Spirocyclic Piperidines in Drug Discovery Spirocyclic scaffolds in general, spirocyclic piperidines in particular, have several advantages over sp2-carbon rich, flat structures. Their 3-D trajectory offers more points of contact with the protein target of interest and can give rise to more potent and selective drugs. The sp3-carbon rich molecules are also blessed with superior physiochemical properties such as higher aqueous solubility. Finally, unexplored new spirocyclic architectures can create novel intellectual property spaces. The success of Novartis’ allosteric SHP2 inhibitors underscores the utility of spirocyclic scaffolds. Their applications in medicinal chemistry are destined to grow rapidly, especially since many of them are now commercially available.
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