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Derivatives of partially desulfated glycosaminoglycans as heparanase inhibitors with antiangiogenic activity and no anticoagulant effect

机译:部分脱硫的糖胺聚糖衍生物作为乙酰肝素酶抑制剂,具有抗血管生成活性,无抗凝作用

摘要

PROBLEM TO BE SOLVED: To provide an optimal glycosaminoglycan structure producing anti-angiogenic activity on the basis of heparanase inhibition and/or FGF growth factor inhibition mechanism, and to provide a medicinal substance which has anti-angiogenic activity substantially free from typical adverse effect of a heparin derivative, for example, anti-angiogenic activity.SOLUTION: A partially desulfated glycosaminoglycan derivative, in particular, heparin, above all, a compound of formula (I) (in the formula, U, R and Rgroups have the meaning described in specification) is provided. The glycosaminoglycan derivative has anti-angiogenic activity and heparanase inhibition activity and has no anticoagulant activity.
机译:解决的问题:提供基于乙酰肝素酶抑制和/或FGF生长因子抑制机制的产生抗血管生成活性的最佳糖胺聚糖结构,并提供具有抗血管生成活性的药物,该药物基本上没有典型的副作用。解决方案:部分脱硫的糖胺聚糖衍生物,特别是肝素,首先是式(I)的化合物(在式中,U,R和R基团的含义如规格)。糖胺聚糖衍生物具有抗血管生成活性和乙酰肝素酶抑制活性,并且不具有抗凝血活性。

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