1. NAEJA Pharmaceutical Inc.
INTEGRATED MEDICINAL CHEMISTRY
International Research for Global Health

2. 1987 1998
SYNPHAR
DRISCORP Inc.
LABORATORIES INC.
Drug Discovery Company Contract Research Company
Over 120 published patents (ID, Major Pharma Contracts
Inflammation, Cancer) 25 Scientific staff
60 Scientific staff Strong Chemistry team
Multidisciplinary team
State of the art facilities
Worldwide Contacts
1999
NAEJA PHARMACEUTICAL INC.

3. NAEJA PHARMACEUTICAL INC.
Drug Discovery Contract Research Organization
Private, revenue generating company
Based in Edmonton, Alberta, Canada

5. NAEJA PHARMACEUTICAL INC.
Drug Discovery Contract Research Organization
Private, revenue generating company
Based in Edmonton, Alberta, Canada
63,000 ft2 well equipped laboratory facility
Vast medicinal chemistry expertise
Well-established multidisciplinary teams

6. Staff
75% Chemistry
10% Biological/ADME
5% Analytical Support
10% G & A
The majority of scientists (over 90%) hold Ph.D. degrees

7. NAEJA’s Core Expertise
New Lead Early Early Development
Medicine Target Hit identifi Lead IND Clinical Clinical Portfolio Phase Phase
Proposal Validation Validation cation Optimization Enabling Safety Efficacy Preparation II III Launched
MILESTONE
MILESTONE
MILESTONE
MILESTONE
MILESTONE
MILESTONE
MILESTONE
MILESTONE
MILESTONE
MILESTONE
MILESTONE
Lead Optimization
Ligand Identification
Computational Chemistry Pharmacokinetics /
Computational Chemistry Metabolism (ADME)
Parallel Synthesis
QSAR Preclinical
Compound Library
Targeted Library Toxicology
Medicinal Chemistry
Generation Microbiology
Process Development
Enzyme Kinetics
Scale-up

8. Medicinal Chemistry Programs by Disease
Area (%)
5
15 25
Antibacterial
Antifungal
Antiviral
Cancer
CVD
15 CNS
Other
20
5
5

9. Clients by Geographical Location since 1999 (%)
10
US
25 Canada
52
Europe
Asia
26

10. Clients by Industry Category since 1999 (% revenue)
30
Large Pharma
Mid-Size
65
Small Biotech
15

11. Chemistry Services
Full FTE: medicinal, synthetic, and process chemists.
Medicinal chemistry programs: hit to candidate including
process development (22 L).
Custom synthesis.
Chemical Information Support
SciFinder™, Reaxys™, ACS journals online, & CISTI.

12. Computational Chemistry Services
Hit Discovery: ligand docking
Sybyl™, Glide/ pharmacophore generation
Schrödinger™
Lead Optimization: ligand docking
Sybyl™, Glide/ QSAR
Schrödinger™
Physical Properties: pKa, log P, log D, & solubility
ACD™ software

13. Chemistry Infrastructure:
•Small scale synthesis laboratories (mg scale)
•Larger scale synthesis (gram – kg scale)
•Microwave reactors
•Hydrogenation facility
•Preparative Chromatography (UV and LC guided)
•Two dedicated analytical suites
•Two 400 MHz NMR

14. Analytical Equipment:
Instrumentation Details internal /
external
1 LC-MS Systems Waters:ZQ with Alliance LC , SQD with Aquity UPLC Internal
systems with PDA detectors
2 LC-MS/MS Systems Waters: Quattro-II with Alliance LC with PDA Detector, Internal
TQD with Aquity UPLC systems with PDA detector
3 HPLC Waters HPLC (Alliance, 600 Series) and Aquity UPLC with Internal
PDA and ELSD detectors
4 Elemental Analysis (CHN) Costech Internal
5 NMR Varian – 400 MHz Internal
6 IR Shimadzu IR 460 Internal
7 Prep-HPLC Preparative HPLC, One complete MS, UV directed Internal
Auto-purification unit

15. Drug Metabolism / Pharmacokinetics: In vitro
Bioanalytical Assay Development
Solution Properties (Solubility, Stability)
In vitro Absorption (Caco 2, Transport
Mechanism)
In vitro Metabolism (CYP 450 – Inhibition,
Drug-Drug Interaction)
Animal studies

16. Drug Metabolism / Pharmacokinetics: In vivo
Bioavailability
Plasma Concentration (AUC, Half-life, Cmax,
Clearance and volume of distribution
Tissue concentration/distribution
In vivo metabolite profiling
Acute & sub acute toxicological evaluation in
rodents

17. Case Studies: Med Chem Programs
Antibacterial:
•β-Lactamase Inhibitor - Tazobactam
•4-year SAR Program
•Design, Synthesis, Screening
Hit Lead Pre-Candidate Candidate Market

18. Case Studies: Med Chem Programs
NSAID:
•COX-1 Inhibitor – Mofezolac (Disopain™)
•Design, Synthesis
Hit Lead Pre-Candidate Candidate Market

19. Case Studies: Med Chem Programs
Antifungal:
•Undisclosed Target
•2-year SAR Program
•6 FTE’s at NAEJA supported by client
•Design, Synthesis, Screening and DPMK
•2 Patents: US 2005/0070503; WO 2005/013892
Hit Lead Pre-Candidate Candidate PIII

20. Case Studies: Med Chem Programs
Antibacterial:
•β-lactamase inhibitors (Syn2190)
•3-year SAR Program
•13 FTE’s at NAEJA supported by client
•Synthesized >700 analogues
•Tested in vitro and in vivo efficacy/DMPK
Hit Lead Pre-Candidate Candidate Market*
* Diagnostic tool

21. Case Studies: Med Chem Programs
Cardiovascular:
Factor Xa (Fxa) inhibitors
2-year SAR Program
8 FTE’s at NAEJA supported by client
Designed and Synthesized >200 analogues
Hit Lead Pre-Candidate Candidate PII

22. Case Studies: Med Chem Programs
Cardiovascular:
Undisclosed targets
3-year SAR Program
13 FTE’s at NAEJA supported by client
Design, Synthesis, DMPK, animal efficacy
Hit Lead Pre-Candidate Candidate PIIb

23. Case Studies: Med Chem Programs
Dermatology:
Androgen Receptor Antagonist - Acne
2-year SAR and Process Development
2 FTE’s at NAEJA supported by client
Design and Synthesis
Hit Lead Pre-Candidate Candidate PI

24. Director NAEJA FTE’s
100% PhD’s
PhD’s & postdocs by location
Project
Canada
Coordinator
100% PhD’s
US
Europe
Asia
Japan
Scientist
90% PhD’s

25. Competitive Advantage
• A proven track record of achievements
• Established Integrated Multi-Disciplinary Teams:
– Medicinal Chemistry- Lead Optimization/Scale Up Synthesis
– Biopharmaceutical Profiling
– Biochemistry
– Microbiology
• Fully Equipped Drug Discovery Laboratories
• Highly Competitive Rates
• Access to State of the Art Animal Facilities

26. Contact Information
Mr. Christopher G. Micetich
President and CEO
cmicetich@naeja.com
Dr. Sameeh M. Salama
Senior Director, Business Development
ssalama@naeja.com
NAEJA Pharmaceutical Inc.
4290-91A Street, Edmonton, Alberta, Canada. T6E 5V2
Tel: (780) 462-4044; Fax: (780) 461-0196
www.naeja.com