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Research Chemistry & Drug Discovery
Dr. Frank MOFFATTDirector of Business Development
January 2014
Team of 120+ people
•Mostly in Illkirch/Strasbourg FR (since 2002)
• Heidelberg DE, (Graffinity)
• Toledo ES, Val de Reuil FR, (In-sourcing)
• Technopôle de Sidi Thabet TN (Synthesis)
Pharma discovery specialists Science and technology oriented
Execution focused Organic synthesis & biophysical sciences
NovAliX Pharma discovery
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Drug Discovery
Organic synthesis
Biophysical
Lab-scale synthesis & integrated drug design
1. Discovery-medicinal chemistry
• Novel & diverse libraries• Graffinity® screening technology• Fragment to lead• Hit to lead• Lead optimization
2. Research & process chemistry• Building exclusivity/freedom• New chemical entities• New routes & processes• Route/process evaluation
3. Supply of chemicals• Focused libraries• Compound supply• Standards/reference materials
A. Modeling• In-silico/docking
B. Biophysical characterization
• X-Ray protein/protein-ligand interactions
• NMR• MS native protein-ligand
nano-ESI• SPR array/channel
C. Protein production• Crystallography grade
protein• Crystallization of proteins &
complexes
Insourcing Synthetic chemistry in Tunisia Novel affinity ligand design for purification of biologics
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Projects = Experience
Chemistry
• 350 Projects
• 5000 Compounds supplied
Proteins
Production
>200 Proteins produced
Kinases, NHRs, PDEs, protease, ECD of membrane protein, anti-infective targets
Structure determination
>600 Crystal structures solved
>90 Targets in the crystal gallery
Drug discovery/Graffinity
111 targets screened
Hit rate 0.1-1%
>90% of cases starting
points for synthesis found
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Discovery alliances- Kiowa Hakko Kirin
Fragment-based drug discovery alliance (Jan 2013)- Teijin Pharmaceutical Limited
Multi-target drug discovery alliance (Nov 2011)
Technology & capabilities deal
- Servier SPR screening collaboration (Nov 2012)
- Shionogi SPR based FBDD screening collaboration (Mar 2011)
- Janssen (J&J) several years, multi-sites medchem support collaboration (Jan
2011)
Service agreements
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1. Pharmaceuticals
2. Agrochemicals
3. Cosmetics
4. Perfume
5. Fine chemicals
1. Pharmaceuticals
2. Agrochemicals
3. Cosmetics
4. Perfume
5. Fine chemicals
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Chemical synthesis in Tunisia
Cost competitive
Pharmaceutical industry quality
Well qualified & trained staff
High ratio of PhDs
Communications & management via Strasbourg
Secure & efficient systems
TUNISIA Sidi Thabet laboratory
Complex chemistry
O
O
O
O
OP
ONH
OHN
O
O
HN
O
R
O 14
14nO
OH
N
NH
NH
NH
HN
O
OO
O
HN
OOHN
NH
NH2
HN
HN
O
Cyclosporin A: peptide chemistry & preparative LC-MS purification stages
S
O
O
HN
O N
SF
O
HN
NNH
HN
OH
OH
HNOH
NH Natural toxin 19 stepsSophisticated skeletons
8 Step set-up for asymmetric reduction
catayst screen
Series of functionalized analogues of PEG phospholipids
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Biophysical toolbox
Affinity, stoichiometry thermodynamics
Structure
Structure,dynamics
Stoichiometryaffinity
ranking
specificity
Stability/aggregation
Binding mode
AffinityKd, Kon, koff
Hits Characterization & optimization
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Protein
Case studies
1. HITS: Graffinity® hits for matrix metaloproteinase MMP-13
2. PAPER ROUTE design: Vitamin A: novel route required
3. OPTIMIZATION: Finding accessible chemistry
4. FEASIBILITY: Unprecedented reaction
5. HIT TO LEAD: - kinase for osteoporosis
6. FTE collaborations
7. NATIVE MS - rRORα from Insect cells
8. NATIVE MS - galectin-3/lactosamine der.
9. VIRTUAL SCREENING: HSP90
10. FRAGMENT BASED DRUG DESIGN: PIM1 - fragment hit to lead
11. XRD PROTEIN-LIGAND: kinases
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For details [email protected]
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Additional concise information
LinkedIn company profileshttp://tiny.cc/novalixhttp://tiny.cc/Graffinity
Useful hint – don’t forget to check out our product & service tab on our LinkedIn profiles
Conclusion – the obvious choice…
1. When innovative chemistry is needed
or
2. When biophysical or in silico expertize is advantageous
or
3. When an integrated drug discovery service is needed
or
1. When cost effectiveness in important
or
2. When reliability is critical
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NovAliX drug discovery & chemistry
Dr. Frank MOFFATTDirector of Business Development
[email protected]/handy/cell
+41 7 86 49 60 50
Let’s talk about how to support your critical projects
& your personal success
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