October 26^th, 2020

The Journal of Medicinal Chemistry has recently reported the results obtained in our Lead Optimisation collaboration with Esteve Pharmaceuticals, aimed at the identification of novel dual ligands of the sigma-1 receptor (σ1R) and the μ-opioid receptor (MOR), as part of Esteve’s R&D activities to develop new, potent and safer analgesics.
The chemistry work was developed by Enantia’s Medicinal Chemistry team, led by Dr. Marina Virgili, in collaboration with Esteve Pharmaceuticals. Previous investigations carried out at Enantia established a suitable Lead, comprised of a spirocyclic morpholino-piperidine core identified using rational drug design strategies. Subsequent Lead Optimization has led to the discovery of EST73502, a clinical candidate undergoing Phase I clinical trials. The compound showed promising results in animal models with potent analgesic efficacy and improved safety compared to oxycodone.

Enantia offers a wide portfolio of drug discovery services for pharmaceutical and biotech companies, including the design and synthesis of new scaffolds and libraries of small molecules with potential biological activity, covering Hit finding, Hit-to-Lead and Lead Optimization programs. Additionally, Enantia can collaborate with Structure-Activity Relationship (SAR) and Drug Metabolism and Pharmacokinetics (DMPK) data analysis. Enantia has a long track record of collaborative research projects with the pharmaceutical industry, leading to more than 20 patent applications related to medicinal chemistry.
Besides the most common MedChem activities, Enantia can also contribute to the early stages of the drug development by preparing cold labelled compounds and metabolites of the candidates. Additionally, for later phases of development, our Solid State department counts with extensive expertise in identifying the best solid form of the candidate to be further developed.

You can read the full paper here.

Within this collaboration, a new robust and scalable synthetic route to obtain calcium acamprosate has been developed. The selective precipitation of calcium acamprosate as an easily filterable solid with 74–77% yield was achieved by the one-pot nucleophilic opening of 1,3-propanesultone with potassium acetamide, following by cation exchange with calcium ion at controlled pH.

In comparison with other procedures described in the literature and used previously, the newly developed and optimized methodology gives rise to a remarkably more efficient and direct synthesis of calcium acamprosate, avoiding the use of toxic chemicals and multistep synthesis.

This is a perfect example of how our process chemistry team can support our customers in designing and optimizing new routes of synthesis, leading to procedures that can be easily scaled up and used later at industrial scale. Furthermore, this type of projects can be complemented at Enantia by performing the carry-over of the impurities, and the characterization thereof.

You can read the full paper here.

Our CEO Dr. Joan Feixas will be attending the Future Cannabis Strategies Europe 2020, taking place in Royal Lancaster London on the 29^th and 30^th of January, 2020.

During the event, we will be discussing with key partners and customers about our Cannabinoids Cocrystal Platform, which enables the manufacturing of a wide range of cannabinoids, both from natural and synthetic origin.

As part of this platform, Enantia is already developing commercial batches of API grade cGMP Cannabidiol (CBD), along with minor cannabinoids such as Cannabidivarin (CBDV), Cannabigerol (CBG), Cannabichromene (CBC) and Cannabinol (CBN).

If you are interested in our very high-quality cannabinoids, or if you are looking for a cost-effective purification technology for your cannabis extracts, do not hesitate to contact us to organize a meeting.

The Journal of Medicinal Chemistry has recently published some of the results obtained in our Medicinal Chemistry collaboration with Esteve Pharmaceuticals, aimed at the identification of novel dual ligands of the sigma-1 receptor (σ1R) and the μ-opioid receptor (MOR), as part of Esteve’s RD activity to develop new, potent and safer analgesics.

The chemistry work, which was carried out by Enantia’s Medicinal Chemistry team led by Dr. Marina Virgili, started with the design of the spirocyclic morpholino-piperidine core using rational drug design strategies. The efficient synthetic approach developed, allowed then for the rapid preparation of analogues with diversification in several positions of the scaffold, rendering the promising Lead described in this paper. The subsequent Lead Optimization program led to the discovery of a clinical candidate, whose identification will be reported soon.

Enantia has a long track record in Medicinal Chemistry services to the pharmaceutical industry, with more than 20 patents related to this activity, which includes the design and synthesis of new scaffolds and libraries of small molecules with potential biological activity.

In addition to conventional MedChem activities such as Hit-to-Lead and Lead Optimization programs, Structure-Activity Relationship (SAR) and Drug Metabolism and Pharmacokinetics (DMPK) interpretation, Enantia can also collaborate in the early stages of the drug development process by preparing cold labelled compounds and metabolites of a given candidate, as well as by identifying its best solid form in our Solid State department.

You can read the full paper here.

December 13th, 2019

November 19th, 2019

Enantia attended the 30th edition of the CPhI Worldwide 2019 event that took place in Frankfurt (Germany) from the 5th to the 7th of November.

Thanks to everyone for the interesting meetings.

We had the chance to discuss not only our services in chemical discovery and development, but also our cannabinoids cocrystal platform and the minor cannabinoids that we offer (CBDV, CBG, CBC, CBN).

We hope to meet you all very soon.

March 26th, 2019

We are pleased to share this article from Chemistry World about Enantia’s cocrystalisation technology.

Enantia has developed new cannabidiol (CBD) cocrystals that allow CBD purification from complex mixtures, either natural or synthetic.

You can read the article here.

March 6th, 2019

Enantia has again succeeded in applying cocrystallisation technology to a new family of compounds, the cannabinoids.

December 17th, 2018

We would like to wish all our customers, collaborators and friends, happy holidays and the best wishes for 2019!