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1. 发明公开

EP3600441A1 HYDROGEL CROSS-LINKED HYALURONIC ACID PRODRUG COMPOSITIONS AND METHODS 审中-实审转让
公开(公告)号：EP3600441A1
公开(公告)日：2020-02-05
申请号：EP18716079.1
申请日：2018-03-22
申请人： Genentech, Inc. , Ascendis Pharma A/S
发明人： STARK, Sebastian , KNAPPE, Thomas , RAU, Harald , BISEK, Nicola , LAUFER, Burkhardt , WEISBROD, Samuel , VOIGT, Tobias , FUH, Germaine , KOENIG, Patrick , LEE, Chingwei Vivian , YADAV, Daniela Bumbaca
IPC分类号： A61K47/61 , A61K47/69

2. 发明授权

EP2906617B1 HYDROGEL PRODRUGS 有权转让
公开(公告)号：EP2906617B1
公开(公告)日：2018-03-14
申请号：EP13773790.4
申请日：2013-10-08
申请人： Ascendis Pharma A/S
发明人： RAU, Harald , VOIGT, Tobias , LAUFER, Burkhardt , BISEK, Nicola , HAHN, Franziska , KNAPPE, Thomas
IPC分类号： C08J3/24 , C08G83/00 , A61K47/10 , C08J3/075 , C08F2/32 , C08G65/32 , C08G65/332
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.

3. 发明公开

EP2988732A1 MODIFIED HYDROGELS 有权
标题翻译：改性凝胶
公开(公告)号：EP2988732A1
公开(公告)日：2016-03-02
申请号：EP14721238.5
申请日：2014-04-16
申请人： Ascendis Pharma A/S
发明人： HERSEL, Ulrich , RAU, Harald , LAUFER, Burkhardt , ZETTLER, Joachim , REIMANN, Romy
IPC分类号： A61K9/10 , A61K47/10 , A61K47/48 , C08G83/00 , C08J3/075 , A61K38/20 , A61K38/28
CPC分类号： A61K47/48215 , A61K9/06 , A61K38/2006 , A61K38/28 , A61K47/10 , A61K47/48784 , A61K47/60 , A61K47/6903 , C08G65/48 , C08J3/075
摘要： The present invention relates to a process for the preparation of a hydrogel suitable as carrier in a hydrogel-linked prodrug, to hydrogels obtainable from said process, the use of such hydrogel as a carrier in a hydrogel-linked prodrug and to hydrogel-linked prodrugs comprising a covalently conjugated hydrogel of the present invention. The hydrogel prodrug carrier has a reduced drug loading on the outside of the hydrogel carrier. This is achieved by reducing the number of functional groups of the hydrogel, in particular those at its surface.

4. 发明公开

EP2928501A1 CARRIER-LINKED PROSTANOID PRODRUGS 审中-公开
标题翻译： TRÄGERVERKNÜPFTEPROSTANOID-PRODRUGS
公开(公告)号：EP2928501A1
公开(公告)日：2015-10-14
申请号：EP13799603.9
申请日：2013-12-06
申请人： Ascendis Pharma A/S
发明人： RAU, Harald , MAITRO, Guillaume , HERSEL, Ulrich , KEIL, Oliver , WEGGE, Thomas
IPC分类号： A61K47/48 , A61P9/12
摘要： The present invention relates to carrier-linked prostanoid prodrugs of formula (I) Z1—(X0-L0-PG0)y (I), wherein Z1, X0, L0, PG0 and y have the meaning as indicated in the description and claims; pharmaceutically acceptable salts thereof and pharmaceutical compositions comprising the same. It further relates to their use as medicaments, especially for treating, controlling, delaying or preventing pulmonary arterial hypertension.
摘要翻译：本发明涉及式（I）Z1-（X0-L0-PG0）y（I）的载体连接前列腺素前体药物，其中Z1，X0，L0，PG0和y具有说明书和权利要求书中指出的含义; 其药学上可接受的盐和包含其的药物组合物。它还涉及它们作为药物的用途，特别是用于治疗，控制，延迟或预防肺动脉高血压。

5. 发明公开

EP2741781A1 CARRIER-LINKED TREPROSTINIL PRODRUGS 审中-公开
标题翻译： TRÄGERVERKNÜPFTETREPROSTINIL-PRODRUGS
公开(公告)号：EP2741781A1
公开(公告)日：2014-06-18
申请号：EP12748194.3
申请日：2012-08-10
申请人： Ascendis Pharma A/S
发明人： HERSEL, Ulrich , RAU, Harald , LESSMANN, Torben , BISEK, Nicola , MAITRO, Guillaume , SPROGØE, Kennett , WEGGE, Thomas , ZETTLER, Joachim , KEIL, Oliver
IPC分类号： A61K47/48 , A61P11/00
CPC分类号： A61K47/48253 , A61K47/60 , A61K47/641 , A61K47/645
摘要： 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).
摘要翻译：本发明涉及包含共价曲前列腺素载体缀合物的前药或其药学上可接受的盐以及包含所述化合物的药物组合物。这些化合物可以用作药物，特别是可以通过曲前列素治疗的疾病或病症，例如肺动脉高压（PAH）。

6. 发明授权

EP3054981B1 PROTECTING GROUP COMPRISING A PURIFICATION TAG 有权
公开(公告)号：EP3054981B1
公开(公告)日：2020-07-29
申请号：EP14781865.2
申请日：2014-10-07
申请人： Ascendis Pharma A/S
发明人： RAU, Harald , BISEK, Nicola , KNAPPE, Thomas , REIMANN, Romy , STARK, Sebastian , WEISBROD, Samuel
IPC分类号： C07K1/107 , C07K1/18 , A61K47/54 , A61K47/64 , C07K16/22

7. 发明授权

EP3054982B1 HYDROGEL-LINKED IL-1RA PRODRUG 有权
公开(公告)号：EP3054982B1
公开(公告)日：2019-05-01
申请号：EP14784022.7
申请日：2014-10-07
申请人： Ascendis Pharma A/S
发明人： RAU, Harald , ZETTLER, Joachim , HERSEL, Ulrich , KALUZA, Nora , KRUSCH, Mathias , VOIGT, Tobias
IPC分类号： A61K47/60 , A61K47/69 , A61P19/02

8. 发明授权

EP2237799B1 PRODRUG COMPRISING A SELF-CLEAVABLE LINKER 有权
公开(公告)号：EP2237799B1
公开(公告)日：2019-04-10
申请号：EP09706788.8
申请日：2009-01-30
申请人： Ascendis Pharma A/S
发明人： CLEEMANN, Felix , HERSEL, Ulrich , KADEN, Silvia , RAU, Harald , WEGGE, Thomas
IPC分类号： A61K38/17 , A61K38/18 , A61K38/26 , A61K31/553 , A61K47/65 , A61K47/60

9. 发明授权

EP2525830B1 DIPEPTIDE-BASED PRODRUG LINKERS FOR ALIPHATIC AMINE-CONTAINING DRUGS 有权
标题翻译： DIPEPTIDBASIERTE前体药物留给阿明脂肪族中药
公开(公告)号：EP2525830B1
公开(公告)日：2016-05-11
申请号：EP11700673.4
申请日：2011-01-21
申请人： Ascendis Pharma A/S
发明人： RAU, Harald , LEßMANN, Torben
IPC分类号： A61K47/48 , C07K1/107 , C07K1/13
CPC分类号： C07K1/13 , A61K47/48215 , A61K47/48338 , A61K47/60 , A61K47/65 , C07K1/1077

10. 发明公开

EP2741779A1 HIGH-LOADING WATER-SOLUBLE CARRIER-LINKED PRODRUGS 审中-实审
标题翻译： HOCHBELADENEWASSERLÖSLICHETRÄGERSTOFFVERNETZTEPRODRUGS
公开(公告)号：EP2741779A1
公开(公告)日：2014-06-18
申请号：EP12748192.7
申请日：2012-08-10
申请人： Ascendis Pharma A/S
发明人： HERSEL, Ulrich , MAITRO, Guillaume , RAU, Harald , VETTER, Dirk
IPC分类号： A61K47/48
CPC分类号： A61K31/519 , A61K31/428 , A61K47/60
摘要： The present invention relates to water-soluble carrier-linked prodrugs of formula (I), wherein B, A and Hyp form the carrier, B is a branching core, each A is independently a poly(ethylene glycol)-based polymeric chain, each Hyp is independently a branched moiety, each SP is independently a spacer moiety, each L is independently a reversible prodrug linker moiety, each D is independently a biologically active moiety, each x is independently 0 or 1, each m is independently an integer of from 2 to 64, n is an integer from 3 to 32; or the pharmaceutically acceptable salt thereof. It further relates to pharmaceutical compositions comprising said water-soluble carrier-linked prodrugs, their use as medicament or diagnostic, and methods of treatment.
摘要翻译：本发明涉及式（I）的水溶性载体连接的前药，其中B，A和Hyp形成载体，B是分支核心，每个A独立地是基于聚（乙二醇）的聚合物链，每个 Hyp独立地是支链部分，每个SP独立地是间隔基部分，每个L独立地是可逆的前药接头部分，每个D独立地是生物活性部分，每个x独立地为0或1，每个m独立地为 2〜64，n为3〜32的整数，或其药学上可接受的盐。它还涉及包含所述水溶性载体连接的前药，其作为药物或诊断用途的药物组合物和治疗方法。

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