The client in this program is a small biotech with a limited internal chemistry capacity. They have taken an IP position across a privileged structure that can be used as an isostere in a number of marketed API’s.
This program was conducted across multiple targets working from finished API to install the isostere.
This client approached us with a looming patent publication and a need to exemplify the use of the privileged structure across a number of API classes. They were keen to have rapid deployment of resource to the project and subsequent to publication a rapid downgrade of numbers.
A route to install the privileged group on the completed API was provided by the client, however given the varied chemistries of the API’s such route was not always applicable to the synthesis of a given compound. In some cases partial syntheses of the compounds had to be pursued to allow synthesis of the final target.
SYNthesis synthesized compounds in 5+ mg amounts at greater than 97% purity. The patent experimental for each compound was written as it was submitted. SYNthesis also managed shipping of the finished compounds to multiple biology CRO’s in international locales.
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.
Medicinal chemistry input in the patent exemplification program was limited. The applicability of the isostere was modeled using Cresset software and synthesis of the analogue priotised on this basis. SYNthesis was responsible for all synthetic design. Where a different analogue was more easily obtained, SYN|the
- SYNthesis managed an increase from an initial team of 10 chemists to a team of 20 chemists within two months.
- This team worked for 6 months until publication of the patent.
- After seeing how we worked, the client elected to continue working with SYNthesis to conduct a number of concurrent research programs across multiple targets and currently employ a 10 chemist team within SYNthesis.
Number of Chemists
Average number of steps per compound
Average productivity (final compounds per fortnight
Length of Contract
1 year – ongoing