公开(公告)号：EP2734645A4

公开(公告)日：2014-12-17

申请号：EP12815580

申请日：2012-07-18

申请人： UNIV GEORGIA STATE RES FOUND

发明人： HENARY MAGED ,  WILSON W DAVID

IPC分类号： C12Q1/68

CPC分类号： C09B23/06 ,  C07D209/14 ,  C07D403/06

摘要： Cyanines which selectively bind to G-quadruplex DNA complexes, particularly quadruplexes expressed in cancer cells, and methods of making and using thereof are described herein. The cyanine can be a symmetrical or unsymmetrical streptocyanine, hemicyanine, closed chain cyanine, or combinations thereof. The cyanine is preferably substituted with one or more groups that minimize or prevent aggregation of the cyanine and/or inhibit binding of the cyanine to duplex DNA. One or more of the cyanines can be formulated with one or more pharmaceutical excipients and/or carrier to prepare pharmaceutical compositions suitable for administration to a patient, particular a human patient. The compounds and compositions described herein can be used to treat diseases or disorders characterized by the expression of G-quadruplex DNA, such as cancer.

摘要翻译： 本文描述了选择性结合G-四链体DNA复合物，特别是在癌细胞中表达的四链体的花青苷及其制备和使用方法。 花青可以是对称或不对称的链花青，半花青，闭环花青或其组合。 花青优选被一个或多个使花青聚集和/或抑制花青与双链DNA结合的聚集或阻止聚集的基团取代。 一种或多种花青可以与一种或多种药物赋形剂和/或载体一起配制，以制备适于给予患者，特别是人类患者的药物组合物。 本文所述的化合物和组合物可用于治疗特征在于表达G-四链体DNA（例如癌症）的疾病或病症。