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    • 3. 发明申请
    • ALPHA-AMINOAMIDINE POLYMERS AND USES THEREOF
    • α-氨基酰胺聚合物及其用途
    • WO2013090861A8
    • 2013-08-22
    • PCT/US2012069961
    • 2012-12-15
    • MASSACHUSETTS INST TECHNOLOGY
    • VEGAS ARTURO JOSEWHITEHEAD KATHRYN ANNANDERSON DANIEL GRIFFITHLANGER ROBERT SDORKIN JOSEPH R
    • C08G73/00A61K9/127A61K9/51A61K47/34C08L79/00C12N15/88
    • A61K47/34A61K9/1271A61K9/5146A61K31/713A61K33/00A61K38/16A61K39/00C08G12/06C08G12/34C08G73/00C08L79/00C12N15/113
    • alpha-Aminoamidine polymers and methods of preparing a-aminoamidine polymers by reacting by reacting one or more amines with one or more isocyanides and one or more aldehydes are described. Methods of preparing a-aminoamidine polymers from commercially available starting materials are also provided, wherein the starting materials are racemic or stereochemically pure. a-Aminoamidine polymers or salt forms thereof are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems and for other purposes as well such as, for example, coatings, additives, excipients, plastics, and materials, etc. Given the amino moiety of these alpha-aminoamidine polymers, they are particularly suited for the delivery of polynucleotides. Complexes, micelles, liposomes or particles containing the inventive alpha-aminoamidine polymers and polynucleotides can be prepared. The inventive alpha-aminoamidine polymers may also be used in preparing microparticles for drug delivery. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings.
    • α-氨基脒聚合物以及通过使一种或多种胺与一种或多种异氰化物和一种或多种醛反应来制备α-氨基脒聚合物的方法。 还提供了由市售原料制备α-氨基脒聚合物的方法,其中原料是外消旋或立体化学纯的。 α-氨基脒聚合物或其盐形式优选是可生物降解的和生物相容的,并且可以用于多种药物递送系统中以及用于其他目的,例如涂料,添加剂,赋形剂,塑料和材料等。给定的 这些α-氨基脒聚合物的氨基部分,它们特别适合于递送多核苷酸。 可以制备含有本发明α-氨基脒聚合物和多核苷酸的复合物,胶束,脂质体或颗粒。 本发明的α-氨基脒聚合物也可以用于制备用于药物递送的微粒。 考虑到它们缓冲周围环境pH的能力,它们在提供不稳定剂方面特别有用。