On March 17, 2022, Yang, Shengyong; Li, Linli published a patent.Electric Literature of 1187582-58-6 The title of the patent was Preparation of 5-substituted indole-3-amide derivatives for disease treatments targeting RIPK1. And the patent contained the following:
Provided are a 5-substituted indole 3-amide derivative, a preparation method and a use thereof, belonging to the field of medicine. A compound represented by formula I [wherein X1 and X3 = independently N or (un)substituted CH; X2 = (un)substituted NH or CH=CH; R2B = -R2-B; R2 = (un)substituted alkylene,; B = (un)substituted aryl, cycloalkyl, heteroaryl, etc.; R3 = H or (un)substituted alkyl; R4 and R5 = independently H, alkyl, CN, OH, CO2H, etc.; A = (un)substituted aryl or heteroaryl] or a pharmaceutically acceptable salt thereof is provided. For example, II was prepared in a multi-step synthesis. This type of compound can significantly inhibit the activity of RIPK1 kinase, has high selectivity and excellent safety, serves as a RIPK1 kinase inhibitor, and can be used as a potential therapeutic drug for inflammation, immune diseases, tumors and neurodegenerative diseases. TNFα-induced SIRS model experiments proved that the compound can inhibit a RIPK1 kinase in vivo. Pharmacokinetic results showed that this series of compounds has excellent pharmacokinetic properties, thus providing a novel strategy and means for disease treatments targeting RIPK1. The experimental process involved the reaction of 5-Bromo-1-(tetrahydro-2H-pyran-2-yl)-1H-pyrazole(cas: 1187582-58-6).Electric Literature of 1187582-58-6
The Article related to preparation indole amide disease treatment ripk1 human, inflammation immune tumor neurodegenerative disease, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Electric Literature of 1187582-58-6
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics