Patent Evaluation: Lipid-A analogues as inhibitors of lipopolysaccharide-induced TNF production

Summary

Novelty: Analogues of lipid A useful as anti-endotoxic drugs for the treatment of septic shock and lipopolysaccharide (LPS)-mediated activation of viral infection (HIV, herpes or influenza) are disclosed.

Biology: The compounds were assayed for their ability to inhibit LPS-induced production of tumour necrosis factor and IL-1β both in vitro and in vivo. One compound effectively inhibited TNF production in mice with an ED₅₀ value of 5.4μg/mouse.

Chemistry: The synthesis of the compounds are described in three examples including that of analogue B318.