Heterocyclic derivatives, pharmaceutical compositions and their use in the treatment, amelioration or prevention of cancer

Posted on 28 June 2021

Earlier this year, our client TOLREMO therapeutics nominated the clinical candidate for a chemical series that was developed together with Symeres. In this article, we spoke with Yorik Bruseker, one of our chemists, who has been involved in the project since it started at Symeres.

Can you introduce yourself? What is your role within Symeres?

I’m Yorik Bruseker and I’ve been working at Symeres in the Netherlands for 12 years. I started as a Research Chemist in the Discovery Chemistry Department and later transferred to the Medicinal Chemistry Department, where I am currently a Senior Scientist on the TOLREMO project.

What is the project about?

TOLREMO’s goal is to identify novel drug-resistance regulators and to develop small molecules that modulate them. This project started as a phenotypic screening (no target known) and progressed into a target-focused MedChem project, from hit finding through to lead optimization and beyond.

What is the team like?

The team consisted of a core team of 4 to 5 chemists, working closely with our computational chemists, the ADME and analytical departments, and the team at TOLREMO. It has been a real team effort with input from everyone.

What was the role of Symeres within the project?

Symeres’ role was the design and synthesis of small molecules, based on the pharmacology and ADME data, and the generation of that ADME data. Additionally, we supported TOLREMO with database management and provided biobased CROs with the requested compounds.

What challenges did you and your team have to overcome?

Some of the asymmetric synthesis was not straightforward at first and required continuing effort to ensure the delivery of final compounds. We also dedicated time to ensure that the various PK and PD models (performed in various labs around the world) received our compounds on time to generate the data the project needed.  

What achievement are you proud of?

We took this early-stage, phenotypic MedChem approach and transformed it into an increasingly advanced target-driven project. The results were some extremely promising compounds and a clinical candidate that will hopefully advance to the clinic. I really enjoyed how we built a great, multidisciplinary team between TOLREMO and Symeres, and we learned a lot along the way.

Recently published patents around this nomination are WO 2020/127200 A1 and WO 2021/064142 A1.

Feel free to contact us!

Curious to know more about what can we do for you? Get in touch and let’s start a conversation.

Contact us