Macromolecules

US10265409B2 · kind B2 · utility

Assignee

• Starpharma Pty Ltd. · AU

Inventors

• David Owen · Melbourne, AU
• Brian Devlin Kelly · Melbourne, AU
• Peter Karellas · Morgan, AU

Key dates

• Filing date: Aug 28, 2017
• Grant date: Apr 23, 2019
• Expiry date: Oct 12, 2037

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C08G83/003
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

A macromolecule includes i) a dendrimer with a core and at least one generation of lysine residue building units, the outermost generation of building units having surface amino groups, ii) a first terminal group covalently attached to a first surface amino group of a building unit, which includes a residue of docetaxel (DTX), and iii) a second terminal group covalently attached to a second surface amino group of a building unit, which includes a pharmacokinetic modifying agent. The pharmacokinetic modifying agent can be a polyethylene glycol (PEG). The first terminal group can be covalently attached to the surface amino group of the dendrimer through a diacid linker. The diacid linker can include a 2,2′-thiodiacetic acid residue. The diacid linker can form an ester bond with a hydroxyl group of the DTX and an amide bond with the surface amino group. A pharmaceutically acceptable salt of the macromolecule can be prepared.