申请人:Ranganathan Ramachandran
公开号:US20080300220A1
公开(公告)日:2008-12-04
Disclosed herein is a class of linkable tetrasaccharide compounds that includes the amino phenyl glycoside of sialyl Lewis X (SLe
X
) and related analogs. These compounds have conjugatable nucleophilic groups, making them useful in preparing multimeric SLe
X
compositions. In particular, the disclosed SLe
X
compounds can be used to prepare selectin binding ligand conjugates by linking them to a reporter moiety, such as a contrast agent, a radiodiagnostic agent, or a cytotoxic or chemotherapeutic agent. The SLe
X
compounds and conjugates of the invention exhibit binding to selectin that is similar to native Sialyl Le
X
, and are, therefore, useful for diagnosing and treating selectin-mediated disorders and related conditions.
本发明涉及一类可连接的四糖化合物,其中包括唾液酸Lewis X(SLeX)的氨基苯基糖苷和相关类似物。这些化合物具有可共轭的亲核基团,使它们在制备多聚SLeX组分方面非常有用。特别是,所披露的SLeX化合物可用于通过将它们连接到报告者基团(如对比剂、放射诊断剂或细胞毒素或化学治疗剂)来制备选择素结合配体共轭物。本发明的SLeX化合物和共轭物表现出与天然唾液酸LeX类似的选择素结合性,因此,它们对于诊断和治疗选择素介导的疾病和相关病症非常有用。