发明名称 Chemically modified dendrimers
摘要 Dendrimers comprising N-acyl urea terminal moieties are described herein. The dendrimers can be used, for example, in the treatment of arthritis.
申请公布号 US9611357(B2) 申请公布日期 2017.04.04
申请号 US201514966935 申请日期 2015.12.11
申请人 Genzyme Corporation 发明人 Avila Luis Z.;Miller Robert J.;Young Lauren Elizabeth;Kamath Rajesh Vasant
分类号 C08G69/48;C08G69/08;C08G73/02;C08G83/00;A61K31/785 主分类号 C08G69/48
代理机构 Fish & Richardson P.C. 代理人 Fish & Richardson P.C.
主权项 1. A method of making a dendrimer, wherein the dendrimer comprises a plurality of branched repeating units radiating out from a central atom, multifunctional moiety, or cluster of atoms, wherein each repeating unit comprises a terminal moiety, wherein at least about 5% of the terminal moieties include a urea of formula (I) wherein each of R1 and R2 is independently C1-C6 alkyl, C1-C6 alkenyl, cyclyl, aryl, heterocyclyl, heteroaryl, cyclylalkyl, arylalkyl, heterocyclylalkyl, or heteroarylalkyl; any of which are optionally substituted by C1-C6 alkyl, amino, C1-C6 alkylamino, C1-C6 dialkylamino, hydroxy, C1-C6 alkoxy, and wherein either of R1 or R2 independently optionally have a net charge; indicates the point of attachment of the terminal moiety of formula (I) to the dendrimer; and less than about 12% of the terminal moieties are covalently bound to a saccharide moiety, wherein the method comprises reacting a dendrimer comprising a plurality of terminal carboxylic acid moieties with a carbodiimide, wherein the carbodiimide is substituted with R1 and R2, thereby making the dendrimer.
地址 Cambridge MA US