Saccharide conjugates

摘要

The invention provides a series of novel Lipid A analogs that are structually simple, synthetically accessible, and capable of blocking the cellular receptor within the signal transduction pathway. The novel Lipid A analogs can include a monosaccharide core with hydrophobic side chains and amino acid ionic motif. The invention further provides methods of using the compounds and compositions thereof in various therapeutic methods.

主权项

1. A compound of Formula I: wherein
R1 is (C1-C6)alkyl;R2 and R3 are each independently (C8-C24)alkyl; (C8-C24)alkenyl; or (C8-C24)alkanoyl;R4 is H, (C1-C6)alkyl, or aryl;n is 0-9;X is O, S, or N;Rx is an oxygen-linked, sulfur-linked, or nitrogen-linked amino acid that is optionally protected on oxygen or nitrogen with an oxygen or nitrogen protecting group;wherein any alkyl, alkenyl, alkanoyl or aryl is optionally substituted with one or more hydroxy, oxo, alkyl, alkoxy, alkylcarbonyl, alkylcarbonyloxy, nitro, halo, trifluoromethyl, trifluoromethoxy, cyano, or amino groups;or a pharmaceutically acceptable salt or solvate thereof.