Case Studies







The CreaGen Leadership Team is composed of industry-recognized medicinal chemists and a highly experienced scientific advisory board with a demonstrated track record across big-pharma and biotech R&D organizations.  This critical mass enables us to offer a comprehensive med chem portfolio management service and partnership capability.  These alliances are designed for flexibility to best meet the clients’ needs and are individually customized with full confidentiality and IP-protection to suit your specific project for an optimal outcome.

Our expertise in drug discovery encompasses numerous drug-target classes and disease areas including:

  • Kinases / Phosphatases / Proteases
  • GPCRs
  • Ion Channels
  • Nuclear Hormone Receptors
  • Peptides / Peptidomimetics
  • Neuropeptides
  • Metabolic syndrome, specifically Type II diabetes
  • Anti-infectives
  • Anti-inflammatory
  • CNS, neurodegeneration
  • Oncology

Current programs encompass these important target classes that represent 70% of the drugs currently on the market.

  • CS-1) Multinational Pharmaceuticals (Oncology target):
  • CS-2) Multinational Biotech (Oncology; Antibody Drug Conjugates (ADC):
  • CS-3) Biotech Start-up (Anti-infectives):
  • CS-4) Biotech Start-up (Type II Diabetes):
  • CS-5) Biotech (Anti-infective):
  • CS-6) Multinational Biotech (Oncology):
  • CS-7) Academic Institute (Antiviral Program):
CS-1) Multinational Pharmaceuticals (Oncology target):

This was a four FTE multi-year contract. Small Molecule Kinase program.

Project requirements:

  • Optimize the leads based on screening results, synthesize novel analogs of the leads for weekly screening
  • Provide all medicinal chemistry expertise to client in designing new analogs and libraries. Explore new synthetic routes.

Accomplishments:

  • Successfully met all the milestones and deadlines
  • Provided more than 2000 compounds and many novel scaffolds during the tenure of the program.
  • CreaGen was a true extension of customers medicinal chemistry program.
CS-2) Multinational Biotech (Oncology; Antibody Drug Conjugates (ADC):

Multi-year FTE based program that involved synthesizing, linkers, small molecules and ADC conjugates.

Project requirements:

  • Design and synthesize novel linkers.
  • Conjugate novel small molecules and drug candidates to linkers.
  • Introduce reactive functionalities on the linker to conjugate to antibodies.
  • Provide conjugation chemistry expertise to client.
  • Synthesize libraries of small molecules and explore new synthetic routes.

Accomplishments:

  • Provided several conjugates to client for screening.
  • Developed several novel hydrophilic molecules to conjugate to antibodies to minimize aggregation.
  • Multi year renewal of collaborations
  • True extension of customer’s ADC program
CS-3) Biotech Start-up (Anti-infectives):

This was a five-year FTE based Lead Optimization program for a small biotech companies based in Massachusetts:

Project requirements:

  • Function as medicinal chemistry department for client
  • Provide all medicinal chemistry expertise in designing and synthesizing new analogs
  • Synthesize analogs for weekly screening
  • Develop SAR and interpret weekly screening results with client and suggest new ideas

Accomplishments:

  • Met all the milestones during the contract work
  • Expanded collaboration to 8 FTEs: Client was subsequently acquired by European pharmaceuticals.
CS-4) Biotech Start-up (Type II Diabetes):

This was a four year FTE based Lead generation and Lead optimization contract.

Project requirements:
• Functioned as de facto medicinal chemistry department
• Provided Integrated drug discovery services to the start-up
• Provided all medicinal chemistry expertise starting with design discussion, literature searches, hit-to-lead evaluation, SAR studies, lead optimization, identification and selection of high-value preclinical candidates

Accomplishments:
• Provided a nanomolar compound and several backup compounds.Expanded to 6 FTEs
• Project grew as milestones have been delivered. Program was subsequently licensed to another organization.

CS-5) Biotech (Anti-infective):

Biotech company focused on anti-infectives. Multi-year FTE based collaborations that involved Scaffold and lead molecule synthesis

Project Requirements:
• Design and synthesize novel scaffolds and develop new and efficient routes for the synthesis
• Provide multi-gram quantities of final compounds for in vivo tox studies with aggressive timeline
• Perform process development for multi-step synthesis of scaffolds and lead molecules

Accomplishments:
• Five year collaborations: Provided 150 scaffolds and multiple libraries of 2000 compounds were delivered.
• Several multigram scale non GMP compounds were synthesized for in-vivo and tox studies

CS-6) Multinational Biotech (Oncology):

Macrocyclic compounds Lead generation and Lead Optimization

Project Requirements:

  • Design and Synthesis of 300-member focused macrocyclic compound library
  • Sample delivery: dry form in duplicate bar-coded vials
  • Quantity: 10 to 50 mg with purity >95+%: 1H NMR and LCMS for all products in FID format

Accomplishments:

  • Synthesized and delivered large compound library in client specified format on time
  • Expansion and extension of the project
CS-7) Academic Institute (Antiviral Program):

Lead optimization and Conjugation chemistry:

Project Requirements:

  • Design and Synthesis of modified Tenofovir nucleosides with suitable site for linker
  • Synthesis of FIAC, FMAU, FIAU, FAC, FAU, and FHMAU analogues with linkers
  • Provide synthetic strategies for SBIR proposals

Accomplishments:

  • Synthesized more 50 nucleoside analogs
  • Synthesized sugar modified nucleosides
  • Performed stability and rate-of-cleavage studies
  • Expansion and extension of the project

For more information:

Please contact our R & D Coordinator for more information.




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© CreaGen Inc 2019. All rights reserved. Designed by Inqude



© CreaGen Inc 2019. All rights reserved. Designed by Inqude