Ascendis Pharma A/s

Ascendis Pharma Inc.

Ascendis Pharma Ophthalmology Division A/s

Ascendis Pharma Oncology Division A/s

Nicola Bisek

Harald Rau

Thomas Knappe

Samuel Weisbrod

Tobias Voigt

Ulrich Hersel

Thomas Wegge

Juha Punnonen

Sebastian Stark

Burkhardt Laufer

Kennett Sprogøe

Romy Reimann

Guillaume Maitro

Joachim Zettler

Oliver Keil

Torben Lessmann

Kennett Sprogoe

Felix Cleemann

David B Rosen

Franziska Hahn

Kornelia Bigott

Yang Yang-malten

Lars Holten-andersen

Kennett SprogØe

Luis Zuniga

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.

Hydrogel cross-linked hyaluronic acid prodrug compositions and methods

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.

Conjugation method for carrier-linked prodrugs

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.

Prodrugs comprising an aminoalkyl glycine linker

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.

Prodrugs comprising a pyroglutamate linker

Prodrugs or a pharmaceutically acceptable salt thereof which comprise a covalent treprostinil carrier conjugate, as well as their pharmaceutical composition, may be used as medicaments, especially for diseases or disorders which can be treated by treprostinil, such as pulmonary arterial hypertension (PAH).

Carrier-linked treprostinil prodrugs

The present invention relates to a pharmaceutical composition comprising one or more pharmaceutically acceptable excipient(s) and a VEGF neutralizing prodrug, which comprises a VEGF neutralizing biologically active moiety, for use in a method for the treatment of one or more ocular conditions.

VEGF neutralizing prodrugs for the treatment of ocular conditions

The present invention relates to compounds comprising a protecting group moiety-tag moiety conjugate, a method of purification and monoconjugates obtained from such method of purification.

Protecting group comprising a purification tag

The present invention relates to a process for the preparation of a hydrogel and to a hydrogel obtainable by said process. The present invention further relates to a process for the preparation of a hydrogel-spacer conjugate, to a hydrogel-spacer conjugate obtainable by said process, to a process for the preparation of a carrier-linked prodrug and to carrier-linked prodrugs obtainable by said process, in particular to carrier-linked prodrugs that provide for a controlled or sustained release of a drug from a carrier. In addition, the invention relates to the use of the hydrogel for the preparation of a carrier-linked prodrug.

Hydrogel prodrugs

The present invention relates to prodrugs or a pharmaceutically acceptable salt thereof comprising a covalent treprostinil carrier conjugate as well as pharmaceutical composition comprising said compounds. The compounds may be used as medicaments, especially for diseases or disorders which can be treated by treprostinil, such as pulmonary arterial hypertension (PAH).

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Heidelberg, Germany

Nicola Bisek