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41. 发明公开

EP3054981A1 PROTECTING GROUP COMPRISING A PURIFICATION TAG 有权
标题翻译：麻醉麻省理工学院
公开(公告)号：EP3054981A1
公开(公告)日：2016-08-17
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： A61K47/48
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.
摘要翻译：本发明涉及包含保护基部分 - 标签部分缀合物的化合物，由这种纯化方法获得的纯化方法和单缀合物。

42. 发明公开

EP2906245A1 DIAGNOSIS, PREVENTION AND TREATMENT OF DISEASES OF THE JOINT 有权
标题翻译： DIAGNOSE，VORBEUGUNG UND BEHANDLUNG VON GELENKERKRANKUNGEN
公开(公告)号：EP2906245A1
公开(公告)日：2015-08-19
申请号：EP13773786.2
申请日：2013-10-08
申请人： Ascendis Pharma A/S
发明人： VETTER, Dirk , HERSEL, Ulrich , SPROGØE, Kennett , KALUZA, Nora , KEIL, Oliver , MAITRO, Guillaume , RAU, Harald
IPC分类号： A61K47/48 , A61P19/02
CPC分类号： A61K47/48215 , A61K9/0019 , A61K38/2006 , A61K47/60 , A61K47/6903 , C07K14/545
摘要： The present invention relates to apolymeric prodrug for use in the treatment, prevention and/or diagnosis a disease of the joint and pharmaceutical compositions and medical devices comprising said polymeric prodrugs.
摘要翻译：本发明涉及用于治疗，预防和/或诊断关节疾病和药物组合物的聚合前药，以及包含所述聚合物前药的医疗装置。

43. 发明公开

EP2596805A1 Prodrug comprising a drug linker conjugate 有权
标题翻译： Prodrug beinhaltend ein Wirkstoff-Linker Konjugat
公开(公告)号：EP2596805A1
公开(公告)日：2013-05-29
申请号：EP13156350.4
申请日：2009-01-30
申请人： Ascendis Pharma A/S
发明人： Cleemann, Felix , Hersel, Ulrich , Kaden-Vagt, Silvia , Rau, Harald , Wegge, Thomas
IPC分类号： A61K47/48
CPC分类号： A61K47/48215 , A61K31/553 , A61K38/1709 , A61K38/18 , A61K38/26 , A61K47/54 , A61K47/542 , A61K47/545 , A61K47/60 , A61K47/65
摘要： The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof comprising a drug linker conjugate D-L, wherein
-D is an amine containing biologically active moiety; and
-L is a
non-biologically active linker moiety -L 1 represented by formula (I),

wherein the dashed line indicates the attachment to the amine of the biologically active moiety and wherein R 1 , R 1a , R 2 , R 2a , R 3 , R 3a , X, X 1 , X 2 , X 3 have the meaning as indicated in the description and the claims and wherein L 1 is substituted with one to four groups L 2 -Z and optionally further substituted, provided that the hydrogen marked with the asterisk in formula (I) is not replaced by a substituent; wherein L 2 is a single chemical bond or a spacer; and Z is a carrier group and wherein D-H is a polypeptide selected from the group of polypeptides consisting of exendins, glucagon, glucagon-like peptides and insulins. The invention also relates pharmaceutical composition comprising said prodrugs and their use as medicaments.
摘要翻译：本发明涉及包含药物连接物缀合物D-L的前药或其药学上可接受的盐，其中-D是含胺的生物活性部分; 和-L是由式（I）表示的非生物活性的连接体部分-L 1，其中虚线表示与生物活性部分的胺的连接，并且其中R 1，R 1a，R 2，R 2a， R 3，R 3a，X，X 1，X 2，X 3具有如说明书和权利要求书中所示的含义，并且其中L 1被一至四个L 2 -Z基团任选地进一步取代，条件是用式（I）中的星号标记的氢不被取代基取代; 其中L 2是单个化学键或间隔基; 并且Z是载体基团，并且其中D-H是选自由毒蜥外泌肽，胰高血糖素，胰高血糖素样肽和胰岛素组成的多肽组的多肽。本发明还涉及包含所述前药的药物组合物及其作为药物的用途。

44. 发明公开

EP2525831A1 CARRIER-LINKED CARBAMATE PRODRUG LINKERS 有权
标题翻译： TRÄGERSTOFFVERKNÜPFTECARBAMAT-PRODRUG-LINKER
公开(公告)号：EP2525831A1
公开(公告)日：2012-11-28
申请号：EP11702163.4
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
CPC分类号： A61K47/48215 , A61K47/60 , A61K47/65 , A61K47/6903
摘要： The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof, comprising a drug linker conjugate D-L, wherein D being a biologically active moiety containing an aromatic hydroxyl group is conjugated to one or more polymeric carriers via secondary carbamate-containing linkers L. Such carrier-linked prodrugs achieve drug releases with therapeutically useful half-lives. The invention also relates to pharmaceutical compositions comprising said prodrugs and their use as medicaments.
摘要翻译：本发明涉及其前体药物或其药学上可接受的盐，其包含药物接头缀合物DL，其中D是含有芳族羟基的生物活性部分，通过含二氨基甲酸酯的接头L与一个或多个聚合物载体缀合。载体连接的前药实现具有治疗有用的半衰期的药物释放。本发明还涉及包含所述前体药物及其用作药物的药物组合物。

45. 发明公开

EP2525830A1 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：EP2525830A1
公开(公告)日：2012-11-28
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
摘要： The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof, comprising a drug linker conjugate D-L, wherein D being a biologically active moiety containing an aliphatic amine group is conjugated to one or more polymeric carriers via dipeptide-containing linkers L. Such carrier-linked prodrugs achieve drug releases with therapeutically useful half-lives. The invention also relates to pharmaceutical compositions comprising said prodrugs and their use as medicaments.

46. 发明公开

EP2525829A1 DIPEPTIDE-BASED PRODRUG LINKERS FOR AROMATIC AMINE-CONTAINING DRUGS 审中-公开
标题翻译： DIPEPTIDBASIERTE PRODRUG-LINKERFÜRAROMATISCHE AMINHALTIGE ARZNEIMITTEL
公开(公告)号：EP2525829A1
公开(公告)日：2012-11-28
申请号：EP11700672.6
申请日：2011-01-21
申请人： Ascendis Pharma A/S
发明人： VETTER, Dirk , RAU, Harald
IPC分类号： A61K47/48
CPC分类号： A61K47/48338 , A61K31/553 , A61K38/26 , A61K47/48215 , A61K47/48784 , A61K47/60 , A61K47/65 , A61K47/6903 , A61M5/19
摘要： The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof, comprising a drug linker conjugate D-L, wherein D being a biologically active moiety containing an aromatic amine group is conjugated to one or more polymeric carriers via dipeptide-containing linkers. Such carrier-linked prodrugs achieve drug releases with therapeutically useful half-lives. The invention also relates to pharmaceutical compositions comprising said prodrugs and their use as medicaments.
摘要翻译：本发明涉及其前体药物或其药学上可接受的盐，其包含药物连接物缀合物DL，其中D是含有脂族胺基团的生物活性部分通过含二肽的接头L与一个或多个聚合物载体缀合。连接的前药实现具有治疗有用的半衰期的药物释放。本发明还涉及包含所述前体药物及其用作药物的药物组合物。

47. 发明公开

EP2485767A1 CARRIER LINKED PALIPERIDONE PRODRUGS 审中-公开
标题翻译：载体连接PALIPERIDONE PRODRUGS
公开(公告)号：EP2485767A1
公开(公告)日：2012-08-15
申请号：EP10760719.4
申请日：2010-10-06
申请人： Ascendis Pharma A/S
发明人： HERSEL, Ulrich , RAU, Harald , MAITRO, Guillaume , WEGGE, Thomas
IPC分类号： A61K47/48
CPC分类号： A61K47/60
摘要： The present invention relates to prodrugs or a pharmaceutically acceptable salt thereof comprising a covalent Paliperidone carrier conjugate of formula (I) wherein Z
0 is defined in the description and the claims as well as pharmaceutical composition comprising said compounds. The compounds are usefull as medicament, especially for diseases or disorders which can be treated by Paliperidone.
摘要翻译：本发明涉及包含其中Z 0如说明书和权利要求书中所定义的式（I）的共价帕潘立酮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。这些化合物作为药物是有用的，特别是对于可以用帕潘立酮治疗的疾病或病症。

48. 发明公开

EP2485712A1 SUBCUTANEOUS PALIPERIDONE COMPOSITION 审中-公开
标题翻译：皮下注射PALPERIDONE组合物
公开(公告)号：EP2485712A1
公开(公告)日：2012-08-15
申请号：EP10768897.0
申请日：2010-10-06
申请人： Ascendis Pharma A/S
发明人： SPROGØE, Kennett , HERSEL, Ulrich , RAU, Harald , MAITRO, Guillaume , WEGGE, Thomas
IPC分类号： A61K9/06 , A61K9/00 , A61K47/48 , A61K31/519
CPC分类号： A61K9/0019 , A61K9/0024 , A61K9/06 , A61K47/60
摘要： The present invention relates to pharmaceutical composition for subcutaneous injection comprising a paliperidone compound wherein the composition releases the paliperidone with an immediate onset of action and continuously for at least 3 weeks, and wherein the composition has a pharmacokinetic profile in vivo with substantially no burst release of the paliperidone. The compositios are useful as medicaments for the treatment of psychotic disorders and diseases.
摘要翻译：本发明涉及用于皮下注射的药物组合物，其包含帕潘立酮化合物，其中所述组合物立即释放帕潘立酮并且持续至少3周，并且其中所述组合物在体内具有药代动力学特征，基本上没有突释帕潘立酮。该组合物可用作治疗精神障碍和疾病的药物。

49. 发明公开

EP2459227A1 PRODRUGS CONTAINING AN AROMATIC AMINE CONNECTED BY AN AMIDO BOND TO A LINKER 有权
标题翻译：用约与粘合剂相关的芳香胺的酰胺化合物前药
公开(公告)号：EP2459227A1
公开(公告)日：2012-06-06
申请号：EP10742799.9
申请日：2010-07-30
申请人： Ascendis Pharma A/S
发明人： RAU, Harald , BARON, Julia , HERSEL, Ulrich , KRUSCH, Mathias
IPC分类号： A61K47/48 , A61P25/16
CPC分类号： A61K47/48315 , A61K47/60 , A61K47/61 , A61K47/645 , A61K47/65
摘要： The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof comprising a drug linker conjugate D-L, wherein an aromatic amine containing biologically active moiety is connected (bound) by an amido bound to a linker. The invention also relates to pharmaceutical compositions comprising said prodrugs and their use as medicaments.

50. 发明公开

EP4159258A1 AUTO INJECTOR WITH TEMPERATURE CONTROL 审中-实审
公开(公告)号：EP4159258A1
公开(公告)日：2023-04-05
申请号：EP22191115.9
申请日：2016-12-29
申请人： Ascendis Pharma A/S
发明人： PEDERSEN, Per Møølgaard , JENSEN, Steen , EGESBORG, Henrik , ANDERSEN, Bjørn Knud
IPC分类号： A61M5/20 , A61M5/315 , A61M5/32
摘要： Disclosed is an auto injector and a method for administering a medicament. The auto injector comprising: a housing; a cartridge receiver; a drive module coupled to move a plunger rod configured to move a first stopper; a temperature sensor configured to provide a temperature signal indicative of the temperature of the medicament in the cartridge; a processing unit configured to: receive the temperature signal; control the drive module to move the plunger rod from a first plunger rod position to a mix plunger rod position wherein the movement from the first plunger rod position to the mix plunger rod position is based on the temperature signal.

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