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    • 7. 发明申请
    • LIPID A AND OTHER CARBOHYDRATE LIGAND ANALOGS
    • 脂肪酸和其他碳水化合物配体模拟物
    • WO2003094850A2
    • 2003-11-20
    • PCT/US2003/014633
    • 2003-05-09
    • BIOMIRA, INC.MCINNIS, PatriciaJIANG, Zi-HuaKOGANTY, R., RaoBUDZYNSKI, Wladyslaw
    • JIANG, Zi-HuaKOGANTY, R., RaoBUDZYNSKI, Wladyslaw
    • A61K
    • C07F9/091C07H13/06C07H15/04
    • The core structure of pentaerythritol has been used as a replacement for one or both sugars in lipid A, leading to the generation of a series of lipid A analogs. These lipid A analogs may further differ from lipid A with respect to, e.g., the number, nature and location of negatively charged groups, and the number, nature and location of the lipid chains. The lipid A analogs may be lipid A agonists useful as immunostimulatory agents, or lipid A antagonists useful in the treatment of septic shock. In a like manner, a residue of pentaerythritylamine may be used as a replacement for an amino sugar residue in a carbohydrate ligand having a biological activity of interest, generating a series of ligand analogs. These are useful, e.g., as haptens, inhibitors of bacterial-host cell adhesion, etc.
    • 季戊四醇的核心结构已被用作脂质A中的一种或两种糖的替代物,导致产生一系列脂质A类似物。 这些脂质A类似物可以进一步不同于脂质A,例如,带负电基团的数目,性质和位置以及脂链的数量,性质和位置。 脂质A类似物可以是可用作免疫刺激剂的脂质A激动剂或可用于治疗败血性休克的脂质A拮抗剂。 以类似的方式,可以使用季戊四胺的残基作为具有目标生物活性的碳水化合物配体中的氨基糖残基的替代物,产生一系列配体类似物。 这些是有用的,例如作为半抗原,细菌宿主细胞粘附抑制剂等