. 1 CPD point = 1 hour of learning.

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    As a formal provider of CPD certified activities, SMI Group can provide an indication of the learning benefit gained and the typical completion. However, it is ultimately the responsibility of the delegate to evaluate their learning, and record it correctly in line with their professional body’s or employers requirements.

    GLOBAL CPD

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