Starpharma Pty Limited

Baker Idi Heart and Diabetes Institute Holdings Limited

David James Owen

Brian Devlin Kelly

Peter Karellas

Karlheinz Peter

Guy Yeoman Krippner

Jeremy Robert Arthur Paull

Jacinth Kincaid Fairley

Zemin Wu

Nicola Jane Main

Pauline Stanislawski

Ryan T Hayes

Abhay Singh Chauhan

Michael Giannis

Veera Reddy Pulgam

Stephanie Ruth Edmondson

Oliver Bernhard

Harsh Vardhan

Christoph Hagemeyer

Olivier Bernhard

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.

Therapeutic dendrimer

The present invention generally relates to macromolecules of dendrimer-drug conjugates. In particular, the invention relates to macromolecules comprising a pharmaceutically active agent, such as a protein or peptide, attached to a core of a dendrimer derived from branched building units, such as lysine or lysine analogues. The invention also relates to the synthesis of the dendrimers and macromolecules, and the use of such macromolecules, particularly in therapeutic applications, and pharmaceutical compositions comprising them.

Dendrimer-drug conjugates

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.

Macromolecules

The present invention relates to a macromolecule comprising a dendrimer having surface amino groups to which at least two different terminal groups are attached including a pharmaceutically active agent and a pharmacokinetic modifying agent, the pharmaceutically active agent comprising a hydroxyl group and being attached to the surface amino group of the dendrimer through a diacid linker. Pharmaceutical compositions comprising the macromolecules and methods of treatment using the macromolecules are also described.

PEHAM dendrimers of the formula:  Specific PEHAM dendrimers are used in a formulation with an active agent for agricultural purposes. In particular, the PEHAM dendrimers may be used for increasing the efficacy of the active agent in various ways, such as by improving solubility of the active agent in the formulation, by improving adhesion and penetration of the active agent to plant surfaces, or by improving the water-fastness of the active agent to the plant or seed. The PEHAM dendrimers may also increase the efficacy of the active agent by increasing soil penetration of the active agent to reach the plant roots or under soil parts, by reducing soil adhesion of the active agent to reach the plant roots or under soil parts, or by reducing enzymatic degradation of the active agent by the plant or seed or microorganisms in the soil.

PEHAM dendrimers for use in agriculture

The present invention relates generally to branched macromolecules and their use as imaging or contrast agents. In particular, the invention relates to dendrimers, derived from lysine or lysine analogs, bearing a plurality of functional moieties and their application to imaging techniques in which a disease state may be imaged with a targeted contrast agent.

Polylysine dendrimer contrast agent

Growing community of inventors

Kew, Australia

David James Owen