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MEDICAL USE OF POLY(PROPYLENE IMINE) GLYCODENDRIMERS

机译:聚丙烯亚胺糖苷配基的医学用途

摘要

The invention relates to poly(propylene imine) glycodendrimers, abbreviated as GD-PPI, wherein GD is a dendrimer coated with a sugar selected from a group comprising monosaccharides, disaccharides and trisaccharides, and PPI is a poly(propylene imine) dendrimer selected from a group of third, fourth and fifth generation dendrimers with a level of coating (surface modification) with a selected sugar within a range above 5 to about 100%, for therapeutic use in neoplastic diseases associated with chromosomal and/or genetic aberrations typical of chronic B cell lymphoproliferative diseases. The above group of compounds includes novel poly(propylene imine) glycodendrimers, abbreviated as GD-PPI, wherein GD is a dendrimer coated with lactose (disaccharide) or mannose (monosaccharide), and PPI is as defined above. In addition, the poly(propylene imine) glycodendrimers, abbreviated as GD-PPI, wherein GD is a dendrimer coated with maltotriose (trisaccharide) with a level of coating within the range above 5 to about 100%, except the values from 35% to 45% and from 80% to 95% which are being excluded, and PPI is as defined above, are novel. Selected compounds from the group of glycodendrimers defined above are intended for the therapeutic use in proliferative neoplastic blood diseases with an impaired apoptosis mechanism. The invention relates also to pharmaceutical compositions comprising the afore-mentioned compounds as therapeutically active substances. The aforementioned compounds are used for the manufacture of medicaments against the indicated medical conditions and in methods of treatment of those medical conditions.
机译:本发明涉及缩写为GD-PPI的聚(丙烯亚胺)糖树状聚合物,其中GD是用糖包被的树状聚合物,糖选自单糖,二糖和三糖,PPI是选自丙烯酰胺的树状聚合物。一组第三,第四和第五代树状聚合物,其被覆糖的水平(表面修饰)在5%至约100%以上的范围内,用于治疗与慢性B型典型的染色体和/或遗传异常有关的肿瘤疾病细胞淋巴增生性疾病。上面的化合物包括新的聚(丙烯亚胺)糖类树状聚合物,缩写为GD-PPI,其中GD是涂有乳糖(二糖)或甘露糖(单糖)的树状聚合物,并且PPI如上定义。另外,聚(丙烯亚胺)糖树状聚合物,缩写为GD-PPI,其中GD是用麦芽三糖(三糖)包被的树状聚合物,包衣水平在5%至约100%的范围内,除了35%至35%的值。排除了45%和80%至95%的PPI是新颖的。从上面定义的糖类树状聚合物的组中选择的化合物旨在用于增殖性肿瘤性血液疾病的治疗用途,其凋亡机制受损。本发明还涉及包含上述化合物作为治疗活性物质的药物组合物。前述化合物用于针对指定的医学状况的药物的生产以及在那些医学状况的治疗方法中。

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