1. Research Chemistry & Drug
Discovery
Dr. Frank MOFFATT
Director of Business Development
January 2014
fm@novalix-pharma.com

2. NovAliX Pharma discovery
Team of 120+ people
•Mostly in Illkirch/Strasbourg FR (since 2002)
Organic
synthesis
• Heidelberg DE, (Graffinity)
Biophysical
• 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
Drug
Discovery
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3. Lab-scale synthesis & integrated drug design
1. Discovery-medicinal chemistry
A. Modeling
• In-silico/docking
Novel & diverse libraries
Graffinity® screening technology
B. Biophysical characterization
Fragment to lead
• X-Ray protein/protein-ligand
Hit to lead
interactions
Lead optimization
• NMR
• MS native protein-ligand
2. Research & process chemistry
nano-ESI
• Building exclusivity/freedom
• SPR array/channel
• New chemical entities
• New routes & processes
C. Protein production
• Route/process evaluation
• Crystallography grade protein
• Crystallization of proteins &
3. Supply of chemicals
complexes
• Focused libraries
• Compound supply
• Standards/reference materials
 Insourcing
 Synthetic chemistry in Tunisia
 Novel affinity ligand design for purification of biologics
•
•
•
•
•
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4. Projects = Experience
Chemistry
Proteins
• 350 Projects
Production
• 5000 Compounds supplied

Drug discovery/Graffinity
Kinases, NHRs, PDEs, protease, ECD of
membrane protein, anti-infective
targets
111 targets screened
Hit rate 0.1-1%
>90% of cases starting
points for synthesis found
>200 Proteins produced
Structure determination

>600 Crystal structures solved

>90 Targets in the crystal gallery
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5. Service agreements
 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)
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6. 1.
1.
2.
2.
3.
3.
4.
4.
5.
5.
Pharmaceuticals
Pharmaceuticals
Agrochemicals
Agrochemicals
Cosmetics
Cosmetics
Perfume
Perfume
Fine chemicals
Fine chemicals
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7. Chemical synthesis in Tunisia
Cost competitive
Pharmaceutical industry quality
Well qualified & trained staff
High ratio of PhDs
TUNISIA
Sidi Thabet laboratory
Communications & management via Strasbourg
Secure & efficient systems
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8. Complex chemistry
OH
H
N
HN
Sophisticated skeletons
HN
NH
NH
OH
OH
N
Natural toxin
19 steps
O
O
H
N
R
O
n
O
HN
O
O
O
H
N
H
N
HN
O
HN
O
NH
N
O
N
H
O
N
H
O
14
O
Series of
functionalized
analogues of PEG
phospholipids
O
NH
O
14
Cyclosporin A: peptide chemistry &
preparative LC-MS
purification stages
NH2
O
N
H
O
OH
O
O
P
O
H
N
HN
O
S
O
O
S
N
F
8 Step set-up for
asymmetric reduction
catayst screen
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9. Biophysical toolbox
Protein

Hits
Binding
mode

Characterization & optimization
Affinity, stoichiometry
thermodynamics
Structure,
dynamics
Structure
Stability/aggre Stoichiometry
affinity
gation
specificity
ranking
Affinity
Kd, Kon, koff
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10. For details CONTACT
fm@novalix-pharma.com
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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11. Additional concise information
LinkedIn company profiles
http://tiny.cc/novalix
http://tiny.cc/Graffinity
Useful hint – don’t forget to check out our product & service tab on our
LinkedIn profiles
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12. 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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13. NovAliX drug discovery & chemistry
Let’s talk about how to support
your critical projects
& your personal success
Dr. Frank MOFFATT
Director of Business Development
fm@novalix-pharma.com
Mobile/handy/cell
+41 7 86 49 60 50
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