Polyanionic multivalent macromolecules for intracellular targeting of proliferation and protein synthesis
AssigneeMivenion GmbH
InventorsKai Licha, Michael Schirner, Pia Welker, Rainer Haag, Marie Weinhart, Florian Paulus
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Abstract
The present invention relates generally to methods and compositions for targeting of intracellular molecules involved in proliferation and protein synthesis of activated cells using polyanionic multivalent macromolecules. In particular aspect, multiple sulfate groups linked to polyol are specifically targeted to the cytoplasm and nucleus of proliferating and activated cells. The invention further comprises novel polyanionic macromolecular compounds and formulations.
Claims24
Pharmaceutical composition comprising a sulfated polyglycerol and a therapeutic or diagnostic effector molecule that is covalently conjugated to said sulfated polyglycerol.
Conjugate comprising a sulfated polyglycerol and a therapeutic or diagnostic effector molecule that is covalently conjugated to said sulfated polyglycerol.
A sulfated polyglycerol of the general formula P(OSO3−M+)n(L-G)m for treating a disease by intracellular uptake into activated cells or proliferative cells and by inhibiting NF-kappaB and/or AP-1 and/or inhibiting TGF-beta synthesis in said cells, with P stands for a polyglycerol wherein a number n of hydroxyl groups is substituted by sulfate groups OSO3−M+, M is a cationic inorganic or organic counter ion to the anionic sulfate group, m is a number of 1-100, L is a linker, G is a reactive group for the covalent attachment with effector molecules, wherein L is a branched or linear C1-20-alkyl group in which one or more non-consecutive methylene groups may be replaced by a group selected from O, S, NH, C(O)NH, C(O), SO2, SO, aryl, ethene or ethyne, and wherein G is selected from the group comprising —OH, —OSO3H, —OSO3−, —NH2, —N3, —COOH, —SH, —SO3−, —C≡C.
Dependencies are inferred from the claim text.