| 摘要 |
The present disclosure provides novel imidazoquinoline derived compounds, derivatives thereof, analogues thereof, and pharmaceutically acceptable salts thereof, and methods of making and using such compounds. The present disclosure also provides TLR7 agonists and TLR7/TLR8 dual agonists, probes, tissue-specific molecules, adjuvants, immunogenic compositions, therapeutic compositions, and self-adjuvanting vaccines including the imidazoquinoline derived compounds, derivatives thereof, analogues thereof, and pharmaceutically acceptable salts thereof. Derivatives of the imidazoquinoline derived compounds also include dendrimers and dimers of the imidazoquinoline derived compounds, and methods of making and using the dendrimeic and dimeric imidazoquinoline derived compounds. The present disclosure also provides dual TLR2/TLR7 hybrid agonists that include imidazoquinoline derived compounds of the present disclosure. |
| 主权项 |
1. An imidazoquinoline derived compound of Formula I, a derivative thereof, or analogue thereof, or pharmaceutically acceptable salt thereof, wherein
Formula I has the structure: wherein, R is selected from the group consisting of: —NH(R5) and isothiocyanate;
R5 is selected from the group consisting of hydrogen, acetyl, —CO-tert-Bu (-Boc), —CO—(CH2)x—R6, C1-C16 alkyl, —CO-4-(phenylboronic acid), —C(S)—NH—(CH2)x—NH—(CH2)x—NH—(CH2)x—NH2, a reporter moiety, a tissue-specific moiety, a peptide antigen moiety, a protein antigen moiety, a polysaccharide antigen moiety, and a TLR2 agonist moiety;R6 is selected from the group consisting of hydrogen, alkyne, azido, carboxylic acid, and —CONH—(CH2)x—O—(CH2)x—O—(CH2)x—O—(CH2)x—R7;R7 is selected from the group consisting of amino, isothiocyanate, and —NH—CO—(CH2)x—CO2H;R8 is selected from a peptide antigen moiety or a protein antigen moiety; andx is any integer from 1 to 10. |
