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From
   Chemistry
       to
Drug Candidates
Agenda

  •   Introduction of Mercachem
  •   Drug Discovery & trends
  •   Development of services of Mercachem
  •   Project examples




                                             1
Facts and figures


   Innovative Netherlands-based chemistry service provider in
   discovery chemistry, medicinal chemistry and process research

   One of the leading CRO’s in Europe

   110 employees (45% Ph.D. and 55% M.Sc./B.Sc.)

   Spin-out of University of Nijmegen

   Founded in 1997
Facts and figures


   4,000 m2 modern research facilities with 10 synthesis
   laboratories (120 fume hoods)

   Moved to a new state-of-the-art laboratory facility in 2006

   Located in Nijmegen (2 sites)

   Independent, privately owned
Services

   Exclusive
   - Discovery chemistry services
   - Medicinal chemistry services
   - Process research & development services
   to support research and development programs of
   companies and research institutes worldwide

   Regions:
   - Europe
   - US
   - Japan
Markets

Pharmaceuticals (~70%)

Agrochemicals (~10 %)

Animal Health (~5%)

Flavors and fragrances (~5%)

Speciality chemicals (~5%)
• cosmetics
• monomers
• diagnostics

Research organizations (~5%)
Drug Discovery
 Definition: process by which drugs are discovered and/or designed

 Process:
 • Identification & validation of target & candidates
 • Synthesis, optimization & characterization
 • Screening and assays for therapeutic efficacy
 • Drug development
 • Clinical trials

 Despite advances in technology and understanding of biology
 drug discovery is still:
 • Lengthy, expensive, difficult, and inefficient process
 • Low rate of new therapeutic discovery

 Currently:
 Research and development cost of each NME: ~ US$1.8 billion
Drug Discovery pipeline




Costs (m$)
(Out of pocket)


Costs (m$)                  8
(capitalized)
Drug Discovery pipeline




   UMC                                UMC


             Mercachem

                                            Synthon


                         Former Organon
Trends in pharmaceutical research

  Mergers and acquisitions at big pharma
  (Organon, Schering-Plough, MSD)

  R&D is moving from big to medium to small specialized
  companies

  Outsourcing of R&D is increasing
        - Total value: 15-24 billion$
        - Increase: 10-20% per year

  Increasing parts of drug discovery are being outsourced

  Virtual pharma

  Open innovation


                                                            10
Outsourcing

     Reasons:

     •   Focus on primary activities
     •   Expertise
     •   New methodologies / technologies
     •   Cost effective
     •   Fasten product development (time to market)
     •   Capacity & Quality




                                                       11
Development of Services
Phase 0: Start

   Start of Mercachem
       •   Two founders with PhD in Organic Chemistry
       •   Market trend for outsourcing and specialized companies
       •   Market niche for chemistry outsourcing
       •   Business plan, financing
       •   Start (1997)

   Characteristics:
      • Independent
      • Professional
      • Pragmatic
      • Product & services according to market needs
      • Compete on quality and innovation

                                                                    12
Development of Services
Phase 1: discovery chemistry

   Market trends (1996-2001):

       •   Outsourcing of small parts of drug discovery
       •   Outsourcing of non-IP projects
       •   Limited outsourcing of biology
       •   Pharma company in charge & initiates projects




                                                           13
Development of Services
Phase 1: discovery chemistry

   Discovery Chemistry Services:

   Lab-scale synthesis of:
      • Research compounds
      • Scaffolds and building blocks
      • Reference compounds and metabolites
      • Synthesis of compound libraries
      • Development of novel chemistries

   Project Goals:
      • Preparation of (new) molecules for testing
      • Method of preparation is not important


                                                     14
Drug Discovery pipeline




       Discovery chemistry
Development of Services
Phase 2: Process R&D services

   Market trends (2002-2005):

       •   Outsourcing of bigger parts of drug discovery
       •   Outsourcing of more IP sensitive projects
       •   Increasing outsourcing of biology
       •   Pharma company in charge & initiates projects
       •   Upcoming competition from low-cost countries
       •   Decreasing nr of new drugs entering the market
       •   Patent cliffs
       •   Mergers & acquisitions (M&A)
       •   Increasing need for innovation




                                                            16
Development of Services
Phase 2: Process R&D services


   Process Research Services:
       • Route development and route scouting
       • Process optimization and catalyst screening
       • Scale-up and small bulk supply
         (~1 kg, non-GMP)

   Project Goals:
      • Candidate or lead molecule is known
      • Development and optimization of
        method of preparation
      • Method development & Scale-up for
        material supply regarding clinical studies (GMP)


                                                           17
Drug Discovery pipeline




       Discovery chemistry


                         Process R&D
Development of Services
Phase 3: Medicinal Chemistry services

   Market trends (2006-2011):

       •   Outsourcing of complete drug discovery projects
       •   Outsourcing of IP sensitive projects
       •   Both pharma company and CRO in charge
       •   Both pharma company and CRO initiates projects
       •   Increasing competition from low-cost countries
       •   Increasing M&A




                                                             19
Development of Services
Phase 3: Medicinal Chemistry services


  Medicinal Chemistry Services:
     •   Hit Finding , Hit optimization
     •   Hit-to-Lead
     •   Lead Optimization
     •   ADME

  Project Goals:
     • Design of molecules based on target information
     • Preparation and optimization of molecules with the right
       properties
     • Screening compounds against their properties
     • Combination of chemistry and biology


                                                                  20
Drug Discovery pipeline




        Discovery chemistry


                           Process R&D


     Medicinal chemistry
Integrated services



       Target             Assay         Hit            Lead         Preclinical      IND filing   Phase 1
    identification     development   finding       optimization    development


                     • Discovery Chemistry                        • Process chemistry
                                       • Medicinal Chemistry



                                               Skilled chemists




                Knowledge
               management                                                         Facilities/Equipment
Mercachem’s strengths
  Unprecedented knowledge solving synthetic challenges by
  team of experienced chemists and knowledge management

  Creative and independent thinking complimentary to customer
  knowhow

  Strong communication skills and proactive attitude when
  project requires

  Reliability reaching success with respect to quality and time

  High impact and high productivity due to combination of
  creativity, proactivity and effective infrastructure
Performance in 2010


     Number of active customers      : > 60
     Number of projects              : 205
     Number of compounds synthesized : ~ 4,500
     Delivery rate                   : 98%
Patents and publications
  Patents and publications:
  • WO2009007098 (Syngenta)
  • WO2009003650 (Bayer CropScience)
  • WO2005019208 (Grünenthal)
  • WO2004016581, WO2004074266 and WO2005028479 (Janssen)
  • WO2003171374 (Johnson & Johnson)


  • Synth. Comm., 2011, 41, 3246 (Janssen)
  • Biorg. Med. Chem. Lett., 2010, 20, 4350 (MSD Newhouse)
  • Eur. J. Org. Chem, 2010, 15, 2852 (Janssen)
  • Tet. Lett., 2010, 51, 543 (Janssen)
  • Synth. Comm., 2006, 36, 365 (Esperion)
  • Biorg. Med. Chem., 2005, 13, 223 (Esperion)
Multidisciplinary Integration


                                Partnerships:

                                ZoBio Leiden
                                FBLG, NMR, Biacore

                                Proqinase Freiburg
                                Cancer pharmacology

                                Vichem Budapest
                                Kinase Inhibitor Library

                                Life Science Park Oss
                                Screening Facilities
                                (HTS, uHTS)
                                100.000 Library




                                                    28
Project Example:
Reverse Transcriptase inhibitors
 Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTI’s)
 anti HIV-drugs

 Collaboration between Janssen Research Foundation and Mercachem

  In silico design
  New molecules designed by molecular modeling.
  X-ray crystallography of HIV reversed transcriptase complexed with key
  analogues
  Result: DAPY (DiArylPYrimidine) compounds
Project Example:
Reverse Transcriptase inhibitors
 Project
 Development & synthesis of 2nd generation DAPY compounds

 Results
 • 2 years of synthesis with a team of 3 chemists
 • 280 compounds synthesized
 • Several patents and publications (novel routes & compounds)




  References
  1. R. Leenders et al. Tetrahedron Lett. 2010, 51, 543 (patent: U.S. 7276510, 2007)
  2. R. Leenders et al. Synth. Comm. 2010, accepted for publication (patent: WO 2005/028479)
  3. R. Leenders et al. Eur. J. Org. Chem. 2010, 2852 (patent: WO2004/074266)
  4. P. Janssen et al. J. Med. Chem. 2005, 48, 1901 (review)
Project Example:
Dr. August Wolff – Mercachem collaboration in Medicinal chemistry

   Dr. August Wolff Arzneimittel GmbH & Co. KG and Mercachem BV
     start two drug development collaborations
   Bielefeld, Germany & Nijmegen, the Netherlands – August 26, 2010.
      Dr. August Wolff GmbH & Co. KG Arzneimittel and Mercachem have
      started two multi-year drug development collaborations.
   Dr. August Wolff GmbH & Co. KG Arzneimittel have licensed a number of
      patents from universities that cover novel classes of molecules with
      potential use in dermatology. Mercachem is responsible for
      medicinal chemistry and project management with the goal to
      further improve the properties of these molecules and to develop
      them into clinical candidates.
Project Example:
PDE inhibitors for Neglected Tropical Diseases

Project T4-302:
PDE inhibitors for Neglected Tropical Diseases
Focus: African Sleeping Sickness
Parasitic Disease (Trypanosome brucei)
100% fatal if untreated
50 million people at risk
Present Medication: A disgrace of modern pharmaceutical sciences
                     old and toxic (~10% patients die from side effects),
                     painful, resistance
Aim of T4-302:
A PDE (PhosphoDiEsterase) inhibitor as novel and well tolerated
medication for the African sleeping sickness
                                            Lead compound




                                                               PDE
Project Example:
PDE inhibitors for Neglected Tropical Diseases

 Project T4-302:
 PDE inhibitors for Neglected Tropical Diseases

  Mercachem:
  • participates in TIPharma (Top Institute Pharma)
  • project management, synthesis, SAR, medicinal chemistry

  PARTNERS IN CONSORTIUM
  • Mercachem, Nijmegen NL
  • Nycomed Pharma, Zurich CH
  • Top Institute Pharma
  • Vrije Universiteit, Amsterdam NL
  • University of Berne, CH
  • IOTA pharmaceuticals, Cambridge UK
  • Drugs for Neglected Disease initiative, Geneva CH
  • Koninklijk instituut van de Tropen, Amsterdam NL
Project Example:
PDE inhibitors for Neglected Tropical Diseases
Volkskrant 13-09-2011
www.mercachem.com
           Dr. Eelco Ebbers
           eelco.ebbers@mercachem.com

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Mercachem - eelco ebbers 22092011

  • 1. From Chemistry to Drug Candidates
  • 2. Agenda • Introduction of Mercachem • Drug Discovery & trends • Development of services of Mercachem • Project examples 1
  • 3. Facts and figures Innovative Netherlands-based chemistry service provider in discovery chemistry, medicinal chemistry and process research One of the leading CRO’s in Europe 110 employees (45% Ph.D. and 55% M.Sc./B.Sc.) Spin-out of University of Nijmegen Founded in 1997
  • 4. Facts and figures 4,000 m2 modern research facilities with 10 synthesis laboratories (120 fume hoods) Moved to a new state-of-the-art laboratory facility in 2006 Located in Nijmegen (2 sites) Independent, privately owned
  • 5. Services Exclusive - Discovery chemistry services - Medicinal chemistry services - Process research & development services to support research and development programs of companies and research institutes worldwide Regions: - Europe - US - Japan
  • 6. Markets Pharmaceuticals (~70%) Agrochemicals (~10 %) Animal Health (~5%) Flavors and fragrances (~5%) Speciality chemicals (~5%) • cosmetics • monomers • diagnostics Research organizations (~5%)
  • 7. Drug Discovery Definition: process by which drugs are discovered and/or designed Process: • Identification & validation of target & candidates • Synthesis, optimization & characterization • Screening and assays for therapeutic efficacy • Drug development • Clinical trials Despite advances in technology and understanding of biology drug discovery is still: • Lengthy, expensive, difficult, and inefficient process • Low rate of new therapeutic discovery Currently: Research and development cost of each NME: ~ US$1.8 billion
  • 8. Drug Discovery pipeline Costs (m$) (Out of pocket) Costs (m$) 8 (capitalized)
  • 9. Drug Discovery pipeline UMC UMC Mercachem Synthon Former Organon
  • 10. Trends in pharmaceutical research Mergers and acquisitions at big pharma (Organon, Schering-Plough, MSD) R&D is moving from big to medium to small specialized companies Outsourcing of R&D is increasing - Total value: 15-24 billion$ - Increase: 10-20% per year Increasing parts of drug discovery are being outsourced Virtual pharma Open innovation 10
  • 11. Outsourcing Reasons: • Focus on primary activities • Expertise • New methodologies / technologies • Cost effective • Fasten product development (time to market) • Capacity & Quality 11
  • 12. Development of Services Phase 0: Start Start of Mercachem • Two founders with PhD in Organic Chemistry • Market trend for outsourcing and specialized companies • Market niche for chemistry outsourcing • Business plan, financing • Start (1997) Characteristics: • Independent • Professional • Pragmatic • Product & services according to market needs • Compete on quality and innovation 12
  • 13. Development of Services Phase 1: discovery chemistry Market trends (1996-2001): • Outsourcing of small parts of drug discovery • Outsourcing of non-IP projects • Limited outsourcing of biology • Pharma company in charge & initiates projects 13
  • 14. Development of Services Phase 1: discovery chemistry Discovery Chemistry Services: Lab-scale synthesis of: • Research compounds • Scaffolds and building blocks • Reference compounds and metabolites • Synthesis of compound libraries • Development of novel chemistries Project Goals: • Preparation of (new) molecules for testing • Method of preparation is not important 14
  • 15. Drug Discovery pipeline Discovery chemistry
  • 16. Development of Services Phase 2: Process R&D services Market trends (2002-2005): • Outsourcing of bigger parts of drug discovery • Outsourcing of more IP sensitive projects • Increasing outsourcing of biology • Pharma company in charge & initiates projects • Upcoming competition from low-cost countries • Decreasing nr of new drugs entering the market • Patent cliffs • Mergers & acquisitions (M&A) • Increasing need for innovation 16
  • 17. Development of Services Phase 2: Process R&D services Process Research Services: • Route development and route scouting • Process optimization and catalyst screening • Scale-up and small bulk supply (~1 kg, non-GMP) Project Goals: • Candidate or lead molecule is known • Development and optimization of method of preparation • Method development & Scale-up for material supply regarding clinical studies (GMP) 17
  • 18. Drug Discovery pipeline Discovery chemistry Process R&D
  • 19. Development of Services Phase 3: Medicinal Chemistry services Market trends (2006-2011): • Outsourcing of complete drug discovery projects • Outsourcing of IP sensitive projects • Both pharma company and CRO in charge • Both pharma company and CRO initiates projects • Increasing competition from low-cost countries • Increasing M&A 19
  • 20. Development of Services Phase 3: Medicinal Chemistry services Medicinal Chemistry Services: • Hit Finding , Hit optimization • Hit-to-Lead • Lead Optimization • ADME Project Goals: • Design of molecules based on target information • Preparation and optimization of molecules with the right properties • Screening compounds against their properties • Combination of chemistry and biology 20
  • 21. Drug Discovery pipeline Discovery chemistry Process R&D Medicinal chemistry
  • 22. Integrated services Target Assay Hit Lead Preclinical IND filing Phase 1 identification development finding optimization development • Discovery Chemistry • Process chemistry • Medicinal Chemistry Skilled chemists Knowledge management Facilities/Equipment
  • 23. Mercachem’s strengths Unprecedented knowledge solving synthetic challenges by team of experienced chemists and knowledge management Creative and independent thinking complimentary to customer knowhow Strong communication skills and proactive attitude when project requires Reliability reaching success with respect to quality and time High impact and high productivity due to combination of creativity, proactivity and effective infrastructure
  • 24. Performance in 2010 Number of active customers : > 60 Number of projects : 205 Number of compounds synthesized : ~ 4,500 Delivery rate : 98%
  • 25. Patents and publications Patents and publications: • WO2009007098 (Syngenta) • WO2009003650 (Bayer CropScience) • WO2005019208 (Grünenthal) • WO2004016581, WO2004074266 and WO2005028479 (Janssen) • WO2003171374 (Johnson & Johnson) • Synth. Comm., 2011, 41, 3246 (Janssen) • Biorg. Med. Chem. Lett., 2010, 20, 4350 (MSD Newhouse) • Eur. J. Org. Chem, 2010, 15, 2852 (Janssen) • Tet. Lett., 2010, 51, 543 (Janssen) • Synth. Comm., 2006, 36, 365 (Esperion) • Biorg. Med. Chem., 2005, 13, 223 (Esperion)
  • 26. Multidisciplinary Integration Partnerships: ZoBio Leiden FBLG, NMR, Biacore Proqinase Freiburg Cancer pharmacology Vichem Budapest Kinase Inhibitor Library Life Science Park Oss Screening Facilities (HTS, uHTS) 100.000 Library 28
  • 27. Project Example: Reverse Transcriptase inhibitors Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTI’s) anti HIV-drugs Collaboration between Janssen Research Foundation and Mercachem In silico design New molecules designed by molecular modeling. X-ray crystallography of HIV reversed transcriptase complexed with key analogues Result: DAPY (DiArylPYrimidine) compounds
  • 28. Project Example: Reverse Transcriptase inhibitors Project Development & synthesis of 2nd generation DAPY compounds Results • 2 years of synthesis with a team of 3 chemists • 280 compounds synthesized • Several patents and publications (novel routes & compounds) References 1. R. Leenders et al. Tetrahedron Lett. 2010, 51, 543 (patent: U.S. 7276510, 2007) 2. R. Leenders et al. Synth. Comm. 2010, accepted for publication (patent: WO 2005/028479) 3. R. Leenders et al. Eur. J. Org. Chem. 2010, 2852 (patent: WO2004/074266) 4. P. Janssen et al. J. Med. Chem. 2005, 48, 1901 (review)
  • 29. Project Example: Dr. August Wolff – Mercachem collaboration in Medicinal chemistry Dr. August Wolff Arzneimittel GmbH & Co. KG and Mercachem BV start two drug development collaborations Bielefeld, Germany & Nijmegen, the Netherlands – August 26, 2010. Dr. August Wolff GmbH & Co. KG Arzneimittel and Mercachem have started two multi-year drug development collaborations. Dr. August Wolff GmbH & Co. KG Arzneimittel have licensed a number of patents from universities that cover novel classes of molecules with potential use in dermatology. Mercachem is responsible for medicinal chemistry and project management with the goal to further improve the properties of these molecules and to develop them into clinical candidates.
  • 30. Project Example: PDE inhibitors for Neglected Tropical Diseases Project T4-302: PDE inhibitors for Neglected Tropical Diseases Focus: African Sleeping Sickness Parasitic Disease (Trypanosome brucei) 100% fatal if untreated 50 million people at risk Present Medication: A disgrace of modern pharmaceutical sciences old and toxic (~10% patients die from side effects), painful, resistance Aim of T4-302: A PDE (PhosphoDiEsterase) inhibitor as novel and well tolerated medication for the African sleeping sickness Lead compound PDE
  • 31. Project Example: PDE inhibitors for Neglected Tropical Diseases Project T4-302: PDE inhibitors for Neglected Tropical Diseases Mercachem: • participates in TIPharma (Top Institute Pharma) • project management, synthesis, SAR, medicinal chemistry PARTNERS IN CONSORTIUM • Mercachem, Nijmegen NL • Nycomed Pharma, Zurich CH • Top Institute Pharma • Vrije Universiteit, Amsterdam NL • University of Berne, CH • IOTA pharmaceuticals, Cambridge UK • Drugs for Neglected Disease initiative, Geneva CH • Koninklijk instituut van de Tropen, Amsterdam NL
  • 32. Project Example: PDE inhibitors for Neglected Tropical Diseases Volkskrant 13-09-2011
  • 33. www.mercachem.com Dr. Eelco Ebbers eelco.ebbers@mercachem.com