Degradable hyaluronic acid hydrogels
AssigneeAscendis Pharma A/S
InventorsSebastian STARK, Burkhardt LAUFER, Thomas KNAPPE, Tobias VOIGT, Nicola BISEK
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Abstract
The present invention relates to conjugates comprising crosslinked hyaluronic acid to which a plurality of drug moieties are covalently and reversibly conjugated, wherein the hyaluronic acid exhibits a certain degree of modification and comprises degradable crosslinker moieties. It also relates to their use as medicaments and their use in the diagnosis, prevention and treatment of diseases.
Claims7
A conjugate comprising crosslinked hyaluronic acid strands to which a plurality of drug moieties are covalently and reversibly conjugated, wherein the conjugate comprises a plurality of connected units selected from the group consisting of
- wherein
- an unmarked dashed line indicates a point of attachment to an adjacent unit at a dashed line marked with # or to a hydrogen;
- a dashed line marked with # indicates a point of attachment to an adjacent unit at an unmarked dashed line or to a hydroxyl;
- a dashed line marked with § indicates a point of connection between at least two units Z3 via a moiety —CL-;
- each —CL- comprises at least one degradable bond between the two carbon atoms marked with the * connected by a moiety —CL- and each —CL- is independently selected from the group consisting of formula (C-i), (C-ii), and (D-i),
- wherein
- dashed lines indicate attachment to a moiety —X0F— of a unit Z3;
- -D, -L1-, -L2-, -L3-, -L4-, —SP—, —X0A—, —X0B—, —X0C—, —X0D—, —X0E—XF, —Ra1 and —Ra2 are used as in claim 1;
- wherein
- all units Z1 present in the conjugate may be the same or different;
- all units Z2 present in the conjugate may be the same or different;
- all units Z3 present in the conjugate may be the same or different;
- the number of Z1 units ranges from 1% to 98% of the total number of units present in the conjugate;
- the number of Z2 units ranges from 0% to 98% of the total number of units present in the conjugate;
- the number of Z3 units ranges from 1% to 97% of the total number of units present in the conjugate, provided that at least one unit Z3 is present per strand which is connected to at least one unit Z3 on a different hyaluronic acid strand.
Dependencies are inferred from the claim text.