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Bioisosteres

Bioisosteres are chemical tools used by medicinal chemists to modify and optimize the properties of drug candidates. But beyond the fast-track optimization of properties, bioisosteric switches are also used to create novel IP space and differentiate from competitors.

Why Bioisosteres?

Bioisosteres are chemical tools used by medicinal chemists to modulate and optimize the properties of drug candidates. But beyond the obvious advantages of fast-track optimization of properties inherent to bioisosterism, bioisosteric switches are also used to explore chemical space, expand chemical diversity and generate novel IP space. Bioisosteres are therefore used extensively in drug discovery and in particular lead optimization. The concept of bioisosterism in drug discovery is becoming of prime importance due to the recent advances in the field. Most routinely used fragments in medicinal chemistry have been studied and novel bioisosteric replacement solutions are now available.

Why SpiroChem?

At SpiroChem, we have a comprehensive understanding of the concept of bioisosteric switches. Our catalog of products contains examples of most of the bioisosteric concepts currently known and used in medicinal chemistry programs and we are always monitoring the literature to identify new opportunities. We also have in-house R&D program aiming at identifying and validating new bioisosteric switch concepts. Our portfolio of building blocks encompasses the recently-developed oxetanes, azetidines and other small rings, but also the corresponding spirocycles, bicycles, cubanes and other carbocyclic rigid scaffolds. Our products can be used both for scaffold-hopping of central fragments (bicyclo[x.y.z]alkanes, cubanes, spirocycles etc.), for the modification of key functionalities (amide -> oxetanylamine switch, etc.) or for modulation of peripheral groups (oxetanes, SF5, bicyclo[1.1.1]pentanes, cubanes, etc.)

SpiroChem has years of experience with the chemistry of oxetanes and spirocycles, and we are also the world leader in the design, synthesis and manufacture of bicyclo[1.1.1]pentanes. SpiroChem has also a comprehensive range of cubanes and has developed new chemical techniques and cost-efficient synthetic routes that allow for their diversification and production on large scale.

In conclusion, SpiroChem has the most diverse range of building blocks for bioisosteric switch and we can also design synthetic routes to new series that are fit for your applications and that will facilitate their introduction in your molecules of interest. Do not hesitate contacting us if you need information or if you need our help. We believe there is a solution to every problem, and we will do everything we can to find it for you! Stay tuned, we have more to come in the coming months!

Get Inspired with our Building Blocks to Create the Drugs of Tomorrow.