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    • 10. 发明申请
    • HYALURONIC ACID DERIVATIVE, METHOD OF PREPARATION THEREOF, METHOD OF MODIFICATION THEREOF AND USE THEREOF
    • 羟丙酸衍生物,其制备方法,其改性方法及其用途
    • WO2014023272A1
    • 2014-02-13
    • PCT/CZ2013/000091
    • 2013-08-05
    • CONTIPRO BIOTECH S.R.O.
    • BUFFA, RadovanSEDOVA, PetraWOLFOVA, LucieBASARABOVA, IvanaPOSPISIL, RobertHASOVA, MartinaNESPOROVA, KristinaVELEBNY, Vladimir
    • C08B37/00A61K31/728C08G81/00
    • C08B37/0072A61K47/61C07K17/10C08J3/075C08J2305/00
    • The invention relates to the preparation and use of α,β-unsaturated aldehyde of hyaluronan having a double bond in the positions 4 and 5 and an aldehydic group in the position 6 of the glucosamine part of the polysaccharide. The method of preparation is based on dehydration of hyaluronan having an aldehydic group in the position 6 of the glucosamine part of the polysaccharide. Two methods have been described, which are dehydration in a solution or heating in solid state in absence of solvents, bases or other additives. This derivative allows stabilization of conjugates of hyaluronan with amino compounds by means of a multiple bond from the aldehyde side, and therefore, it is possible to effectively immobilize practically any compound containing an amino group to such modified hyaluronan in physiological conditions. In case of using a diamine or compounds or polymers containing three or more amino groups, it is possible to prepare crosslinked hyaluronan derivatives. The described solution brings along a significant advantage not only in the field of carriers of biologically active substances, but also in tissue engineering where crosslinking with biologically acceptable amino compounds in physiological conditions is very much demanded.
    • 本发明涉及在位置4和5具有双键的透明质酸的α,β-不饱和醛和多糖的葡糖胺部分6位的醛基的制备和用途。 制备方法是基于在多糖的葡糖胺部分的位置6中具有醛基的透明质酸的脱水。 已经描述了两种方法,其在溶液中脱水或在没有溶剂,碱或其它添加剂的情况下以固态加热。 该衍生物允许透明质酸与氨基化合物的缀合物通过来自醛侧的多重键进行稳定化,因此,有可能在生理条件下实际上将含有氨基的任何化合物有效地固定在这种修饰的透明质酸上。 在使用二胺或含有三个以上氨基的化合物或聚合物的情况下,可以制备交联的透明质酸衍生物。 所描述的解决方案不仅在生物活性物质的载体领域具有显着的优点,而且在组织工程中,其中非常需要在生理条件下与生物可接受的氨基化合物进行交联。