The use of oxetanes in drug discovery has known an exponential growth in the last 10 years. They proved to be useful fragments in drug discovery as demonstrated by the group of Prof. Erick Carreira at ETH Zürich and researchers at Roche, Basel. In particular, they were shown to be bioisosteres of gem-dimethyl groups and carbonyl groups. Oxetanylamines can be seen and used as bioisosteres of amide fragments.
The use of oxetanes in drug discovery has known an exponential growth in the last 10 years and they have now become part of the standard toolbox of medicinal chemists. They proved to be useful fragments in drug discovery as demonstrated by the group of Prof. Erick Carreira at ETH Zürich and researchers at Roche, Basel.1 In particular, they were shown to be suitable bioisosteres for gem-dimethyl groups and carbonyl groups in a number of case studies. The corresponding oxetanylamines can also be seen and used as bioisosteres of amide fragments. The beneficial properties of oxetanes in medicinal chemistry allow for modulation and improvement of physicochemical and pharmacokinetic properties. This ability to quickly improve ADME properties can lead to accelerated lead optimization programs.
Another advantage of these structures is that their introduction into your molecules of interest usually comes with novel chemical space and therefore new intellectual property.
SpiroChem has years of experience with the chemistry of oxetanes. SpiroChem is not only a spin-off of ETH-Zürich and of the Carreira group: we have internal R&D programs and collaborations with key academic groups and life science companies worldwide to increase our knowledge in the field of medicinal chemistry and make sure that we are always on top of the recent developments in drug discovery. In a number of cases, we have been trendsetters and we are always at the forefront of chemical innovation, especially in the field of bioisosteres. These years of experience and our understanding of what really matters to the medicinal chemistry community has helped us design a comprehensive catalog of advanced building blocks containing oxetanes. The chemical diversity of our portfolio of oxetane derivatives should allow their introduction in most medicinal chemistry programs, and we are here to support you and help you if you need advice.
Our involvement in the field of oxetane chemistry since its origin also allows us to design synthetic routes to new series that are fit for your applications and that will facilitate introduction of oxetanes in your molecules of interest. Do not hesitate contacting us if you have specific needs and we will provide tailor-made solutions!
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