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    1,3,5-triazinane-2,4,6-trione derivatives and uses thereof
    3.
    发明授权
    1,3,5-triazinane-2,4,6-trione derivatives and uses thereof 有权
    1,3,5-三氮杂环戊烷-2,4,6-三酮衍生物及其用途

    公开(公告)号：US09315472B2

    公开(公告)日：2016-04-19

    申请号：US14267530

    申请日：2014-05-01

    Applicant: Massachusetts Institute of Technology

    Inventor： Yizhou Dong ,  Akinleye C. Alabi ,  Hao Yin ,  Joseph R. Dorkin ,  Delai Chen ,  Robert S. Langer ,  Daniel Griffith Anderson ,  Ahmed A. Eltoukhy

    IPC: C07D251/30 ,  A61K31/53 ,  A61K31/713

    CPC classification number: C07D251/30 ,  A61K31/53 ,  A61K31/713

    Abstract: The present invention provides novel 1,3,5-triazinane-2,4,6-trione derivatives, such as compounds of any one of Formulae (I) and (II), and salts thereof, and methods of preparing the compounds. Also provided are compositions including a compound of the invention and an agent (e.g., an siRNA, mRNA, or plasmid DNA). The present invention also provides methods and kits using the compositions for delivering an agent to a subject (e.g., to the liver, spleen, or lung of the subject) or cell and for treating and/or preventing a range of diseases, such as genetic diseases, proliferative diseases, hematological diseases, neurological diseases, liver diseases, and lung diseases.

    Abstract translation: 本发明提供新的1,3,5-三氮杂环丁烷-2,4,6-三酮衍生物，如式（I）和（II）中任一项的化合物及其盐，以及制备该化合物的方法。 还提供了包含本发明化合物和试剂（例如siRNA，mRNA或质粒DNA）的组合物。 本发明还提供了使用组合物将试剂递送至受试者（例如，受试者的肝脏，脾脏或肺）或细胞的方法和试剂盒，并用于治疗和/或预防一系列疾病，例如遗传 疾病，增殖性疾病，血液疾病，神经系统疾病，肝脏疾病和肺部疾病。

    ALPHA-AMINOAMIDINE POLYMERS AND USES THEREOF
    5.
    发明申请
    ALPHA-AMINOAMIDINE POLYMERS AND USES THEREOF 有权
    ALPHA-氨基丁胺聚合物及其用途

    公开(公告)号：US20140322309A1

    公开(公告)日：2014-10-30

    申请号：US14364028

    申请日：2012-12-15

    Applicant: Massachusetts Institute of Technology

    Inventor： Arturo Jose Vegas ,  Kathryn Ann Whitehead ,  Daniel Griffith Anderson ,  Robert S. Langer ,  Joseph R. Dorkin

    IPC: A61K47/34 ,  A61K31/713 ,  C08G12/34 ,  A61K39/00 ,  C12N15/113 ,  C08G12/06 ,  A61K33/00 ,  A61K38/16

    CPC classification number: A61K47/34 ,  A61K9/1271 ,  A61K9/5146 ,  A61K31/713 ,  A61K33/00 ,  A61K38/16 ,  A61K39/00 ,  C08G12/06 ,  C08G12/34 ,  C08G73/00 ,  C08L79/00 ,  C12N15/113

    Abstract: α-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 α-aminoamidine polymers, they are particularly suited for the delivery of polynucleotides. Complexes, micelles, liposomes or particles containing the inventive α-aminoamidine polymers and polynucleotides can be prepared. The inventive α-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.

    Abstract translation: α-氨基脒聚合物和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而制备α-氨基脒聚合物的方法。 还提供了从市售的原料制备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和生物相容的，并且可以用于各种药物递送系统和用于其它目的，例如涂料，添加剂，赋形剂，塑料和材料等。给定 这些α-氨基脒聚合物的氨基部分特别适用于递送多核苷酸。 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-氨基脒聚合物也可用于制备用于药物递送的微粒。 考虑到缓冲其周围环境的pH值，它们特别适用于提供不稳定剂。

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