3-Indolyl sultams as selective CRTh2 antagonists

Novel CRTH2 antagonists: a review of patents from 2006 to 2009

“…A recent paper describes that the sultam compounds (39 --40, Figure 6) were discovered by inspiration from ramatroban and TM30089 (9, 10; Figure 1) and that the compounds have low or no activity on the DP 1 and TP receptors [74]. Athersys has also patented a series of benzimidazoles (e.g., 41 --44, Figure 7) which, although the compounds are not indoles and the substitution pattern is different, have an overall structural resemblance to ramatroban and TM30089 [75].…”

The Role of Sulphonamides and N‐Sulphonyl Ketimines/Aldimines as Directing Groups in the Field of C−H Activation

“…There are many documented synthetic reactions for the synthesis of this class of compounds but C−H activation approach has garnered attention of researchers due to its practicality, environmental sustainability and atom economy (Figure 2). [57–60] …”

CH-Diazomethane Sulfonamides Generated in Situ for Intramolecular [3+2] Cycloaddition of Alkynes: An Entry into Novel Pyrazole-Fused Five-Membered Sultams

“…Being essentially bioisosteres of privileged isoindolinones, 1 (hetero)arene-fused five-membered sultams 1 are important scaffolds in drug discovery. 2 This notion is supported by such examples as prostaglandin D2 receptor (CRTh2) antagonist 2 for the treatment of asthma, 3 antibacterial compound 3, 4 DNAcleaving agent 4, 5 M4 muscarinic acetylcholine receptor modulator 5, 6 aggrecanase inhibitor 6 for the treatment of arthritis, 7 PI3K kinase inhibitor 7 8 and cathepsin inhibitor 8 for the treatment of various diseases, e. g., rheumatoid arthritis ( Figure 1). 9 In light of the prominence of this general chemotype (1) in drug discovery, it comes as a surprise that no versions of it containing an azole (i. e. a nitrogen-containing five-membered aromatic) heterocycle as the fused heteroaromatic moiety have been reported.…”