公开(公告)号：US09522192B2

公开(公告)日：2016-12-20

申请号：US14103463

申请日：2013-12-11

申请人： EPITECH GROUP S.r.l.

发明人： Antonio Calignano ,  Giuseppe D'Agostino ,  Sonia Laneri ,  Rosaria Meli ,  Carmine Ostacolo ,  Roberto Russo ,  Antonia Sacchi ,  Diana Tronino ,  Francesco Della Valle ,  Maria Federica Della Valle ,  Gabriele Marcolongo

IPC分类号： A61K31/164 ,  C07C235/08 ,  A61K47/48 ,  C07C231/12 ,  C07C235/20 ,  C08G59/00

CPC分类号： A61K47/48215 ,  A61K31/164 ,  A61K47/60 ,  C07C231/12 ,  C07C235/20 ,  C08G65/332 ,  C08G65/33324 ,  C08L2203/02

摘要： The synthesis of a series of Polyethylene glycol conjugates (esters and carbonates) of PEA and its analogous acylethanolamides, have higher water solubility and good hydrophilic/lipophilic balance, resulting in (i) improved accumulation in tissues (particularly skin and mucosae), (ii) prolonged release, and (iii) increased bioavailability. Improvement of PEA and analogous acylethanolamides levels in the tissues—particularly in the skin and mucosae—and their prolonged release is due to the improved bioavailability of related conjugates. Conjugates are able to extend the time frame in which PEA and analogous acylethanolamides exert their pharmacological effects.

摘要翻译： 一系列聚乙二醇共轭物（酯和碳酸酯）的一系列PEA及其类似的酰基乙醇酰胺的合成具有较高的水溶性和良好的亲水/亲油平衡，导致（i）改善组织（特别是皮肤和粘膜）中的积累，（ii ）延长释放，和（iii）增加的生物利用度。 组织中特别是皮肤和粘膜中PEA和类似的乙酰乙酰胺水平的改善及其延长的释放是由于相关缀合物的生物利用度得到改善。 共轭物能够延长PEA和类似的乙酰乙酰胺发挥其药理作用的时间框架。