Abstract: The present invention relates to reagents comprising a substituted acyl borate or a substituted hydroxylamine, to a method of synthesizing a carrier-linked prodrug using said reagents and to carrier-linked prodrugs obtainable by said method.

Abstract: The present invention relates to hydrogel prodrug compositions comprising cross-linked hyaluronic acid (HA), or a derivative or a salt thereof, wherein the cross-linker system comprises a biodegradable spacer, wherein the cross-linked HA comprises a conjugated drug-linker, and wherein the linker is capable of releasing the drug under physiological conditions. The present invention further relates to methods for preparing the hydrogel prodrug compositions. The present invention further relates to methods for treating an ocular condition using the hydrogel compositions.

Abstract: The present invention relates to a process for the irradiation of a water-insoluble conjugate comprising a polymer Z to which a plurality of moieties -L2-L1-D is covalently conjugated or of a water-insoluble complex comprising a plurality of releasably and non-covalently bound drug molecules D-H or D-OH embedded in a polymer Z?, wherein the process comprises the steps of (a) providing said conjugate or complex; and (b) exposing the conjugate or complex to ionizing radiation; wherein each -L2- is independently a chemical bond or is a spacer moiety; each -L1- is independently a linker moiety covalently and reversibly attached to -D; and each -D is independently a drug moiety.

Abstract: The present invention relates to hydrogel prodrug compositions comprising cross-linked hyaluronic acid (HA), or a derivative or a salt thereof, wherein the cross-linker system comprises a biodegradable spacer, wherein the cross-linked HA comprises a conjugated drug-linker, and wherein the linker is capable of releasing the drug under physiological conditions. The present invention further relates to methods for preparing the hydrogel prodrug compositions. The present invention further relates to methods for treating an ocular condition using the hydrogel compositions.

Abstract: The present invention relates to novel prodrugs of primary or secondary amine- or hydroxyl-comprising biologically active moieties and pharmaceutically acceptable salts thereof, prodrug reagents, pharmaceutical compositions comprising these prodrugs and the use of these prodrugs. A disclosed prodrug may include a biologically active moiety reversibly and covalently linked to a specialized protective group; the linker may be reversible (i.e., hydrolytically cleavable in the absence of enzymes under physiological conditions) and, upon cleavage, may release a drug in its unmodified, pharmacologically active form.

Abstract: The present invention relates to a tyrosine kinase inhibitor (“TKI”) conjugate or a pharmaceutically acceptable salt thereof, wherein said conjugate comprises a plurality of TKI moieties -D covalently conjugated via at least one moiety -L1-L2- to a polymeric moiety Z, wherein -L1- is covalently and reversibly conjugated to -D and -L2- is covalently conjugated to Z and wherein -L1- is a linker moiety and -L2- is a chemical bond or a spacer moiety; and to related aspects.

Abstract: The present invention relates to conjugates of ?-electron-pair-donating heteroaromatic nitrogen-comprising drugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising said conjugates and the use of said conjugates as medicaments.

Abstract: The present invention relates to conjugates of ?-electron-pair-donating heteroaromatic nitrogen-comprising drugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising said conjugates and the use of said conjugates as medicaments.

Abstract: The present invention relates to conjugates of an electron-donating heteroaromatic nitrogen or tertiary amine comprising drugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising said conjugates and the use of said conjugates as medicaments.

Abstract: The present invention relates to novel prodrugs of primary or secondary amine-comprising biologically active moieties and pharmaceutically acceptable salts thereof, prodrug reagents, pharmaceutical compositions comprising said prodrugs and the use of prodrugs.

Abstract: The present invention relates to a conjugate or its pharmaceutically acceptable salt, wherein said conjugate is water-in-soluble and comprises a carrier moiety Z to which one or more moieties -L2-L1-D are conjugated, wherein each -L2- is individually a chemical bond or a spacer moiety; each -L1- is individually a linker moiety to which -D is reversibly and covalently conjugated; and each -D is individually a pattern recognition receptor agonist. It further relates to pharmaceutical compositions comprising such conjugate and to their use in the treatment of cell-proliferation disorders; and to related aspects.

Abstract: The present invention relates to a water-insoluble controlled-release pattern recognition receptor agonist (“PRRA”) for use in the treatment of a cell-proliferation disorder, wherein the water-insoluble controlled-release PRRA is administered by intra-tissue administration, and wherein the protein levels of at least one cytokine selected from the group consisting of IL-6, CCL2 and EL-10 in plasma has a more than 10-fold lower maximum protein level within 24 hours compared to an equivalent molar dose of the corresponding free PRRA upon intra/tissue administration; and to related aspects.

Abstract: The present invention relates to a water-insoluble controlled-release pattern recognition receptor agonist (“PRRA”) or its pharmaceutically acceptable salt or a pharmaceutical composition comprising such water-insoluble controlled-release PRRA or its pharmaceutical acceptable salt for use in the treatment of a cell-proliferation disorder, wherein the water-insoluble controlled-release PRRA, its pharmaceutically acceptable salt or the pharmaceutical composition is administered by intra-tissue administration, and wherein such intra-tissue administration results in local inflammation; and to related aspects.

Abstract: The present invention relates to a water-insoluble controlled-release pattern recognition receptor agonist (“PRRA”) or its pharmaceutically acceptable salt or a pharmaceutical composition comprising such water-insoluble controlled-release PRRA or its pharmaceutical acceptable salt for use in the treatment of a cell-proliferation disorder, wherein the water-insoluble controlled-release PRRA, its pharmaceutically acceptable salt or the pharmaceutical composition is administered by intra-tissue administration, and wherein at least 25% of the amount of PRRA remains local in such tissue 3 days after administration; and to related aspects.

Abstract: The present invention relates to reagents comprising a substituted acyl borate or a substituted hydroxylamine, to a method of synthesizing a carrier-linked prodrug using said reagents and to carrier-linked prodrugs obtainable by said method.

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 crosslinked moieties. It also relates to their use as medicaments and their use in the diagnosis, prevention and treatment of diseases.

Abstract: The present invention relates among other aspects to a conjugate or a pharmaceutically acceptable salt thereof or a pharmaceutical composition comprising said conjugate or its pharmaceutically acceptable salt for use in a method of preventing or treating an infection, wherein said conjugate is water-insoluble and comprises a polymeric moiety —Z to which a plurality of moieties -L2-X0D-L1-D are covalently conjugated, wherein each -D is independently an antibiotic moiety; each -L1- is independently a linker moiety to which -D is covalently and reversibly conjugated; each —X0D— is independently absent or a linkage and each -L2- is independently either a chemical bond or a spacer moiety.

Abstract: The present invention relates to conjugates comprising backbone moieties that are crosslinked via particular crosslinker moieties to which a plurality of drug moieties are covalently and reversibly conjugated. It also relates to their use as medicaments and their use in the diagnosis, prevention and treatment of diseases.

Abstract: The present invention relates to IL-2 conjugates, a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising such IL-2 conjugate or a pharmaceutically acceptable salt thereof and their uses.

Abstract: The present invention relates to a conjugate comprising a moiety of formula (I) or to conjugates of formula (I?) and to pharmaceutical compositions comprising such conjugates.