FoRx Therapeutics AG

In 2013, the first review article recommending the introduction of the sulfoximine group to the medicinal chemist's toolbox was published.Sulfoximines, the mono-aza analogs of sulfones, by then had received little interest in drug discovery, despite their very interesting properties.However, interest in sulfoximines has increased substantially in recent years, which is exemplified by an ever-increasing number of scientific articles and life science patent applications, as well as com. available sulfoximine building blocks.Moreover, the selection of novel sulfoximine clin. candidates (e.g.VIP152, AZD6738, IM-250) serves to highlight the increased acceptance of this formerly neglected functional group by the drug discovery community.This presentation highlights emerging trends and opportunities for drug designers for the utilization of the versatile sulfoximine group in medicinal chem., such as in the construction of complex mols., proteolysis targeting chimeras (PROTACs), antibody-drug conjugates (ADCs), cyclic peptides and novel warheads for covalent inhibition.

A review.Extension of the medicinal chem. toolbox is in the vital interest of drug designers who are confronted with the task of finding mol. solutions for an ever-increasing biol. target space.However, the diffusion of an innovation can be a lengthy process even within the drug discovery community which faces enormous pressure to formulate effective solutions for patients in a timely manner.Along these lines, it took almost 70 years before the use of the sulfoximine group reached a critical mass in medicinal chem.Even though interest in this versatile functional group has increased exponentially in recent years, there is ample room for further innovative applications.This minireview highlights emerging trends and opportunities for drug designers for the utilization of the sulfoximine group in medicinal chem., such as in the construction of complex mols., proteolysis targeting chimeras (PROTACs), antibody-drug conjugates (ADCs) and novel warheads for covalent inhibition.