[EN] DIPROVOCIMS: A NEW AND POTENT CLASS OF TLR AGONISTS<br/>[FR] DIPROVOCIMS: UNE NOUVELLE CLASSE PUISSANTE D'AGONISTES TLR
申请人:SCRIPPS RESEARCH INST
公开号:WO2018005812A1
公开(公告)日:2018-01-04
A diprovocim compound that corresponds in structure to structural Formula V is disclosed, wherein A, W, Z, R1, R2, R3 and R4 (when present) are defined within. A diprovocim compound has immune-adjuvant properties on human and mouse cells in culture and on in vivo immunization of mice. A composition containing a diprovocim and a method of using a compound are also disclosed. The immunostimulatory activity of a diprovocim compound is similar to that of LPS, to which there is no apparent structural similarity. A contemplated compound bears no structural similarity to either the TLR1/TLR2 lipoprotein agonists nor to any other synthetic TLR agonist, and is remarkably easy to prepare and synthetically modify.
揭示了一种与结构式V相对应的二丙醇化合物,其中A、W、Z、R1、R2、R3和R4(存在时)在内部定义。二丙醇化合物在培养的人类和小鼠细胞以及小鼠体内免疫接种中具有免疫佐剂特性。还揭示了含有二丙醇化合物的组合物和使用化合物的方法。二丙醇化合物的免疫刺激活性类似于脂多糖(LPS),但与之没有明显的结构相似性。所考虑的化合物与TLR1/TLR2脂蛋白激动剂或任何其他合成的TLR激动剂都没有结构相似性,并且非常容易制备和合成修饰。