公开(公告)号：US09266924B2

公开(公告)日：2016-02-23

申请号：US13641947

申请日：2011-04-20

申请人： Oliver Demmer ,  Horst Kessler ,  Hans-Jürgen Wester ,  Margret Schottelius ,  Ingrid Dijkgraaf ,  Andreas Konard Buck

发明人： Oliver Demmer ,  Horst Kessler ,  Hans-Jürgen Wester ,  Margret Schottelius ,  Ingrid Dijkgraaf ,  Andreas Konard Buck

IPC分类号： A61K51/00 ,  A61M36/14 ,  C07K7/64 ,  A61K51/08

CPC分类号： C07K7/64 ,  A61K51/088

摘要： The present invention, among others, relates to a compound having a structure according to formula (I) or a pharmaceutically acceptable salt thereof, wherein Xaa1 to Xaa4 are independently of each other, an optionally N-alkylated natural or unnatural amino acid, R is H or methyl, L is a linker moiety, Ar is a spacer comprising an aromatic moiety, and D comprises, preferably is i) a combination of an organic complexation agent and a detectable label; or ii) a detectable label, an organic complexation agent or an active substance, said active substance particularly being selected from cytotoxic agents, lipids, sugars, sugar conjugates, sugar derivatives, proteins and combinations thereof, with the proviso that -L-Ar-D does not comprise a 18F-benzoyl residue.

摘要翻译： 本发明尤其涉及具有式（I）结构的化合物或其药学上可接受的盐，其中Xaa1至Xaa4彼此独立，任选N-烷基化天然或非天然氨基酸，R为 H或甲基，L是连接体部分，Ar是包含芳族部分的间隔基，D包括，优选i）有机络合剂和可检测标记的组合; 或ii）可检测标记，有机络合剂或活性物质，所述活性物质特别选自细胞毒性剂，脂质，糖，糖结合物，糖衍生物，蛋白质及其组合，条件是-L-Ar- D不包含18 F-苯甲酰残基。

公开(公告)号：US20130129622A1

公开(公告)日：2013-05-23

申请号：US13641947

申请日：2011-04-20

申请人： Oliver DEMMER ,  Horst KESSLER ,  Hans-Jürgen WESTER ,  Margret SCHOTTELIUS ,  Ingrid DIJKGRAAF ,  Andreas Konard BUCK

发明人： Oliver DEMMER ,  Horst KESSLER ,  Hans-Jürgen WESTER ,  Margret SCHOTTELIUS ,  Ingrid DIJKGRAAF ,  Andreas Konard BUCK

IPC分类号： C07K7/64 ,  A61K51/08

CPC分类号： C07K7/64 ,  A61K51/088

摘要： The present invention, among others, relates to a compound having a structure according to formula (I) or a pharmaceutically acceptable salt thereof, wherein Xaa1 to Xaa4 are independently of each other, an optionally N-alkylated natural or unnatural amino acid, R is H or methyl, L is a linker moiety, Ar is a spacer comprising an aromatic moiety, and D comprises, preferably is i) a combination of an organic complexation agent and a detectable label; or ii) a detectable label, an organic complexation agent or an active substance, said active substance particularly being selected from cytotoxic agents, lipids, sugars, sugar conjugates, sugar derivatives, proteins and combinations thereof, with the proviso that -L-Ar-D does not comprise a 18F-benzoyl residue.

摘要翻译： 本发明尤其涉及具有式（I）结构的化合物或其药学上可接受的盐，其中Xaa1至Xaa4彼此独立，任选N-烷基化天然或非天然氨基酸，R为 H或甲基，L是连接体部分，Ar是包含芳族部分的间隔基，D包括，优选i）有机络合剂和可检测标记的组合; 或ii）可检测标记，有机络合剂或活性物质，所述活性物质特别选自细胞毒性剂，脂质，糖，糖结合物，糖衍生物，蛋白质及其组合，条件是-L-Ar- D不包含18 F-苯甲酰残基。