RE: Inflammatory Bowel disease treatment18 Sep 2024 11:12
Anyone got enough knowledge to know if this is related to our design?
Compound design and synthesis
Compound 18 was first designed and synthesized by our group. The precise synthetic route was followed a previously published reference [21]. 8-(5-Methyl-2-((1-methyl-1H-pyrazol-4-yl)amino)pyrimidin-4-yl)-2,8-diazaspiro[4.5] decan-1-one (18). To a flask containing the general intermediate (1.0 equiv), 1-methyl-1H-pyrazol-4-amine (1.2 equiv), n-butanol (10 equiv), and concentrated hydrochloric acid (1% equiv) were added with stirring at 100 °C for 10–12 h.
However close the two compounds are, this is very positive.
Conclusion
Overall, we identified a selective JAK1 and TYK2 dual inhibitor, 18, and confirmed its therapeutic effect in two different of IBD mouse models. Concurrently, 18 exhibited suitable oral bioavailability and low toxicity for long-term use. Based on all of these results, 18 is a meaningful lead compound for further studies of IMIDs.