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US 2016/0096926 A1Published application
Chemically Modified Dendrimers
AssigneeGenzyme Corporation
InventorsLuis Z. Avila, Robert J. Miller, Lauren Elizabeth Young, Rajesh Vasant Kamath
Life of this patent
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Abstract
Dendrimers comprising N-acyl urea terminal moieties are described herein. The dendrimers can be used, for example, in the treatment of arthritis.
Claims20
(canceled)
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.
5 more elements
Dependencies are inferred from the claim text.