Therapeutic conjugates with sulfated dendrimers for intracellular targeting

US11045560B2 · kind B2 · utility

Inventors

• Kai Licha · Berlin, DE
• Michael Schirner · Berlin, DE

Key dates

• Filing date: May 21, 2015
• Grant date: Jun 29, 2021
• Expiry date: May 21, 2035

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C12Y305/01001
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present invention relates to novel dendrimer conjugates, methods for their preparation and their use for treatment of diseases. The invention discloses a new method for the delivery of dendrimer conjugates with therapeutically active molecules into the cell by utilizing transmembrane solute carrier proteins enabling uptake of the inventive dendrimer conjugates. Particular subject-matter of the present invention is a conjugate of the formula E-[G-L-D(OSO3−M+)n]m, wherein E is a therapeutic or diagnostic effector molecule, wherein D(OSO3−M+)n is a dendrimer D carrying a number n of sulfate groups OSO3−M+, wherein the number n of sulfate groups is selected from 6 to 96, wherein M is a cationic inorganic or organic counter ion to the anionic sulfate group, wherein L is a linker or spacer between D and E, wherein G is a connecting functional group forming the attachment between L and E, and wherein m is an integer from 1 to 20.