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1. 发明申请

WO2011131731A1 CYCLOPEPTIDE DERIVATIVES AND USES THEREOF 审中-公开
标题翻译：环孢菌素衍生物及其用途
公开(公告)号：WO2011131731A1
公开(公告)日：2011-10-27
申请号：PCT/EP2011/056354
申请日：2011-04-20
申请人： TECHNISCHE UNIVERSITÄT MÜNCHEN , DEMMER, Oliver , KESSLER, Horst , WESTER, Hans-Jürgen , SCHOTTELIUS, Margret , DIJKGRAAF, Ingrid , BUCK, Andreas, Konrad
发明人： DEMMER, Oliver , KESSLER, Horst , WESTER, Hans-Jürgen , SCHOTTELIUS, Margret , DIJKGRAAF, Ingrid , BUCK, Andreas, Konrad
IPC分类号： A61K51/08 , C07K7/64
CPC分类号： C07K7/64 , A61K51/08 , A61K51/088
摘要： The invention relates to compounds having a structure according to formula (I), cyclo[(R 1 )Xaa 1 B-(R 2 )Xaa 2 (R3)Xaa 3 -(R 4 )Xaa 4 ], or pharmaceutically acceptable salts thereof, wherein Xaa 1 and Xaa 3 are independently of each other, a natural or unnatural amino acid, preferably with Xaa 1 and Xaa 3 being, independently of each other, an amino acid comprising an aromatic moiety in its side chain, Xaa 2 is a natural or unnatural basic amino acid, Xaa 4 is glycine or a D-amino acid, R 1 , R 2 , R 3 and R 4 are independently of each other H or methyl, B is an amino acid group having a structure according to formula (II), -N(-Q)-CHR 5 -C(=0)-, wherein R 5 is selected from the group consisting of H, optionally substituted alkyl, optionally substituted aryl and optionally substituted heteroaryl, and a moiety L, and wherein Q is a group being sterically more demanding than a methyl group. The invention also relates to compositions, methods and uses related to said compounds.
摘要翻译：本发明涉及具有式（I），环[（R1）Xaa1B-（R2）Xaa2（R3）Xaa3-（R4）Xaa4]结构的化合物或其药学上可接受的盐，其中Xaa1和Xaa3独立地为彼此为天然或非天然氨基酸，优选Xaa1和Xaa3彼此独立地为包含其侧链中芳族部分的氨基酸，Xaa2为天然或非天然碱性氨基酸，Xaa4为甘氨酸或D - 氨基酸，R 1，R 2，R 3和R 4彼此独立地为H或甲基，B为具有式（II）结构的氨基酸，-N（-Q）-CHR 5 -C（= O） - ，其中R 5选自H，任选取代的烷基，任选取代的芳基和任选取代的杂芳基，以及部分L，并且其中Q是在空间上比甲基更苛刻的基团。本发明还涉及与所述化合物相关的组合物，方法和用途。

2. 发明申请

WO2011131735A1 CYCLOPENTAPEPTIDE DERIVATIVES AND USES THEREOF 审中-公开
标题翻译：环磷酰胺衍生物及其用途
公开(公告)号：WO2011131735A1
公开(公告)日：2011-10-27
申请号：PCT/EP2011/056358
申请日：2011-04-20
申请人： TECHNISCHE UNIVERSITÄT MÜNCHEN , DEMMER, Oliver , KESSLER, Horst , WESTER, Hans-Jürgen , SCHOTTELIUS, Margret , DIJKGRAAF, Ingrid , BUCK, Andreas, Konrad
发明人： DEMMER, Oliver , KESSLER, Horst , WESTER, Hans-Jürgen , SCHOTTELIUS, Margret , DIJKGRAAF, Ingrid , BUCK, Andreas, Konrad
IPC分类号： A61K51/08 , C07K7/64
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 Xaa 1 to Xaa 4 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 18 F-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。

3. 发明申请

WO02085418A3 TC AND RE LABELER RADIOACTIVE GLYCOSYLATED OCTREOTIDE DERIVATIVES 审中-公开
标题翻译： TC和RE标签放射性糖苷化衍生物
公开(公告)号：WO02085418A3
公开(公告)日：2003-09-12
申请号：PCT/US0212565
申请日：2002-04-23
申请人： MALLINCKRODT INC , WESTER HANS-JURGEN , SCHOTTELIUS MARGRET , SCHWAIGER MARKUS
发明人： WESTER HANS-JURGEN , SCHOTTELIUS MARGRET , SCHWAIGER MARKUS
IPC分类号： A61K51/00 , A61K51/08 , C07B59/00 , C07K2/00
CPC分类号： A61K51/088 , A61K51/083
摘要： Improved sst-receptor binding peptidic ligands for diagnostic and therapeutic applications in nuclear medicine are provided. The improved ligands contain either natural or unnatural amino acids or peptidomimetic structures that are modified at either the N-terminal or the C-terminal end or at both termini, a carbohydrate unit and a chelator or prosthetic group to provide a complexation of a radioisotope binding or holding the radioisotope. The sst- or SSTR- receptor binding peptidic ligands may also contain one or more multifunctional linker units optionally coupling the peptide, and/or the sugar moiety and/or the chelator and/or the prosthetic group. Upon administering the ligand to a mammal through the blood system the ligand provides improved availability, clearance kinetics, sst-receptor targeting and internalization over the non-carbohydrated ligands.
摘要翻译：提供了用于核医学诊断和治疗应用的改善的sst-受体结合肽配体。改进的配体含有天然或非天然氨基酸或在N-末端或C-末端或两末端修饰的拟肽结构，碳水化合物单元和螯合剂或修饰基团以提供放射性同位素结合的络合或持有放射性同位素。 Sst-或SSTR-受体结合肽配体还可以含有一个或多个任选地连接肽和/或糖部分和/或螯合剂和/或假体基团的多官能连接基团。通过血液系统向哺乳动物施用配体时，配体提供了非碳水化合物配体上改善的可用性，清除动力学，sst受体靶向和内化。

4. 发明申请

WO2002085418A2 TC AND RE LABELER RADIOACTIVE GLYCOSYLATED OCTREOTIDE DERIVATIVES 审中-公开
标题翻译： TC和RE标签放射性糖苷化衍生物
公开(公告)号：WO2002085418A2
公开(公告)日：2002-10-31
申请号：PCT/US2002/012565
申请日：2002-04-23
申请人： MALLINCKRODT INC. , WESTER, Hans-Jurgen , SCHOTTELIUS, Margret , SCHWAIGER, Markus
发明人： WESTER, Hans-Jurgen , SCHOTTELIUS, Margret , SCHWAIGER, Markus
IPC分类号： A61K51/08
CPC分类号： A61K51/088 , A61K51/083
摘要： Improved sst-receptor binding peptidic ligands for diagnostic and therapeutic applications in nuclear medicine are provided. The improved ligands contain either natural or unnatural amino acids or peptidomimetic structures that are modified at either the N-terminal or the C-terminal end or at both termini, a carbohydrate unit and a chelator or prosthetic group to provide a complexation of a radioisotope binding or holding the radioisotope. The sst- or SSTR- receptor binding peptidic ligands may also contain one or more multifunctional linker units optionally coupling the peptide, and/or the sugar moiety and/or the chelator and/or the prosthetic group. Upon administering the ligand to a mammal through the blood system the ligand provides improved availability, clearance kinetics, sst-receptor targeting and internalization over the non-carbohydrated ligands.
摘要翻译：提供了用于核医学诊断和治疗应用的改善的sst-受体结合肽配体。改进的配体含有天然或非天然氨基酸或在N-末端或C-末端或两末端修饰的拟肽结构，碳水化合物单元和螯合剂或修饰基团以提供放射性同位素结合的络合或持有放射性同位素。 Sst-或SSTR-受体结合肽配体还可以含有一个或多个任选地连接肽和/或糖部分和/或螯合剂和/或假体基团的多官能连接基团。通过血液系统向哺乳动物施用配体时，配体提供了非碳水化合物配体上改善的可用性，清除动力学，sst受体靶向和内化。

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