2013 speakers oxford global conferences are proud to present discovery combined 2013 agenda.pdf ·...

Innovation Driven Discovery Discovery Chemistry & Drug Design

Day 1 Stream 1 R&D Models For The Future

Polypharmacology: new opportunities for open innovation

Virtual R&D: defining critical activities

Public/Private partnerships

M&A: the modern industry landscape

Harnessing innovation: enabling the entrepreneur

New paradigms for CRO collaboration

Day 1 Stream 2 Screening & Assays: Enabling Technologies

RNAi screening

Integrated lead discovery

Phenotypic screening

FBS-by-biochemical assays

Embryonic stem cell technologies

Assays for anti-viral research

Flow chemistry

New approaches to antibody screening

Day 1 Stream 3 Discovery Chemistry: Latest Case Studies

Structure-activity relationships

Fragment based drug discovery

Combinatorial and high-throughput chemistry

Multi-target drug discovery

Predicting solubility

Kinase data: impact on on selectivity and pharmacology profiling

Day 2 Stream 1

Innovative Drug Targets

Novel biological targets

Promising targets for neurology

Fragment-based approaches for difficult

targets

Purinome-targeted oncology libraries

Target identification in endocrinology

GPCR signalling pathways

Day 2 Stream 2

Supporting Innovation: Data & Information

Management

Using multifactorial data to improve

compound survival

Data analysis & omics data integration

Innovative compound bank programs

Sharing & consolidating information

Managing complex discovery portfolios

Day 2 Stream 3

Drug Design: Novel Approaches

Optimising allosteric kinase inhibitors

Structure based drug design

Anti-target modelling in early drug

discovery

Protein-ligand interactions: a new

theory of binding

In silico profiling of compounds

Oxford Global Conferences Are Proud To Present... The 14

th Annual Drug Discovery Leaders Summit, taking place on 10 & 11 June in Geneva. The

summit is made up of two co-located events: Innovation Driven Discovery and Discovery Chemistry & Drug Design.

The drug discovery industry faces a decade of monumental change – stem cell research, generic threat, big data challenges, PHC strategies and the growing focus on biologics all threaten to change the face of the global market. This long-established summit will explore the critical opportunities in drug discovery today, while updating key decision makers on the latest technological breakthroughs.

The Innovation Driven Discovery congress explores new approaches to screening, assay development and target identification, while experts describe the data integration technologies capable of supporting this innovation. Our esteemed speaker panel will also discuss their strategies for harnessing external innovation and building effective collaborative working methods.

The Discovery Chemistry & Drug Design congress features presentations on lead optimisation, structure-activity relationships and multi-target drug discovery. Our internationally renowned speakers will also discuss the latest developments in drug design, including anti-target modelling, new theories of protein-ligand binding and the impact of kinase data on selectivity profiling. The event will be co-located with our 5

th Annual Drug Development Congress; a high-level meeting

for those working at the forefront of research, development and translational medicine.

www.pharmaresearch-series.com

2013 Speakers

Robert Hayes Janssen

Lorenz Mayr AstraZeneca

Vic Myer Novartis

Networking And Business Meeting Opportunities Meet face-to-face with leading solution providers and senior-level industry peers through a series of formal and informal networking opportunities. Categories of solution provider include:

Drug Discovery Drug Design Medicinal Chemistry

Exploratory Medicine Target Discovery Target Validation

Screening Assay Development Lead Optimisation

Lead Generation Cell-Based Assays Data Mining

Computational Chemistry Library Design Discovery Services

Selectivity Profiling Structural Biology PK/PD Evaluation

Who You Will Meet 250 senior attendees from leading pharmaceutical, biopharmaceutical, biotechnology, diagnostics, CRO, solution provider and academic organisations. Meet Senior VPs, Directors & Managers with the following job titles:

http://www.pharmaresearch-series.com/

Confirmed Speakers:

Paul Germann, Vice President New Frontier Science Europe, Takeda Robert Hayes, Vice President and Venture Leader, Centyrex Venture, Janssen R&D Emilio Diez Monedero, VP MDR & Director Basic Research Centre GSK William Strohl, VP, Biologics Research, Johnson & Johnson Lorenz Mayr, Vice President & Global Head, Reagents & Assay Development, AstraZeneca Michael Braxenthaler, President, Pistoia Alliance William Pennie, Executive Director of Compound Safety Prediction, Pfizer Vic Myer, Executive Director, Developmental and Molecular Pathways, Novartis Peter Hamley, Global Head Parallel Synthesis & Natural Products, Sanofi Aventis Campbell Wilson, Executive Business Development Director, Science & Technology Licensing, AstraZeneca Uwe Huedepohl, Vice President, R&D Project, Portfolio and Science Submission Management, MedImmune Alastair Lawson, Senior Director of Structural Biology, UCB Trevor Howe, Scientific Director and Janssen Fellow Guido Koch, Director in Global Discovery Chemistry, Novartis Ulrich Betz, Director, Department Head Innovation & Entrepreneurship Incubator, Merck Serono Andreas Marzinzik, Director, Exploratory Medicinal Chemistry, Novartis Björn Peters, Director Business Development, Shire Marius Hoener, Senior Principal Scientist, Drug Discovery Project Team Leader, Vice Director, Roche Francoise Bono, Research Director, Sanofi Henning Nielsen, Director, Novo Nordisk Sergio Cantoreggi, CSO & Global Head of R&D, Helsinn Group Tina Flatau, VP Alliances and Project Management, Prosensa David Elder, Director Scinovo, GSK R&D Daniel Baeschlin, Director Compound Management And Engineering, Novartis Institutes of BioMedical Research Andrew Leach, Director of Computational Chemistry Europe, GSK Ton Rijnders, Scientific Director, TI Pharma Karl-Heinz Baringhaus, Head of Structure, Design & Informatics, Sanofi Aventis Francisca Zanoguera, Former Head of Discovery Bioinformatics Geneva, Merck Serono Matthias Frech, Head of Molecular Interactions & Biophysics, Merck Philippe Couttet, Head Pathway Integration, Discovery and Investigative Safety, Novartis José Duca, Head, Computer-Aided Drug Discovery, Novartis Pascal Furet, Research Director, Novartis Ulrich Schopfer, Director, Integrated Lead Discovery Head, Novartis Jens Pohlmann, Head of Chemistry, Basilea Rainer E. Martin, Principal Scientist, F. Hoffmann-La Roche, Basel Johannes Grosse, Head of Discovery Biology, Takeda Wojtek Auerbach, Senior Director, Embryonic Stem Cell Technologies, Regeneron Ali Jazayeri, Head of Protein Engineering, Heptares Adrian Gill, Head of Medicinal Chemistry , CVGI, AstraZeneca Tomas Mow, Head of Department Exploratory Toxicology, H. Lundbeck A/S Ivan Efremov, Senior Principal Scientist, Pfizer Huw Rees, Senior Principal Scientist, Pfizer Julian Woelcke, Associate Director Expertise Platform Proteases, Novartis Bharat Lagu, Associate Director, Novartis Richard Morphy, Senior Research Advisor, Lilly Atli Thorarensen, Associate Research Fellow, Pfizer Eduard Felder, Director, Head of Chemical Core Technologies Dept, Nerviano Medical Sciences Patrick Jimonet, Discovery Sourcing And Leader Global Chemical Library Team, Sanofi Ian Wall, Computational Chemist, GSK Prakash Purohit, Associate Director, Scientific Affairs, Ipsen Rod Hubbard, Professor, York and Senior Fellow, Vernalis Xavier Leroy, Associate Director, Project Leader, Actelion Sjoerd Wadman, VP R&D, Lanthio Pharma Christoph Wiessner, Head of Discovery, Asceneuron Alexander Schuhmacher, Professor, School of Applied Chemistry, Reutlingen University Axel Vater, VP Drug Discovery, Noxxon Matthew Gardener, Senior Scientist, MedImmune

Sponsors:

Day 1 – Monday 10th June

07.30 – 08.20 Registration

08.20 – 08.25 Oxford Global Welcome Address

08.25 – 08.30 Stream Chair Welcome Address

08.30 – 09.00 Keynote Presentation Collaborative Models – Different Approaches To Improve Innovation Productivity The global healthcare industry is undergoing substantial changes and adaptations to the constant decline of approved new medical entities. This decrease in internal research productivity is resulting in a major decline of patent protected sales (patent cliff) of most of the pharmaceutical companies.

Three major global adaptive trends as driving forces to cope with these challenges are evident: 1. Cut backs of internal research and development jobs in the western hemisphere 2. Follow the market growth potential of Asia by building up internal or external research and development capabilities there; 3. And finally “early innovation hunting” with an increased focus on identifying and investing in very early innovation sources within academia and small start up companies.

Paul Germann, Vice President New Frontier Science Europe, Takeda

Innovation Driven Discovery Congress Discovery Chemistry & Drug Design Congress

R&D Models For The Future Screening & Assays: Enabling Technologies Discovery Chemistry: Latest Case Studies

Stream Chair: Manfred Horst, Director Business Development, European External Scientific Affairs, Merck

Stream Chair: Henrik Konarkowski, CEO, TeaRx Stream Chair: Alex Kiselyov, President, ChemDiv

09.00 – 09.30 Stream Keynote Presentation Innovation in Drug Discovery Enabling the entrepreneur

Open source approaches

New ways of academia-industry collaboration

Leveraging the global brain pool

Ulrich Betz, Director, Department Head Innovation & Entrepreneurship Incubator, Merck Serono

Stream Keynote Presentation Integrated Lead Discovery To Tackle Difficult & Unprecedented Targets Overview of currently available lead discovery

technologies

Limitations of existing lead discovery technologies

Case studies from target-based lead discovery

Case studies from phenotypic lead discovery

Integration of lead discovery strategies

Summary and outlook

Lorenz Mayr, Vice President & Global Head, Reagents & Assay Development, AstraZeneca

Stream Keynote Presentation Discovery Research – Title to be confirmed Emilio Diez Monedero, VP MDR & Director Basic Research Centre GSK

09.30 – 10.00 Solving the Informatics Challenges in Collaborative Network Research As discovery organizations move rapidly towards a collaborative network model for research, research IT organizations are presented with significant challenges in supporting their scientists and the external partners. We will present software solutions that can help solve the problems of tech transfer and collaborative data exchange and present case studies on the use of these solutions from both the pharma/biotech and CRO point of view.

Robert Brown, Senior Director Life Sciences Research, Accelrys Inc

Solution Provider Presentation

Spinning Fragments Into Lead Molecules: A New Impulse In Fragment Based Drug Discovery ZoBio has integrated advanced & proprietary NMR

techniques into its drug discovery pipeline that yield unique synergies when combined with its other capabilities including X-ray crystallography.

ZoBio has successfully applied its technologies to more than 60 different targets including protein protein interactions, epigenetics targets and membrane protein including GPCRs to yield tractable, validated hits and leads.

This talk will describe ZoBio’s technologies and provide real life examples of how they have been used to provide our customers with ideal starting points for even the most challenging targets.

Gregg Siegal, CSO, ZoBio BV

10.00 – 11.00 Morning Refreshments One To One Meetings X 3 Exhibition & Poster Presentation Session


11.00 – 11.30 Open Innovation In Janssen Pharma The vision of the future landscape of healthcare in J&J J

Janssen Innovation Centre’s, the raison d’être

Effectively building and integrating public-private ventures (such as IMI programmes) into drug discovery efforts

Case studies on how to manage IP in PPP’s

Lessons learned

Trevor Howe, Scientific Director and Janssen Fellow

RNAi Screening: Go Big or Go Home The advent of sequencing technologies coupled to loss of function assessment is theoretically a powerful combination when directed towards target discovery for eventual pharmacological intervention. Yet, the promise of myriad validated targets arising from deep genomic and transcriptomic understanding of cellular systems interrogated by systematic RNAi assessment remains unrealized…

Vic Myer, Executive Director, Developmental and Molecular Pathways, Novartis

Centyrins, A New Biologics Platform For J&J Efficient production of multi-specific molecules that engage

more than one target at a time

Local delivery options such as pulmonary or nasal to CNS delivery

The attachment of cytotoxic drugs or attachment to nanoparticles for targeting applications

Robert Hayes, Vice President and Venture Leader Centyrex Venture, Janssen R&D

11.30 – 12.00 Solution Provider Presentation



For sponsorship opportunities please contact [email protected]

12.00 – 12.30 Innovation In Biopharma: Ipsen's Approach Overview of drug discovery innovation models in Biopharma

industry

Changing landscape in the industry

Ipsen's approach to innovation

Collaborative model - keys to success

Prakash Purohit, Associate Director, Scientific Affairs, Ipsen

Creative Collaboration Models – The Challenges For Deal-Making The drive to access innovation has generated new

creative collaboration models

These creative models require creative agreements to support them

What challenges do these agreements present and how do we address them?

Campbell Wilson, Executive Business Development Director, Science & Technology Licensing, AstraZeneca

Allosteric Interactions: Mechanism Of Actions And Consequent Biological Effects

Francoise Bono, Research Director, Sanofi

12.30 – 13.00 Mergers & Acquisitions – Title to be confirmed Björn Peters, Director Business Development, Shire

Integrated Lead Discovery – Innovation beyond Technology Drivers of change in Lead Discovery

Innovation in technology and collaborative models

The Integrated Lead Discovery strategy applied

Ulrich Schopfer, Director, Integrated Lead Discovery Head, Novartis

The Importance Of Physical Properties (Particularly Solubility) In Decreasing Drug Attrition Reasons for Attrition

Critical Role of Solubility in PK

Impact of Combinatorial and High Throughput Chemistry

Evolution of Physicochemical Properties of Marketed Drugs

Importance of lipophilicity (logP) and MP in solubility

Strategies to improve ADMET properties (including solubility)

Predicting solubility (SFI)

Impact on Various Developability Criteria

David Elder, Director Scinovo, GSK R&D

13.00 – 14.00 Lunch – Helvetia A & B & Foyer One to One Meetings x 2

mailto:[email protected]


14.00 – 14.30 Collaboration: What Is It Going To Do For Us?

Biopharma and the importance of collaborations

Collaboration options and styles

Achieving win-win

Tina Flatau, VP Alliances and Project Management , Prosensa

Flow Chemistry - An Enabling Tool in Drug Discovery Discovery chemistry

Enhanced process window

Automation in flow

Rainer E. Martin, Principal Scientist, F. Hoffmann-La Roche, Basel

Antibodies As Tools In Small Molecule Drug Discovery Antibodies have successfully addressed modulation of

protein-protein interactions in the clinic, and are set to enable the discovery of small molecules, which have similar biological activities. Such small molecules may be considered as ‘chemosuperiors’, as they can be expected to follow on from pioneering therapeutic antibodies, but display improved drug characteristics.

Antibodies have already proved to be of significant value as chaperones in crystallography.

Antibodies are now being used to define specific conformations of proteins, providing new and previously unexpected opportunities for intervention with small molecules.

Small molecule fragment screening against antibody-constrained targets offers the prospect of discovering new chemical entities, which would otherwise be unable to gain a foothold on proteins. The approach is particularly well suited to the discovery of small molecules which modulate protein-protein interactions through binding at allosteric sites.

Alastair Lawson, Senior Director of Structural Biology, UCB

14.30 – 15.00 Library-Scale Gene-Expression Profiling and Digital Open Innovation Match diseases with drugs through the transitive property of

common gene-expression changes

Realized through library-scale gene-expression profiling technology, online database of small-molecule gene-expression profiles, and simple self-service search engine

Digital open-innovation medium creates self-selected partnerships between domain-expert biologists and the owners of proprietary chemical matter

Justin Lamb, President and CEO, Genometry


Reserved: Axiogenesis





15.00 – 15.30

Public/Private Partnerships: A Potential Solution For The Modern Pharmaceutical Industry Public-private partnerships in drug discovery in the

Netherlands

Critical success factors

The European perspective

The European Lead Factory

Ton Rijnders, Scientific Director, TI Pharma

Panel Discussion: Innovations In Screening Assessing different screening approaches

Continuous hit-finding

Utilising bioinformatics tools

Advances in biologics screening

Antibody tools for screening

(Chair) Eduard Felder, Director, Head of Chemical Core Technologies Dept, Nerviano Medical Sciences Vic Myer, Executive Director, Developmental and Molecular Pathways, Novartis Alastair Lawson, Senior Director of Structural Biology, UCB

New Models For Lead Generation The risk-sharing approach for accessing innovative

chemical space

Exposing Sanofi's chemical space to new biological innovation

New models to fully exploit Sanofi's natural product universe

Peter Hamley, Global Head Parallel Synthesis & Natural Products, Sanofi Aventis

15.30 – 16.00 Virtual R&D: The Helsinn Success Story The Helsinn R&D structure and its performance

Definition of core and critical activities

CRO selection and monitoring: focus on quality and relationships

The Aloxi success story

Join forces with other mid-pharma companies

The "human factor"

Sergio Cantoreggi, CSO & Global Head of R&D, Helsinn Group

The Spiegelmer® Therapeutics Discovery Platform: From Evolution In Vitro To Efficacy In Vivo Spiegelmers are plasma-stable oligonucleotides that are

generated by in vitro evolution from random DNA or RNA libraries. They bind and neutralize a target of interest.

Similar to antibodies, Spiegelmers can inhibit large-surface interactions between proteins where small molecules often fail.

In contrast to antibodies, Spiegelmers are produced by a chemical process and stimulation of the immune system or generation of anti-drug antibodies have not been observed.

Efficacy in vivo has been shown for several Spiegelmers. Three candidates are currently in four international Phase IIa studies.

Axel Vater, VP Drug Discovery, Noxxon

Increasing Effectiveness Of Early Drug Discovery Projects Teams Integrated Lead Finding (ILF) in early drug discovery is a coordinated approach involving different disciplines. A diagnostic exercise to understand the critical factors will be presented. Key areas enabling successful lead finding will be discussed. A particular focus of the presentation will cover leadership challenges faced by R&D teams. The distributed leadership concept will be introduced and suggestions for drug discovery teams will be presented.

Guido Koch, Director in Global Discovery Chemistry, Novartis

16.00 – 16.40 Afternoon Refreshments One To One Meetings X 2 Exhibition & Poster Presentation Session

16.40 – 17.10

Is There A New Business Model For Pharma Innovation? Open innovation in the pharmaceutical industry

Examples for inside-out and outside-in processes

R&D strategies of pharmaceutical companies

New business models in R&D offer new opportunities

Alexander Schuhmacher, Professor, School of Applied Chemistry, Reutlingen University

Screening & Assays Concept of continuous hit finding

FBS-by-biochemical assays

Fluorescence lifetime as powerful new readout for lead discovery

Julian Woelcke, Associate Director Expertise Platform Proteases, Novartis

Enhancement Of Chemical Matter For Lead Finding Through Innovative Business Models Lessons learned from failure in development at Sanofi

and evolving discovery portfolio highlight the need to access improved chemicals and novel chemical space

Chemical matter improvement for Lead finding through innovative business models: risk-shared partnerships and other novel models to replace traditionnal buy-and-sell, or explore new opportunities; examples of implemented deals

Patrick Jimonet, Discovery Sourcing And Leader Global Chemical Library Team, Sanofi


17.10 – 17.40 Redefining ‘CRO’ To Mean ‘Creative Research

Opportunities’ Big Pharma’s evolving drug discovery paradigms in working

with CROs: collaboration is a two-way street

Defining metrics and successes with new paradigms

Case study-lessons learned

Bharat Lagu, Associate Director, Novartis

Gene Targeting in Embryonic Stem Cells as a Tool for New Targets Discovery, Therapeutic Antibody Production and Drug Validation Understanding the function of each gene and expression

pattern

Development of mice producing fully human monoclonal antibody

Delivering unprecedented speed and capacity for the validation of therapeutic targets in humanized mice

Wojtek Auerbach, Senior Director, Embryonic Stem Cell Technologies, Regeneron

Discovery Chemistry Case Studies: Structure Activity Relationships

Drug Residence Time

Matthias Frech, Head of Molecular Interactions & Biophysics, Merck

17.40 – 18.10 Opportunities And Challenges In Drug Discovery For Alzheimer's Disease Why is Alzheimer's Disease emerging as one of the largest

healthcare problems worldwide

What is the unmet medical need in AD

What has worked, what has failed and why, and what is currently explored clinically

What are the most promising and innovative new treatment strategies and targets in AD drug discovery

Christoph Wiessner, Head of Discovery, Asceneuron

Exploratory Toxicology Fully Integrated Into Drug Discovery In an effort to reduce toxicity-related attrition, different strategies have been implemented throughout the pharmaceutical industry. When a development candidate is selected the properties of the molecule are fixed, including those causing toxicity. Therefore, only during the drug discovery phase one has the chance to modify these properties. At Lundbeck, exploratory toxicology research has been fully integrated into the drug discovery process. The aim is to not only provide timely go/no go decisions (“fail early”), but rather also provide a direction to the drug discovery teams (“show what will not fail”), by steering away from potential liabilities during drug discovery. Examples of compound testing paradigms using early in vitro, ex vivo and in vivo assays and models to assess safety risks will be presented. Instead of testing “everything early” we aim to test “the right things at the right time” by focusing on toxicities and adverse events which occur frequently and/or have high impact during the development of novel drug candidates. Furthermore considerations for the choice of assays, including predictivity, throughput, and turn-around time will be discussed.

Tomas Mow, Head of Department Exploratory Toxicology, H. Lundbeck A/S

ATP Mediated Kinome Selectivity Impact of using kinase data generated under Km condition

for interpretation of selectivity and pharmacology

Alternative discovery paradigm for kinase drug discovery projects

Examples for several kinase project will be provided

Expansion of this to different classes of kinase inhibitors (eg. type 2) will be discussed.

Atli Thorarensen , Associate Research Fellow, Pfizer

18.10 – 18.40 Polypharmacology Presents Opportunities For Open Innovation Richard Morphy, Senior Research Advisor, Eli Lilly

Screening Of Biologics During The Lead Identification Phase: New Assay Technologies And Functional Approaches Used Moving beyond traditional antibody screening approaches

Targeting complex membrane proteins

Functional screening of biologics

Matthew Gardener, Senior Scientist, MedImmune

Challenges For Fragment-Based Drug Discovery Fragment-based methods are now successfully delivering clinical candidates, but challenges remain. For conventional targets these are mainly organisational; for non-conventional targets (such as protein-protein) there are additional technical challenges which we are only beginning to understand.

Rod Hubbard, Professor, York and Senior Fellow, Vernalis

18.40 Networking Drinks

Day 2 – Tuesday 11th June

Stream Chair

08.30 – 09.00 Keynote Presentation Using Multifactorial Data To Improve Compound Survival In Drug Discovery The incorporation of predictive toxicology approaches in early preclinical drug development will be important for reducing the attrition rate within the industry. To identify potential toxic compounds and guide medicinal chemistry efforts, targeted in vitro assays have been integrated with structure activity-relationship rules and physicochemical properties to predict in vivo effects…

William Pennie, Executive Director of Compound Safety Prediction, Pfizer

Innovation Driven Discovery Congress Discovery Chemistry & Drug Design Congress

Innovative Drug Targets Supporting Innovation: Data Integration, Analysis &

Management

Drug Design: Novel Approaches

Stream Chair: Oliver Lehner, VP Sales Europe & APAC, Definiens AG

Stream Chair: DDS

09.00 – 09.30 Stream Keynote Presentation Targets for Biologics – Choice Of Targets And Biological Approach There is significant competition on the “hot” targets, which

will result in a sorting out of those that are not “first-in-class” or “best-in-class”

New targets will create innovation in the antibody field

Novel targets may require novel approaches including use of alternative scaffolds or peptides

William Strohl, VP, Biologics Research, Johnson & Johnson

Stream Keynote Presentation The Role of Pre-Competitive Collaboration in the Search for Innovation Models in Biomedical R&D Does pre-competitive collaboration deliver true innovation

or just efficiency gains?

Hurdles and opportunities for pre-competitive collaboration

The Pistoia Alliance in the pre-competitive collaboration landscape

Michael Braxenthaler, President, Pistoia Alliance

Stream Keynote Presentation Anti-Target Modelling In Early Drug Discovery Modern drug discovery aims to achieve development compounds with a clean profile. Any effects on anti-targets (e.g. hERG, CYP2D6, CYP2C9, CYP3A4, a1a, ...) or potential toxic liabilities (e.g. Phospholipidosis, CYP induction, phototoxicity) should be avoided. Computational chemistry enables early assessment of anti-target effects of compounds as well as design principles to get rid of these activities. This presentation captures several techniques to build and validate anti-target models as well as its application in hit to lead and lead optimization. The emerging field of polypharmacology and in silico profiling of compounds will be also addressed.

Karl-Heinz Baringhaus, Head of Structure, Design & Informatics, Sanofi Aventi



CONFIRMED: Thomson Reuters






RESERVED: Certara



10.30 – 12.10 Morning Refreshments One To One Meetings X 5 Exhibition & Poster Presentation Session

12.10 – 13.10 Lunch One To One Meetings x 2





13.10 – 13.40

Target Identification In Endocrinology: Case Studies In Favour Of Private-Public Collaborations In addition to established members of endocrine systems

recently discovered factors are the ‘hot spots’ for pharmacological intervention

Enteroendocrine hormones are the main signals of the gut-brain axis which is responsible for the efficacy of bariatric surgery

The recent discovery of novel players in the complex response pattern of enteroendocrine hormones to fasting and feeding opens new opportunities for drug discovery.

Johannes Grosse, Head of Discovery Biology, Takeda

Omics Data Integration Drug-induced heart liabilities is a safety concern in drug

development

We have studied the Doxorubicin-induced cardiotoxicity mechanism at the transcriptomic (mRNA and microRNA) level in rodents and anchored these data to histopathology observation and clinical chemistry endpoints.

We have built up a transcriptomic (mRNA and microRNA) heart Atlas of 8 heart structures across species and identified heart structure specific gene signatures.

Philippe Couttet, Head Pathway Integration, Discovery and Investigative Safety, Novartis

Identification And Optimization Of Allosteric Kinase Inhibitors How to find and characterize allosteric kinase inhibitors?

Optimization of potency, selectivity, clearance, and PK

In vivo proof of concept for the allosteric paradigm on IGF1R

Andreas Marzinzik, Director, Exploratory Medicinal Chemistry, Novartis

13.40 – 14.10

Targeting The Nav1.7 Sodium Channel Mechanistic studies exploring the role of NaV1.7 in rats

and mice

Being more clinical about experimental design; addressing bias in preclinical studies

Future directions; re-evaluating the role of spinal dorsal horn neurones in models of nerve injury

Huw Rees, Senior Principal Scientist, Pfizer

Enabling Drug Discovery Through Innovative Compound Sample & Data Workflows The compound management groups of the Novartis Institutes of BioMedical Research (NIBR) are challenged by increasingly changing requirements: drug discovery project teams operate globally across the eight research sites, employ an increasing number of technologies for lead finding & lead optimisation and continue to grow the number of requested compound samples. NIBR has therefore initiated a major program called “Novartis compound bank” to transform its compound sample handling infrastructure into an adaptable, modular framework of hardware and software systems enabling not only reliable and efficient sample handling, but also flexibility in process adaptation. The presentation will detail not only NIBR’s vision for this modern infrastructure, but also the actual benefits for the drug discovery processes of the first part of the implementation.

Daniel Baeschlin, Director Compound Management And Engineering, Novartis Institutes of BioMedical Research

Reconsidering Protein-Ligand Interactions And Drug Design Through Disruptive Thinking Protein-Ligand Interactions reassessed via innovative ways

to understand how proteins function

A whole new theory of binding arising

Dynamic imprints of proteins can gate selectivity and specificity

José Duca, Head, Computer-Aided Drug Discovery, Novartis


14.10 – 14.40

Discovery And Characterization Of TAAR1 Agonists, Modulators Of Dopaminergic And Serotonergic Neurotransmission With Therapeutic Potential In Neuropsychiatric Disorders The trace amine-associated receptor 1 (TAAR1) is a G

protein-coupled receptor activated by trace amines like p-tyramine and beta-phenylethylamine, endogenous compounds with structural similarity to biogenic amines.

TAAR1 agonists were developed, characterized and, together with TAAR1 transgenic animals, used to evaluate TAAR1 as a potential drug target for neuropsychiatric disorders.

TAAR1 partial agonists are proposed to be superior to existing atypical antipsychotic drugs based on preclinical studies by displaying antipsychotic efficacy with the benefit of improved cognition and mood as well as with a reduced side effect profile (e.g., no sedation, no weight gain, no extrapyramidal symptoms).

Marius Hoener, Senior Principal Scientist, Drug Discovery Project Team Leader, Vice Director, Roche

IMI OpenPHACTS Initiative Andrew Leach, Director of Computational Chemistry Europe, GSK

Lead Optimisation Case Histories In The Diabetes And Obesity Area

Adrian Gill, Head of Medicinal Chemistry , CVGI, AstraZeneca

14.40 – 15.10 Fragments And Enablement Of Tough Targets – Beta-Secretase As The Case Study The talk will highlight application of fragment-based approaches to accelerate identification and optimization of chemical matter for a difficult target – beta-secretase. Diversity-based and knowledge-based approaches will be discussed as alternative and complementary hit ID strategies together with use of fragment-derived information to accelerate progression of a more advanced series. Multidisciplinary approach was the key to rational decision making in the hit optimization process and will be a focal point of the talk.

Ivan Efremov, Senior Principal Scientist, Pfizer

Innovation Is Fostered By Information And Knowledge Trends and strategies in information management

Henning Nielsen, Director, Novo Nordisk

Optimization of an Anti-Cancer Lead Novel microtubule destabilizers with a unique mode of

action were identified

Low solubility presented a hurdle for further development

Systematic evaluation of prodrugs provided a compound for clinical development

Jens Pohlmann, Head of Chemistry, Basilea

15.10 – 15.30 Afternoon Refreshments

15.30 – 16.00 Stabilised Receptor (StaR) Technology Enables Structure Based Drug Design For GPCRs Introduction to Heptares

Introduction to StaR technology

Utility of StaRs for SBDD

Ali Jazayeri, Head of Protein Engineering, Heptares

Successful Management Of MedImmune’s Complex And Rich Discovery Portfolio In the talk I will introduce the complexity (size and

diversity) of our MedImmune Research portfolio

Explain the way how we manage it

And show the linkage between the way it is managed to the success in delivery

Uwe Huedepohl, Vice President, R&D Project, Portfolio and Science Submission Management, MedImmune

The Design Of MDM2-p53 Antagonists In The Protein-Protein Interaction (PPI) Area Generic approaches in the design of PPI inhibitors

Pocket adapted approach: the generation of new p53-MDM2 inhibitor scaffolds by pure structure-based design

Optimization towards in vivo efficacious compounds

Pascal Furet, Research Director, Novartis


16.00 – 16.30 Purinome Targeted Libraries In Oncology Research The generation of novel chemotypes for oncology projects

expands from a canonical design of kinase-targeted compound libraries to a broader interpretation of purinome-targeted libraries (PTL).

Screening of structurally diverse ATP-binding targets calls for compound libraries covering multiple design elements, which may include phosphate surrogate moieties in ATPase inhibitors or far reaching lipophilic residues stabilizing inactive kinase conformations.

We compared overall hit rates of PTL with a simultaneously tested unbiased collection of 200,000 compounds and confirmed that a multidisciplinary support of library design translates into significantly more effective targeted libraries.

The performance analysis of various chemotypes on a panel of ATP-binding targets facilitates the exploitation of drug discovery synergies across the whole purinome

Eduard Felder, Director, Head of Chemical Core Technologies Dept., Nerviano Medical Sciences

Computational Approaches in Fragment Based Drug Discovery Development and use of computational tools for data

management and analysis, structure-based design and ligand-based design

Examples of application to drug discovery programmes

Discussion of gaps in current capabilities and efforts to address the gaps

Ian Wall, Computational Chemist, GSK

Lanthipeptides : New Therapeutic Applications for Nature’s own Stabilised Peptides Introduction to Lanthipeptides

Harnessing natural biosynthetic systems for therapeutic uses

Case study : Lantipeptides as specific GPCR agonists

Sjoerd Wadman, VP R&D, Lanthio Pharma

16.30 – 17.00 Innovation In GPCR Research And Signalling Pathways Xavier Leroy, Associate Director, Project Leader, Actelion

How Data Analysis Can Help Drug Discovery – Title to be confirmed Francisca Zanoguera, Former Head of Discovery Bioinformatics Geneva, Merck Serono

Delegates are welcome to attend the co-located presentation.

17.00 End of Conference

2013 speakers oxford global conferences are proud to present discovery combined 2013 agenda.pdf ·...

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