Researchers at Academia Sinica, CSIC (Consejo Superior de Investigaciones Cientificas) and Universidad de Sevilla have divulged 5-aminohexahydro-6,7,8-trihydroxy-3h-oxazolo[3,4-a]pyridin-3-one derivatives acting as Toll-like receptor 4 (TLR4; CD284) antagonists or TLR4 agonists reported to be useful for the treatment of autoimmune disease, metabolic syndrome, asthma, inflammatory bowel disease, allergic rhinitis, nonalcoholic steatohepatitis, atherosclerosis and infections, among others, and also as vaccine adjuvants.