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1.发明授权TYROSINE BASED LINKERS FOR THE RELEASABLE CONNECTION OF PEPTIDES 有权TYROSINBASIERTE连接器ZURLÖSBARENVERBINDUNG VON PEPTIDEN
公开(公告)号：EP2773375B1
公开(公告)日：2017-02-08
申请号：EP12779063.2
申请日：2012-10-29
发明人： FLAMME, Ingo , KÖBBERLING, Johannes , LERCHEN, Hans-Georg , GRIEBENOW, Nils , SCHOHE-LOOP, Rudolf , WITTROCK, Sven , KRENZ, Ursula
CPC分类号： C07K5/0815 , A61K38/05 , A61K38/06 , A61K47/50 , A61K47/65 , C07K5/0215 , C07K5/06086
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2.发明公开POLYETHYLENE GLYCOL BASED PRODRUG OF ADRENOMEDULLIN AND USE THEREOF 有权ADRENOMEDULLIN-PRODRUG AUF POLYETHYLINGLYKOLBASIS UND VERWENDUNG DAVON
公开(公告)号：EP3075395A1
公开(公告)日：2016-10-05
申请号：EP15192265.5
申请日：2012-10-30
发明人： FLAMME, Ingo , KÖBBERLING, Johannes , LERCHEN, Hans-Georg , GRIEBENOW, Nils , SCHOHE-LOOP, Rudolf , WITTROCK, Sven , KÖLLNBERGER, Maria , WUNDER, Frank , REDLICH, Gordon , KNORR, Andreas , MARLEY, July , PRITCHARD, Iain
CPC分类号： C07K5/06017 , A61K9/007 , A61K38/22 , A61K45/06 , A61K47/60 , C07K5/02 , C07K5/06078 , C07K14/575
摘要： The invention relates medicaments comprising novel polyethylene glycol (PEG) based prodrugs of Adrenomedullin, or one of the salts thereof, solvates thereof or the solvates of salts thereof, in combination with an inert nontoxic pharmaceutically suitable excipient, wherein the medicament is in a pharmaceutical form for inhalation, its use for treatment and/or prevention of diseases, especially of cardiovascular, edematous and/or inflammatory disorders, to specific PEG-adrenomedullin prodrugs and its synthesis intermediates.
摘要翻译： 本发明涉及包含新型聚乙二醇（PEG）基于前体药物的肾上腺髓质素或其盐之一，其溶剂合物或其盐的溶剂合物与惰性无毒药学上合适的赋形剂组合的药物，其中药物为药物形式 用于吸入，其用于治疗和/或预防特定PEG-肾上腺髓质素前体药物及其合成中间体的疾病，特别是心血管，水肿和/或炎症性疾病的疾病。
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公开(公告)号：EP2773375A1
公开(公告)日：2014-09-10
申请号：EP12779063.2
申请日：2012-10-29
发明人： FLAMME, Ingo , KÖBBERLING, Johannes , LERCHEN, Hans-Georg , GRIEBENOW, Nils , SCHOHE-LOOP, Rudolf , WITTROCK, Sven , KRENZ, Ursula
CPC分类号： C07K5/0815 , A61K38/05 , A61K38/06 , A61K47/50 , A61K47/65 , C07K5/0215 , C07K5/06086
摘要： The invention relates to novel tyrosine based linkers that allow the releasable connection of peptides or proteins with other molecular entities, e.g. polyethylene glycol, to processes for their preparation and their use for preparing medicaments for the treatment and/or prophylaxis of diseases.
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公开(公告)号：EP3075395B1
公开(公告)日：2017-11-22
申请号：EP15192265.5
申请日：2012-10-30
发明人： FLAMME, Ingo , KÖBBERLING, Johannes , LERCHEN, Hans-Georg , GRIEBENOW, Nils , SCHOHE-LOOP, Rudolf , WITTROCK, Sven , KÖLLNBERGER, Maria , WUNDER, Frank , REDLICH, Gorden , KNORR, Andreas , MARLEY, July , PRITCHARD, Iain
CPC分类号： C07K5/06017 , A61K9/007 , A61K38/22 , A61K45/06 , A61K47/60 , C07K5/02 , C07K5/06078 , C07K14/575
摘要： The invention relates medicaments comprising novel polyethylene glycol (PEG) based prodrugs of Adrenomedullin, or one of the salts thereof, solvates thereof or the solvates of salts thereof, in combination with an inert nontoxic pharmaceutically suitable excipient, wherein the medicament is in a pharmaceutical form for inhalation, its use for treatment and/or prevention of diseases, especially of cardiovascular, edematous and/or inflammatory disorders, to specific PEG-adrenomedullin prodrugs and its synthesis intermediates.
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5.发明授权POLYETHYLENE GLYCOL BASED PRODRUG OF ADRENOMEDULLIN AND USE THEREOF 有权西班牙语VERWENDUNG的ADRENOMEDULLIN-PRODRUG AUF POLYETHYLINGLYKOLBASIS
公开(公告)号：EP2773376B1
公开(公告)日：2016-01-13
申请号：EP12783566.8
申请日：2012-10-30
发明人： FLAMME, Ingo , KÖBBERLING, Johannes , LERCHEN, Hans-Georg , GRIEBENOW, Nils , SCHOHE-LOOP, Rudolf , WITTROCK, Sven , KÖLLNBERGER, Maria , WUNDER, Frank , REDLICH, Gorden , KNORR, Andreas , MARLEY, July , PRITCHARD, Iain
CPC分类号： C07K5/06017 , A61K9/007 , A61K38/22 , A61K45/06 , A61K47/60 , C07K5/02 , C07K5/06078 , C07K14/575
摘要： The invention relates medicaments comprising novel polyethylene glycol (PEG) based prodrugs of Adrenomedullin, or one of the salts thereof, solvates thereof or the solvates of salts thereof, in combination with an inert nontoxic pharmaceutically suitable excipient, wherein the medicament is in a pharmaceutical form for inhalation, its use for treatment and/or prevention of diseases, especially of cardiovascular, edematous and/or inflammatory disorders, to specific PEG-adrenomedullin prodrugs and its synthesis intermediates.
摘要翻译： 本发明涉及包含新型聚乙二醇（PEG）基于前体药物的肾上腺髓质素或其盐之一，其溶剂化物或其盐的溶剂合物与惰性无毒药学上合适的赋形剂组合的药物，其中药物为药物形式 用于吸入，其用于治疗和/或预防特定PEG-肾上腺髓质素前体药物及其合成中间体的疾病，特别是心血管，水肿和/或炎症性疾病的疾病。
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公开(公告)号：EP2773376A1
公开(公告)日：2014-09-10
申请号：EP12783566.8
申请日：2012-10-30
发明人： FLAMME, Ingo , KÖBBERLING, Johannes , LERCHEN, Hans-Georg , GRIEBENOW, Nils , SCHOHE-LOOP, Rudolf , WITTROCK, Sven , KÖLLNBERGER, Maria , WUNDER, Frank , REDLICH, Gorden , KNORR, Andreas , MARLEY, July , PRITCHARD, Iain
CPC分类号： C07K5/06017 , A61K9/007 , A61K38/22 , A61K45/06 , A61K47/60 , C07K5/02 , C07K5/06078 , C07K14/575
摘要： The invention relates medicaments comprising novel polyethylene glycol (PEG) based prodrugs of Adrenomedullin, or one of the salts thereof, solvates thereof or the solvates of salts thereof, in combination with an inert nontoxic pharmaceutically suitable excipient, wherein the medicament is in a pharmaceutical form for inhalation, its use for treatment and/or prevention of diseases, especially of cardiovascular, edematous and/or inflammatory disorders, to specific PEG-adrenomedullin prodrugs and its synthesis intermediates.
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公开(公告)号：EP3086814B1
公开(公告)日：2020-06-24
申请号：EP14833342.0
申请日：2014-12-10
发明人： LERCHEN, Hans-Georg , WITTROCK, Sven , GRIEBENOW, Nils , STELTE-LUDWIG, Beatrix , SOMMER, Anette , BERNDT, Sandra , MAHLERT, Christoph , LOBELL, Mario , TERJUNG, Carsten , GREVEN, Simone , CANCHO GRANDE, Yolanda
IPC分类号： A61K47/22 , C07D233/64 , C07D207/335 , A61K35/00 , A61K47/68 , A61K31/40 , A61K31/415 , A61P35/00
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8.发明公开ANTIKÖRPER-WIRKSTOFF-KONJUGATE (ADCS) VON KSP-INHIBITOREN MIT ANTI-CD123-ANTIKÖRPERN 审中-公开具有抗CD123抗体的KSP抑制剂的抗体 - 活性偶联物（ADCS）
公开(公告)号：EP3313524A1
公开(公告)日：2018-05-02
申请号：EP16736011.4
申请日：2016-06-20
发明人： LERCHEN, Hans-Georg , REBSTOCK, Anne-Sophie , CANCHO-GRANDE, Yolanda , WITTROCK, Sven , STELTE-LUDWIG, Beatrix , MAHLERT, Christoph , GREVEN, Simone , MÄRSCH, Stephan , KIRCHHOFF, Dennis
IPC分类号： A61P35/00
CPC分类号： A61K47/6803 , A61K31/40 , A61K31/4025 , A61K47/6849 , A61K47/6851 , A61K2039/505 , A61K2039/572 , A61P35/00 , C07K16/2866 , C07K2317/24 , C07K2317/56 , C07K2317/565 , C07K2317/73 , C07K2317/76 , C07K2317/92
摘要： The invention relates to novel antibody drug conjugates (ADCs), active metabolites of said ADCs, to methods for producing said ADCs, to the use of said ADCs for the treatment and/or prevention of diseases, and to the use of said ADCs for the production of medicaments for the treatment and/or prevention of diseases, in particular hyperproliferative and angiogenic diseases, such as cancer diseases. Such treatments can be effected as monotherapy or else in combination with other medicaments or further therapeutic measures.
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9.发明公开ANTIKÖRPER-WIRKSTOFF-KONJUGATE (ADCS) VON KSP-INHIBITOREN MIT AGLYCOSYLIERTEN ANTI-TWEAKRANTIKÖRPERN 审中-公开ANTIKÖRPER-WIRKSTOFF-KONJUGATE（ADCS）VON KSP -INHIBITOREN MIT AGLYCOSYLIERTEN ANTI-TWEAKRANTIKÖRPERN
公开(公告)号：EP3233127A1
公开(公告)日：2017-10-25
申请号：EP15816395.6
申请日：2015-12-10
发明人： LERCHEN, Hans-Georg , WITTROCK, Sven , CANCHO GRANDE, Yolanda , STELTE-LUDWIG, Beatrix , SOMMER, Anette , BERNDT, Sandra , MAHLERT, Christoph , REBSTOCK, Anne-Sophie , TERJUNG, Carsten , GREVEN, Simone
CPC分类号： A61K47/6803 , A61K31/03 , A61K31/131 , A61K31/16 , A61K31/4025 , A61K31/4192 , A61K31/497 , A61K38/00 , A61K47/6851
摘要： The aim of the present invention is to provide substances which show an apoptotic effect after administration in a relatively low concentration and can thus be useful for cancer therapy. To achieve this aim, the invention provides conjugates of an aglycosylated or aglycosyl anti-TWEAKR antibody with KSP inhibitors of formula (I), wherein one or more of the compounds of formula (I) is or are connected to the antibody via a linker L. Aglycosylated antibodies are antibodies which have no glycans at the preserved N-binding site in the CH2 domain of the Fc region. The antibody is preferably a human, humanised or chimeric monoclonal antibody. More preferably, the antibody is an anti-TWEAKR antibody, which specifically binds to the amino acid D in position 47 (D47) of TWEAKR (SEQ ID NO:169), in particular the anti-TWEAKR antibody TPP-2658.
摘要翻译： 本发明的目的是提供以较低浓度给药后显示细胞凋亡效应的物质，因此可用于癌症治疗。 为了实现该目的，本发明提供了无糖基化或无糖基化抗TWEAKR抗体与式（I）的KSP抑制剂的缀合物，其中一种或多种式（I）化合物通过接头L与抗体连接 。糖基化抗体是在Fc区的CH2结构域的保存的N-结合位点不含聚糖的抗体。 该抗体优选是人类，人源化或嵌合单克隆抗体。 更优选地，抗体是抗TWEAKR抗体，其特异性结合TWEAKR（SEQ ID NO：169）的位置47（D47）中的氨基酸D，特别是抗TWEAKR抗体TPP-2658。
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10.发明公开
公开(公告)号：EP3919518A1
公开(公告)日：2021-12-08
申请号：EP21186955.7
申请日：2017-06-08
发明人： LERCHEN, Hans-Georg , REBSTOCK, Anne-Sophie , CANCHOGRANDE, Yolanda , WITTROCK, Sven , STELTE-LUDWIG, Beatrix , KIRCHHOFF, Dennis , MAHLERT, Christoph , GREVEN, Simone , MÄRSCH, Stephan
IPC分类号： C07K16/28 , A61K47/68 , A61P35/00 , C07D207/335 , C07D233/64
摘要： The invention relates to specific Antibody-Drug-Conjugates (ADCs) with KSP inhibitors and anti-CD 123-antibodies, to the use of these conjugates for the treatment and/or prophylaxis of diseases and to the use of these conjugates for preparing medicaments for treatment and/or prevention of diseases, in particular hyperproliferative and/or angiogenic disorders such as, for example, cancer diseases. Such treatments can be carried out as monotherapy or else in combination with other medicaments or further therapeutic measures.
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