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公开(公告)号:US20140296150A1
公开(公告)日:2014-10-02
申请号:US14238437
申请日:2012-08-10
申请人: Ulrich Hersel , Harald Rau , Torben Lessmann , Nicola Bisek , Guillaume Maitro , Kennett Sprogøe , Thomas Wegge , Oliver Keil , Joachim Zettler
发明人: Ulrich Hersel , Harald Rau , Torben Lessmann , Nicola Bisek , Guillaume Maitro , Kennett Sprogøe , Thomas Wegge , Oliver Keil , Joachim Zettler
IPC分类号: A61K47/48
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)。
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公开(公告)号:US20120184489A1
公开(公告)日:2012-07-19
申请号:US13387940
申请日:2010-07-30
申请人: Harald Rau , Felix Cleeman , Ulrich Hersel , Silvia Kaden-Vagt , Torben Lessman
发明人: Harald Rau , Felix Cleeman , Ulrich Hersel , Silvia Kaden-Vagt , Torben Lessman
IPC分类号: A61K38/28 , A61P3/10 , A61P3/04 , B32B1/08 , C07K14/62 , A61M5/31 , B32B5/16 , C07K17/08 , A61P9/12
CPC分类号: A61K38/28 , A61K47/60 , A61K47/6903 , C07K14/62 , Y10T428/13 , Y10T428/2982
摘要: The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof comprising an insulin linker conjugate D-L, wherein D represents the insulin moiety; and -L is a non-biologically active linker moiety -L1 represented by formula (I), wherein the dashed line indicates the attachment to one of the amino groups of the insulin by forming an amide bond. The invention further relates to pharmaceutical compositions comprising said prodrugs as well as their use as a medicament for treating or preventing diseases or disorders which can be treated by insulin.
摘要翻译: 本发明涉及其前体药物或其药学上可接受的盐,其包含胰岛素连接物缀合物D-L,其中D表示胰岛素部分; 并且-L是由式(I)表示的非生物活性连接体部分-L1,其中虚线表示通过形成酰胺键与胰岛素的一个氨基的连接。 本发明还涉及包含所述前体药物的药物组合物及其作为治疗或预防可由胰岛素治疗的疾病或病症的药物的用途。
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公开(公告)号:US20080241102A1
公开(公告)日:2008-10-02
申请号:US10594097
申请日:2005-03-22
申请人: Ulrich Hersel , Harald Rau , Robert Schnepf , Dirk Vetter , Thomas Wegge
发明人: Ulrich Hersel , Harald Rau , Robert Schnepf , Dirk Vetter , Thomas Wegge
IPC分类号: A61K38/21 , C07C271/10 , A61K31/27 , C07H21/04 , A61K38/28 , C07K2/00 , A61K31/7052 , A61K38/02
CPC分类号: A61K47/48246 , A61K47/58 , A61K47/60 , A61K47/61 , A61K47/64 , A61K47/643 , A61K47/6903 , C07C69/96 , C07D207/46 , C07D401/12 , C07K14/00 , C07K14/61 , C07K14/62
摘要: A cascade carrier linked prodrug is described which comprises a biologically active moiety and a masking group having at least one nucleophile and being distinct from the carrier.
摘要翻译: 描述了级联载体连接的前药,其包含生物活性部分和具有至少一个亲核体并且与载体不同的掩蔽基团。
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公开(公告)号:US20070020224A1
公开(公告)日:2007-01-25
申请号:US10574213
申请日:2004-10-01
申请人: Dirk Vetter , Ulrich Hersel , Harald Rau , Robert Schnepf , Thomas Wegge
发明人: Dirk Vetter , Ulrich Hersel , Harald Rau , Robert Schnepf , Thomas Wegge
IPC分类号: A61K48/00 , A61K38/50 , A61K38/48 , A61K38/19 , A61K38/18 , A61K38/28 , A61K31/785 , C12N9/02 , C12N9/24 , C12N9/48
CPC分类号: B82Y5/00 , A61K47/56 , A61K47/6949 , Y10S977/70 , Y10S977/702 , Y10S977/705 , Y10S977/754
摘要: The application relates to a composition comprising a hyperbranched polymer attached to a core and a biologically active moiety. The biologically active moiety is attached to the core by means of a substantially non-enzymatically cleavable linker L. The composition can be used to deliver the biologically active moiety to its target.
摘要翻译: 本申请涉及包含连接到核和生物活性部分的超支化聚合物的组合物。 生物活性部分通过基本上非酶切割的接头L连接到芯上。该组合物可用于将生物活性部分递送至其靶。
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公开(公告)号:US10729778B2
公开(公告)日:2020-08-04
申请号:US15418180
申请日:2017-01-27
申请人: Ulrich Hersel , Harald Rau , Torben Lessmann , Nicola Bisek , Guillaume Maitro , Kennett Sprogøe , Thomas Wegge , Oliver Keil , Joachim Zettler
发明人: Ulrich Hersel , Harald Rau , Torben Lessmann , Nicola Bisek , Guillaume Maitro , Kennett Sprogøe , Thomas Wegge , Oliver Keil , Joachim Zettler
摘要: 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).
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公开(公告)号:US09272048B2
公开(公告)日:2016-03-01
申请号:US12990101
申请日:2009-04-29
申请人: Harald Rau , Susanne Kinderman , Torben Lebmann , Grethe Norskov Rasmussen , Ulrich Hersel , Thomas Wegge , Kennett Sprogoe
发明人: Harald Rau , Susanne Kinderman , Torben Lebmann , Grethe Norskov Rasmussen , Ulrich Hersel , Thomas Wegge , Kennett Sprogoe
摘要: A chemically modified human Growth Hormone (rhGH) prepared by attaching a transient linker which comprises a polyethylene glycol. The chemically modified protein may have a much longer lasting rhGH activity than that of the unmodified rhGH, enabling reduced dose and scheduling opportunities and the modified rhGH may not cause lipoatrophy. Also includes methods of use for the treatment and/or prevention of diseases or disorders in which use of growth hormone is beneficial.
摘要翻译: 通过连接包含聚乙二醇的瞬时接头制备的化学修饰的人生长激素(rhGH)。 化学修饰的蛋白质可能具有比未修饰的rhGH更持久的rhGH活性,能够减少剂量和调度机会,并且修饰的rhGH可能不引起脂肪萎缩。 还包括用于治疗和/或预防使用生长激素有益的疾病或病症的方法。
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公开(公告)号:US09138462B2
公开(公告)日:2015-09-22
申请号:US13387940
申请日:2010-07-30
申请人: Harald Rau , Felix Cleemann , Ulrich Hersel , Silvia Kaden-Vagt , Torben Lessman , Thomas Wegge
发明人: Harald Rau , Felix Cleemann , Ulrich Hersel , Silvia Kaden-Vagt , Torben Lessman , Thomas Wegge
CPC分类号: A61K38/28 , A61K47/60 , A61K47/6903 , C07K14/62 , Y10T428/13 , Y10T428/2982
摘要: The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof comprising an insulin linker conjugate D-L1, wherein D is insulin; and -L1 is: wherein the dashed line indicates the attachment to one of the amino groups of the insulin by forming an amide bond. The invention further relates to pharmaceutical compositions comprising said prodrugs as well as their use as a medicament for treating or preventing diseases or disorders which can be treated by insulin.
摘要翻译: 本发明涉及其前体药物或其药学上可接受的盐,其包含胰岛素连接体缀合物D-L1,其中D为胰岛素; -L1为:其中虚线表示通过形成酰胺键与胰岛素的一个氨基的连接。 本发明还涉及包含所述前体药物的药物组合物及其作为治疗或预防可由胰岛素治疗的疾病或病症的药物的用途。
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公开(公告)号:US09133276B2
公开(公告)日:2015-09-15
申请号:US13822170
申请日:2011-09-16
申请人: Felix Cleemann , Ulrich Hersel , Torben Lessman , Harald Rau
发明人: Felix Cleemann , Ulrich Hersel , Torben Lessman , Harald Rau
CPC分类号: C07K17/08 , A61K47/60 , A61K47/65 , A61K47/6903
摘要: The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof comprising an exendin linker conjugate D-L1, wherein D represents an exendin moiety; and -L1 is represented by formula (I), wherein the dashed line indicates the attachment to one of the amino groups of the exendin moiety by forming an amide bond. The invention further relates to pharmaceutical compositions comprising said prodrugs as well as their use as a medicament for treating or preventing diseases or disorders which can be treated by exendin.
摘要翻译: 本发明涉及前药或其药学上可接受的盐,其包含毒蜥外泌肽连接体缀合物D-L1,其中D表示毒蜥外泌肽部分; -L1由式(I)表示,其中虚线表示通过形成酰胺键与毒蜥蜴蛋白部分的一个氨基的连接。 本发明进一步涉及包含所述前体药物的药物组合物及其作为治疗或预防可被毒蜥外泌肽治疗的疾病或病症的药物的用途。
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公开(公告)号:US20140296257A1
公开(公告)日:2014-10-02
申请号:US14237429
申请日:2012-08-10
申请人: Ulrich Hersel , Guillaume Maitro , Harald Rau , Dirk Vetter
发明人: Ulrich Hersel , Guillaume Maitro , Harald Rau , Dirk Vetter
IPC分类号: A61K31/519 , A61K31/428 , 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是支化核心,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的药物组合物,它们作为药物或诊断用途以及治疗方法。
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公开(公告)号:US08450097B2
公开(公告)日:2013-05-28
申请号:US12967285
申请日:2010-12-14
申请人: Dirk Vetter , Ulrich Hersel , Harald Rau , Robert Schnepf , Thomas Wegge
发明人: Dirk Vetter , Ulrich Hersel , Harald Rau , Robert Schnepf , Thomas Wegge
CPC分类号: B82Y5/00 , A61K47/56 , A61K47/6949 , Y10S977/70 , Y10S977/702 , Y10S977/705 , Y10S977/754
摘要: The application relates to a composition comprising a hyperbranched polymer attached to a core and a biologically active moiety. The biologically active moiety is attached to the core by means of a substantially non-enzymatically cleavable linker L. The composition can be used to deliver the biologically active moiety to its target.
摘要翻译: 本申请涉及包含连接到核和生物活性部分的超支化聚合物的组合物。 生物活性部分通过基本上非酶切割的接头L连接到芯上。该组合物可用于将生物活性部分递送至其靶。
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