61565-36-4Relevant academic research and scientific papers
Discovery of Chromane-6-Sulfonamide Derivative as a Potent, Selective, and Orally Available Novel Retinoic Acid Receptor-Related Orphan Receptor γt Inverse Agonist
Chen, Lei,Su, Mei,Jin, Qiu,Wang, Wei,Wang, Chun-Gu,Assani, Israa,Wang, Mu-Xuan,Zhao, Shi-Feng,Lv, Shen-Min,Wang, Jia-Wei,Sun, Bo,Li, Yan,Liao, Zhi-Xin
, p. 16106 - 16131 (2021/11/18)
Interleukin-17 (IL-17) is a proinflammatory cytokine that plays a dominant role in inflammation, autoimmunity, and host defense. RORγt is a key transcription factor mediating T helper 17 (Th17) cell differentiation and IL-17 production, which is able to activate CD8+ T cells and elicit antitumor efficacy. A series of sulfonamide derivatives as novel RORγt inverse agonists were designed and synthesized. Using GSK2981278 (phase II) as a starting point, we engineered structural modifications that significantly improved the activity and pharmacokinetic profile. In animal studies, oral administration of compound d3 showed a robust and dose-dependent inhibition of the IL-17A cytokine expression in a mouse imiquimod-induced skin inflammation model. Docking analysis of the binding mode revealed that the compound d3 occupied the active pocket suitably. Thus, compound d3 was selected as a clinical compound for the treatment of Th17-driven autoimmune diseases.
INDANYL COMPOUNDS AS VOLTAGE GATED SODIUM CHANNEL MODULATORS
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Page/Page column 54-55, (2018/09/28)
The invention relates to indanyl compounds, their pharmaceutically acceptable salts thereof, processes for their preparation and pharmaceutical compositions comprising the same for the treatment, management and /or lessening severity of diseases, disorders, syndromes or conditions which are associated with the voltage-gated sodium channels (VGSC). More specifically the present invention provides compounds having the structure of Formula (I).
Synthesis of N-(1-Keto) and N-(1-Hydroxy-5-indansulfonyl)-N'-(4-chlorophenyl)urea, Two Major Metabolites of the Antitumor Agent Sulofenur (LY 186641)
Howbert, J. Jeffry,Crowell, Thomas A.
, p. 3193 - 3200 (2007/10/02)
A brief (3-4 step), large-scale synthesis of two major metabolites of the antitumor agent sulofenur was developed.The required intermediate, 1-keto-5-indansulfonamide, was prepared in only two steps, utilizing a novel method for converting an aromatic chl
