Therapeutic dendrimer
AssigneeStarpharma Pty Limited
InventorsDavid James Owen, Brian Devlin Kelly
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Abstract
Provided herein are dendrimers comprising: a core unit, five generations of building units which are lysine residues or analogues thereof, first terminal groups comprising a cabazitazel residue covalently attached to a diglycolyl linker group, and second terminal groups comprising a PEG group. Also provided herein are pharmaceutical compositions comprising the dendrimers, and methods and uses of the dendrimers in therapy of disorders such as cancers. Processes for making the dendrimers and intermediates are also provided.
Claims24
A method of treating cancer comprising administering to a subject in need thereof a therapeutically effective amount of a dendrimer comprising:
- i) a core unit (C), wherein the core unit is:
- and
- ii) building units (BU), wherein the building unit are each:
- 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 cabazitazel residue covalently attached to a diglycolyl linker group;
- and
- iv) a plurality of second terminal groups (T2) each comprising a PEG group having an average molecular weight in the range of from 1,000 to 2,500 Daltons;
- wherein at least one third of the nitrogen atoms present in outer building units are each covalently attached to a first terminal group;
- and
- at least one third of the nitrogen atoms present in outer building units are each covalently attached to a second terminal group;
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.