Fast Follower

The client in this program was a small biotech with minimal internal chemistry and a long standing contract with a biology CRO.

The Target:

This client works in a specialised therapeutic area. SYNthesis were initially approached with a kinase target.

The Chemistry:

For the initial kinase target the client had IP around a scaffold which they were keen to explore further. SYNthesis provided 3 chemists to help exemplify the compounds within the IP claimed. The chemistry as expected for a kinase program was largely heterocyclic aromatic chemistry.

Compound Design:

Literature analysis and identification of a chemical start point were conducted as a collaborative effort between SYNthesis and the client. Subsequent SAR data were shared and SYNthesis has continued to contribute to the medicinal chemistry design with solubility and metabolic profile being two key requirements for potential clinical candidates.

The Chemistry:

The GPCR program initially used a team of 3 chemists, but was expanded on the basis of the results obtained to a team of 7 chemists. Compounds within the program are complex aromatics necessitating multistep (>8) syntheses. SYNthesis has provided final compounds in 100mg quantities at over 95% purity. SYNthesis have also provided larger quantities of key compounds for additional in vitro and in-vivo testing.

Key achievements:

The fast-follower project was licensed to a big pharma after the preclinical drug candidate was obtained after 18 months collaboration
A clinical candidate was identified in the GPCR program within 12 months from the start date.
Three novel series of compounds have been identified and explored within the GPCR program each containing potent molecules (sub nanomolar) with high selectivity (>1000).
SYNthesis scientists are named as inventors on the client’s patent.
At the conclusion of that project the client elected to continue with SYNthesis and pursue a GPCR program.