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US 12,616,711 B2Granted
Therapeutic dendrimer
AssigneeStarpharma Pty Limited
InventorsDavid James Owen, Rashmi Pathak
Life of this patent
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Abstract
Provided herein are dendrimers comprising a core unit, five generations of building units being a lysine residue or analogue thereof, a plurality of first terminal groups each comprising a residue of a nucleoside analogue, and a plurality of second terminal groups each comprising a hydrophilic polymeric group. Also provided herein are pharmaceutical compositions comprising the dendrimer, and methods and uses of the dendrimers in therapy of disorders such as cancer.
Claims22
A dendrimer comprising:
- i) a core unit (C) which is
- and
- ii) building units (BU), which are
- wherein the acyl group of each building unit provides a covalent attachment point for attachment to the core or to a previous generation building unit;
- and wherein each nitrogen atom provides a covalent attachment point for covalent attachment to a subsequent generation building unit, a first terminal group or a second terminal group;
- wherein the core unit is covalently attached to two building units via amide linkages, each amide linkage being formed between a nitrogen atom present in the core unit and the carbon atom of an acyl group present in a building unit;
- the dendrimer being a five generation building unit dendrimer;
- wherein building units of different generations are covalently attached to one another via amide linkages formed between a nitrogen atom present in one building unit and the carbon atom of an acyl group present in another building unit;
- the dendrimer further comprising:
- iii) a plurality of first terminal groups (T1) each comprising a residue of a nucleoside analogue, which nucleoside analogue has a hydroxyl group, covalently attached to a diacyl linker group of formula:
- and
- iv) a plurality of second terminal groups (T2) each comprising a hydrophilic polymeric group which is a polyethylene glycol (PEG) group;
- or
- a pharmaceutically acceptable salt thereof.
11 more elements
Dependencies are inferred from the claim text.