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1. 发明申请

US20070010652A1 Polyamino acids functionalised with at least one hydrophobic group and applications thereof particularly therapeutic applications 失效
标题翻译：用至少一个疏水基团官能化的聚氨基酸及其应用特别是治疗应用
公开(公告)号：US20070010652A1
公开(公告)日：2007-01-11
申请号：US10558617
申请日：2004-05-28
申请人： Stephanie Angot , Olivier Breyne , You-Ping Chan
发明人： Stephanie Angot , Olivier Breyne , You-Ping Chan
IPC分类号： C08G69/10
CPC分类号： A61K8/88 , A61K47/645 , A61K2800/57 , A61Q19/00 , C08G69/10 , C08G69/48
摘要： The invention relates to novel materials based on biodegradable polyamino acids, particularly useful for the vectorisation of active principals (PA). The invention further relates to novel, pharmaceutical, cosmetic, dietary or phytosanitary compositions based on said polyamino acids. The aim of the invention is to provide a novel polymeric raw material, for use in the vectorisation of PA and with an optimal match for all the requirements of the type: biocompatibility, biodegradability, stability, ability to easily associate with numerous active principals or to solubilise the same and to liberate said active principals in vivo. Said aim is achieved with polyamino acids comprising aspartic and/or glutamate units, some of which carry at least one graft, characterised in that at least one of said grafts is bonded to an aspartic or glutamate unit by means of an amino acids spacer based on Leu, and/or Ileu, and/or Val, and/or Phe and a hydrophobic group with C6-C30 is connected by an ester bond to the spacer. Said specific amino acid spacers guarantee an improved stability to hydrolysis and a higher association quotient with proteins when compared with conventional analogous products. Said polymers have the advantage of easily and economically being transformed into vectorisation particles for active principals said particles being themselves able to form stable aqueous colloidal suspensions.
摘要翻译：本发明涉及基于可生物降解的聚氨基酸的新型材料，特别适用于活性成分（PA）的向量化。本发明进一步涉及基于所述聚氨基酸的新型药物，化妆品，膳食或植物检疫组合物。本发明的目的是提供一种新型的聚合物原料，用于PA的向量化，并具有与以下类型的所有要求的最佳匹配：生物相容性，生物可降解性，稳定性，容易与许多活性成分相关的能力或溶解相同并在体内释放所述活性成分。所述目的通过包含天冬氨酸和/或谷氨酸单体的聚氨基酸实现，其中一些氨基酸携带至少一个接枝物，其特征在于至少一个所述移植物通过氨基酸间隔基与天冬氨酸或谷氨酸单元结合，基于 Leu和/或Ileu和/或Val，和/或Phe和具有C6-C30的疏水基团通过酯键连接到间隔物上。当与常规类似产物相比时，所述特异性氨基酸间隔物保证了水解的稳定性提高和与蛋白质的较高缔合商。所述聚合物具有容易且经济地转化成用于活性原料的载体化颗粒的优点，所述颗粒本身能够形成稳定的水性胶体悬浮液。

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