公开(公告)号：US11642415B2

公开(公告)日：2023-05-09

申请号：US16575749

申请日：2019-09-19

申请人： Ascendis Pharma A/S

发明人： Sebastian Stark ,  Thomas Knappe ,  Harald Rau ,  Nicola Bisek ,  Burkhardt Laufer ,  Samuel Weisbrod ,  Tobias Voigt

IPC分类号： A61K47/61 ,  A61K47/69 ,  A61K9/00 ,  A61K39/395

CPC分类号： A61K47/61 ,  A61K9/0019 ,  A61K9/0048 ,  A61K39/395 ,  A61K47/6903

摘要： 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.

公开(公告)号：US11896671B2

公开(公告)日：2024-02-13

申请号：US16317689

申请日：2017-07-12

申请人： Ascendis Pharma A/S

发明人： Nicola Bisek ,  Samuel Weisbrod ,  Kornelia Bigott

IPC分类号： A61K47/61 ,  A61K47/54 ,  A61K47/64 ,  A61K47/60

CPC分类号： A61K47/545 ,  A61K47/542 ,  A61K47/60 ,  A61K47/61 ,  A61K47/64

摘要： 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.

公开(公告)号：US20150258205A1

公开(公告)日：2015-09-17

申请号：US14434585

申请日：2013-10-08

申请人： ASCENDIS PHARMA A/S

发明人： Harald Rau ,  Tobias Voigt ,  Burkhardt Laufer ,  Nicola Bisek ,  Franziska Hahn ,  Thomas Knappe

IPC分类号： A61K47/48 ,  C08G69/44 ,  C08G69/48 ,  A61K31/4188

CPC分类号： A61K47/60 ,  A61K31/4188 ,  A61K47/557 ,  A61K47/59 ,  A61K47/645 ,  A61K47/6845 ,  A61K47/6849 ,  A61K47/6903 ,  C08F2/22 ,  C08G65/332 ,  C08G65/3322 ,  C08G65/33337 ,  C08G65/33389 ,  C08G69/44 ,  C08G69/48 ,  C08G83/004 ,  C08G83/006 ,  C08G2210/00 ,  C08J3/075 ,  C08J2300/202 ,  C08J2371/02 ,  C08J2400/202 ,  C08J2471/02 ,  C08L2203/02

摘要： 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.

摘要翻译： 本发明涉及一种制备水凝胶和通过所述方法获得的水凝胶的方法。 本发明还涉及一种制备水凝胶 - 间隔物缀合物的方法，可通过所述方法获得的水凝胶 - 间隔缀合物，制备载体连接的前药的方法和由所述载体连接的前体药物可获得的载体连接的前药 方法，特别是提供从载体中控制或持续释放药物的载体连接的前药。 此外，本发明涉及水凝胶用于制备载体连接的前药的用途。

公开(公告)号：US11633487B2

公开(公告)日：2023-04-25

申请号：US15502084

申请日：2015-08-04

申请人： Ascendis Pharma A/S

发明人： Nicola Bisek ,  Harald Rau ,  Felix Cleemann ,  Thomas Knappe ,  Romy Reimann

IPC分类号： A61K47/65 ,  A61K47/60 ,  A61K38/28 ,  A61K47/54 ,  A61K47/68

摘要： 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.

公开(公告)号：US20190216940A1

公开(公告)日：2019-07-18

申请号：US15577606

申请日：2016-05-25

申请人： Ascendis Pharma A/S ,  Ascendis Pharma Inc.

发明人： Harald Rau ,  Nicola Bisek ,  Samuel Weisbrod

IPC分类号： A61K47/64 ,  A61K47/60

CPC分类号： A61K47/645 ,  A61K47/54 ,  A61K47/60

摘要： 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.

公开(公告)号：US20180312582A1

公开(公告)日：2018-11-01

申请号：US16026397

申请日：2018-07-03

申请人： Ascendis Pharma A/S

发明人： Harald Rau ,  Nicola Bisek ,  Thomas Knappe ,  Romy Reimann ,  Sebastian Stark ,  Samuel Weisbrod

IPC分类号： C07K16/22 ,  A61K47/64 ,  C07K1/107 ,  A61K47/54 ,  C07K1/18

CPC分类号： C07K16/22 ,  A61K47/543 ,  A61K47/641 ,  A61K47/645 ,  C07K1/1075 ,  C07K1/18 ,  C07K2317/24 ,  C07K2317/55 ,  Y02P20/55

摘要： 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.

公开(公告)号：US11298427B2

公开(公告)日：2022-04-12

申请号：US15577606

申请日：2016-05-25

申请人： Ascendis Pharma A/S ,  Ascendis Pharma Inc.

发明人： Harald Rau ,  Nicola Bisek ,  Samuel Weisbrod

IPC分类号： A61K47/64 ,  A61K47/60 ,  A61K47/54

摘要： 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.

公开(公告)号：US20210008168A1

公开(公告)日：2021-01-14

申请号：US17042530

申请日：2019-03-27

申请人： Ascendis Pharma A/S

发明人： Thomas` Knappe ,  Kennett Sprogøe ,  Nicola Bisek ,  Burkhardt Laufer

IPC分类号： A61K38/20 ,  A61K47/54 ,  A61K47/18 ,  A61K47/60

摘要： 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.

公开(公告)号：US10040850B2

公开(公告)日：2018-08-07

申请号：US15027976

申请日：2014-10-07

申请人： Ascendis Pharma A/S

发明人： Harald Rau ,  Nicola Bisek ,  Thomas Knappe ,  Romy Reimann ,  Sebastian Stark ,  Samuel Weisbrod

IPC分类号： C07K16/22 ,  C07K1/107 ,  C07K1/18 ,  A61K47/54 ,  A61K47/64

摘要： 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.

公开(公告)号：US09855340B2

公开(公告)日：2018-01-02

申请号：US14434585

申请日：2013-10-08

申请人： Ascendis Pharma A/S

发明人： Harald Rau ,  Tobias Voigt ,  Burkhardt Laufer ,  Nicola Bisek ,  Franziska Hahn ,  Thomas Knappe

IPC分类号： A61K47/48 ,  C08G83/00 ,  C08J3/075 ,  C08G65/332 ,  A61K31/4188 ,  C08G69/44 ,  C08G69/48 ,  C08G65/333 ,  C08F2/22

CPC分类号： A61K47/60 ,  A61K31/4188 ,  A61K47/557 ,  A61K47/59 ,  A61K47/645 ,  A61K47/6845 ,  A61K47/6849 ,  A61K47/6903 ,  C08F2/22 ,  C08G65/332 ,  C08G65/3322 ,  C08G65/33337 ,  C08G65/33389 ,  C08G69/44 ,  C08G69/48 ,  C08G83/004 ,  C08G83/006 ,  C08G2210/00 ,  C08J3/075 ,  C08J2300/202 ,  C08J2371/02 ,  C08J2400/202 ,  C08J2471/02 ,  C08L2203/02

摘要： 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.