TLR agonists

摘要

The present invention provides for TLR agonist conjugates (compounds) and compositions, as well as methods of using them. The compounds of the invention are broad-spectrum, long-lasting, and non-toxic combination of synthetic immunostimulatory agents, which are useful for activating the immune system of a mammal, preferably a human and can help direct the pharmacophore to the receptor within the endosomes of target cells and enhance the signal transduction induced by the pharmacophore.

主权项

1. A compound having formula (IA) and R3: wherein X1 is —O; R1 is (C1-C10)alkyl or substituted (C1-C10)alkyl, wherein the substituents are hydroxy, C1-6alkyl, hydroxyC1-6alkylene, or C1-6alkoxy; wherein n=4 and each R2 is —H; X2 is a bond or a linking group having up to about 24 atoms; wherein the atoms in the chain of the linking group are selected from the group consisting of carbon, nitrogen, sulfur, non-peroxide oxygen, and phosphorous; and R3 is a protein that directs formula (IA) to receptors within endosomes of target cells; or a pharmaceutically acceptable salt of the compound, wherein the ratio of the compound having formula (IA) to R3 is 5:1.