首页> 外国专利> DERIVATIVES OF PARTIALLY DESULPHATED GLYCOSAMINOGLYCANS AS HEPARANASE INHIBITORS, ENDOWED WITH ANTIANGIOGENIC ACTIVITY AND DEVOID OF ANTICOAGULATING EFFECT

DERIVATIVES OF PARTIALLY DESULPHATED GLYCOSAMINOGLYCANS AS HEPARANASE INHIBITORS, ENDOWED WITH ANTIANGIOGENIC ACTIVITY AND DEVOID OF ANTICOAGULATING EFFECT

机译:部分脱硫的糖氨聚糖作为肝素酶抑制剂的衍生物,具有抗血管生成活性和抗凝作用

摘要

PROBLEM TO BE SOLVED: To find optimal glycosaminoglycan structures for generating antiangiogenic activity based on heparanase inhibition and/or FGF growth factor inhibition mechanisms, and to provide a medicament with antiangiogenic activity which is essentially devoid of the typical side effects of heparin derivatives, such as anticoagulant activity.;SOLUTION: Partially desulphated glycosaminoglycan derivatives are described, particularly heparin, and more particularly a compound of formula (I) where the U, R and R1 groups have the meanings indicated herein. These glycosaminoglycan derivatives have antiangiogenic and heparanase-inhibiting activity and are devoid of anticoagulant activity.;COPYRIGHT: (C)2016,JPO&INPIT
机译:要解决的问题:基于乙酰肝素酶抑制和/或FGF生长因子抑制机制寻找产生抗血管生成活性的最佳糖胺聚糖结构,并提供一种具有抗血管生成活性的药物,该药物基本上没有肝素衍生物的典型副作用,例如解决方案:解决方案:描述了部分脱硫的糖胺聚糖衍生物,特别是肝素,更特别是其中U,R和R Sub 1 具有本文所指含义的式(I)化合物。这些糖胺聚糖衍生物具有抗血管生成和抑制乙酰肝素酶的活性,并且没有抗凝血活性。;版权所有:(C)2016,JPO&INPIT

著录项

  • 公开/公告号JP2016014148A

    专利类型

  • 公开/公告日2016-01-28

    原文格式PDF

  • 申请/专利权人 SIGMA-TAU RESEARCH SWITZERLAND SA;

    申请/专利号JP20150178518

  • 申请日2015-09-10

  • 分类号C08B37/10;A61P43/00;A61P29/00;A61P9/00;A61P37/06;A61P35/00;A61P35/04;A61P9/10;A61P27/02;A61P17/06;A61P19/02;A61P7/02;A61P13/12;A61P9/12;A61P11/06;A61P9/04;A61P25/00;A61P3/10;A61P1/04;A61K31/727;A61K47/36;A61K45/00;C12N9/88;C12N9/99;C12P11/00;C12P13/00;C12P19/00;C12N9/14;

  • 国家 JP

  • 入库时间 2022-08-21 14:45:23

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