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International Research for Global Health NAEJA Pharmaceutical Inc. INTEGRATED MEDICINAL CHEMISTRY
International Research for Global Health
NAEJA Pharmaceutical Inc.
INTEGRATED MEDICINAL CHEMISTRY
SYNPHAR LABORATORIES INC.
DRISCORP Inc.
NAEJA PHARMACEUTICAL INC.
1987
1999
1998
Drug Discovery Company
Over 120 published patents (ID,
Inflammation, Cancer)
60 Scientific staff
Multidisciplinary team
State of the art facilities
Worldwide Contacts
Contract Research Company
Major Pharma Contracts
25 Scientific staff
Strong Chemistry team
NAEJA PHARMACEUTICAL INC.
� Drug Discovery Contract Research Organization
� Private, revenue generating company
� Based in Edmonton, Alberta, Canada
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
Staff
� 75% Chemistry
� 10% Biological/ADME
� 5% Analytical Support
� 10% G & A
� The majority of scientists (over 90%) hold Ph.D. degrees
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New New Medicine Medicine ProposalProposal
TargetValidation
HitValidation
Leadidentification
LeadOptimization
IND Enabling
EarlyClinicalSafety
EarlyClinicalEfficacy
DevelopmentPortfolio
PreparationPhase
IIPhase
III Launched
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Ligand Identification
Computational Chemistry
QSAR
Targeted Library Generation
Lead Optimization
Pharmacokinetics / Metabolism (ADME)
Preclinical Toxicology
Microbiology
Enzyme Kinetics
Computational Chemistry
Parallel Synthesis
Compound Library
Medicinal Chemistry
Process Development
Scale-up
NAEJA’s Core Expertise
Medicinal Chemistry Programs by Disease Area (%)
25
20
55
15
15
5
Antibacterial
Antifungal
Antiviral
Cancer
CVD
CNS
Other
Clients by Geographical Location since 1999 (%)
52
26
25
10
US
Canada
Europe
Asia
Clients by Industry Category since 1999 (% revenue)
65
15
30
Large Pharma
Mid-Size
Small Biotech
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.
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, & solubilityACD™ software
•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
Chemistry Infrastructure:
InternalPreparative HPLC, One complete MS, UV directed
Auto-purification unit
Prep-HPLC7
InternalShimadzu IR 460IR6
InternalVarian – 400 MHzNMR5
InternalCostechElemental Analysis (CHN)4
InternalWaters HPLC (Alliance, 600 Series) and Aquity UPLC with PDA and ELSD detectors
HPLC3
InternalWaters: Quattro-II with Alliance LC with PDA Detector, TQD with Aquity UPLC systems with PDA detector
LC-MS/MS Systems2
InternalWaters:ZQ with Alliance LC , SQD with Aquity UPLC systems with PDA detectors
LC-MS Systems1
internal / external
DetailsInstrumentation
Analytical Equipment:
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
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
Case Studies: Med Chem Programs
Antibacterial:
•β-Lactamase Inhibitor - Tazobactam
•4-year SAR Program
•Design, Synthesis, Screening
Hit Lead Pre-Candidate Candidate Market
Case Studies: Med Chem Programs
NSAID:
•COX-1 Inhibitor – Mofezolac (Disopain™)
•Design, Synthesis
Hit Lead Pre-Candidate Candidate Market
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
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
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
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
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
NAEJA FTE’s Director100% PhD’s
Project
Coordinator100% PhD’s
Scientist90% PhD’s
Canada
US
Europe
Asia
Japan
PhD’s & postdocs by location
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
Contact Information
Mr. Christopher G. MicetichPresident and [email protected]
Dr. Sameeh M. SalamaSenior Director, Business [email protected]
NAEJA Pharmaceutical Inc.4290-91A Street, Edmonton, Alberta, Canada. T6E 5V2
Tel: (780) 462-4044; Fax: (780) 461-0196
www.naeja.com
