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Relevant academic research and scientific papers

Conjugated TLR7 and/or TLR8 and TLR2 polycationic agonists

The present invention relates to a conjugated compound of Formula I : Q-Z-R4 wherein Q is a TLR7 and/or TLR8 agonist and Z-R4 is a TLR2 agonist, said conjugated compound being chosen among compounds of Formula II :

Conjugated TLR7 and/or TLR8 and TLR2 polycationic agonists

A conjugated compound of Formula I: Q-Z—R4 wherein Q is a TLR7 and/or TLR8 agonist and Z—R4 is a TLR2 agonist, the conjugated compound being chosen among compounds of Formula II:

CONJUGATED TLR7 AND/OR TLR8 AND TLR2 AGONISTS

A conjugated compound of formula Q-Z—R4 wherein Q is a TLR7 and/or TLR8 agonist and Z—R4 is a TLR2 agonist, and the uses thereof in the treatment of infection, cancer or immune disorders or for use in vaccines.

Novel compositions of TLR7 and/or TLR8 agonists conjugated to lipids

The present invention concerns a conjugated compound of formula Q-Z-R4 wherein Q is a TLR7 and/or TLR8 agonist and Z-R4 is a lipid covalently linked to an amino acid or peptide coupled to a polyamine group, and a process for the manufacture of said conjugated compound, as well as a complex formed between said conjugated compound and a polyanionic molecule and a pharmaceutical composition containing said conjugated compound or complex. The invention further concerns the use of said conjugated compound or complex in the treatment of infection, cancer or immune disorders or for use in vaccines.

Synthesis and biological evaluation of novel 9-substituted-8-hydroxyadenine derivatives as potent interferon inducers

Recently we reported the adenine derivatives 3a-d as novel interferon (IFN) inducers. In the present study, we conducted a detailed structure-activity relationship study of analogues of 3a-d with respect to their IFN-inducing activity, mainly focusing on the N(9)-position of the adenine. From this study, we found that introduction of the 3-pyridylmethyl moiety was effective to increase in vitro activity, and compound 9ae was identified as being the most potent IFN inducer. This compound gave a minimum effective concentration (MEC) of 3 nM, which is comparable with that of R-848, a second generation IFN inducer. Compound 9ae also demonstrated potent IFN-inducing activity at a dose of 0.1 mg/kg by oral administration in mice. Furthermore, compound 9ae induced IFN in monkeys in a dose dependent manner, with a potency superior to that of R-848. In addition, 9ae did not cause emesis in ferrets even at a dose of 30 mg/kg. In this study the maximum plasma concentration of 9ae was 1019 ng/mL (ca. 3.1 μM), which was approximately 1000-fold higher than the MEC value. Therefore, with respect to both the efficacy and the safety margin, compound 9ae (SM-276001) is considered to be a promising compound as an orally active IFN inducer.