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1. 发明申请

WO2012107577A1 HYDROPHOBIC MODIFIED PEPTIDES FOR LIVER SPECIFIC DIAGNOSIS 审中-公开
标题翻译：用于肝脏特异性诊断的疏水性修饰肽
公开(公告)号：WO2012107577A1
公开(公告)日：2012-08-16
申请号：PCT/EP2012/052343
申请日：2012-02-10
申请人： RUPRECHT-KARLS-UNIVERSITÄT HEIDELBERG , MIER, Walter , URBAN, Stephan , MEHRLE, Stefan , HABERKORN, Uwe , MUELLER, Thomas , ASKOXYLAKIS, Vasileios
发明人： MIER, Walter , URBAN, Stephan , MEHRLE, Stefan , HABERKORN, Uwe , MUELLER, Thomas , ASKOXYLAKIS, Vasileios
IPC分类号： A61K49/00 , A61K49/08 , A61K51/08 , C07K14/005
CPC分类号： A61K51/088 , A61K38/00 , A61K49/0056 , A61K49/085 , A61K49/14 , C07K14/005 , C07K2319/50 , C12N7/00 , C12N2730/10122 , Y02A50/409 , Y02A50/411 , Y02A50/423 , Y02A50/463
摘要： The present invention relates to hydrophobic modified peptides for the specific delivery of labels to the liver, preferably to hepatocytes, in vitro as well as in vivo . The present invention relates to pharmaceutical compositions comprising said hydrophobic modified peptide(s) and the label(s) to be specifically delivered to the liver. The present invention furthermore relates to the diagnostic use of the inventive hydrophobic modified peptides as well as to a method for the diagnosis of liver diseases or disorders.
摘要翻译：本发明涉及用于在体外和体内特异性递送给肝脏，优选肝细胞的疏水性修饰肽。本发明涉及包含所述疏水性修饰肽和要特异性递送至肝脏的标签的药物组合物。本发明还涉及本发明的疏水性修饰肽的诊断用途以及用于诊断肝脏疾病或病症的方法。

2. 发明申请

WO2012107579A1 HYDROPHOBIC MODIFIED PEPTIDES AND THEIR USE FOR LIVER SPECIFIC TARGETING 审中-公开
标题翻译：疏水性改性肽及其用于肝脏特异性靶向
公开(公告)号：WO2012107579A1
公开(公告)日：2012-08-16
申请号：PCT/EP2012/052349
申请日：2012-02-10
申请人： RUPRECHT-KARLS-UNIVERSITÄT HEIDELBERG , MIER, Walter , URBAN, Stephan , MEHRLE, Stefan , HABERKORN, Uwe
发明人： MIER, Walter , URBAN, Stephan , MEHRLE, Stefan , HABERKORN, Uwe
IPC分类号： A61K49/00 , A61K49/08 , A61K51/08 , C07K14/005 , A61K47/48
CPC分类号： C07K7/08 , A61K47/542 , A61K47/64 , A61K51/0402 , A61K51/088 , C07K14/00
摘要： The present invention relates to hydrophobic modified peptides for the specific delivery of compounds to the liver, preferably to hepatocytes, in vitro as well as in vivo. The present invention relates to pharmaceutical compositions comprising said hydrophobic modified peptide(s) and the compound(s) to be specifically delivered to the liver. The present invention furthermore relates to the use of the inventive hydrophobic modified peptides as well as to a method for the prevention and/or treatment of liver diseases or disorders.
摘要翻译：本发明涉及用于在体外和体内将化合物特异性递送至肝脏，优选肝细胞的疏水性修饰肽。本发明涉及包含所述疏水性修饰肽和要特异性递送至肝脏的化合物的药物组合物。本发明还涉及本发明的疏水性修饰肽的用途以及预防和/或治疗肝脏疾病或病症的方法。

3. 发明申请

WO2012016713A1 TUMOUR TARGETING WITH POLYPEPTIDES 审中-公开
标题翻译：肿瘤定位与多糖
公开(公告)号：WO2012016713A1
公开(公告)日：2012-02-09
申请号：PCT/EP2011/003946
申请日：2011-08-05
申请人： RUPRECHT-KARLS-UNIVERSITÄT HEIDELBERG , DEUTSCHES KREBSFORSCHUNGSZENTRUM , ASKOXYLAKIS, Vasileios , HABERKORN, Uwe , ALTMANN, Annette , MIER, Walter , DEBUS, Jürgen
发明人： ASKOXYLAKIS, Vasileios , HABERKORN, Uwe , ALTMANN, Annette , MIER, Walter , DEBUS, Jürgen
IPC分类号： G01N33/574
CPC分类号： C07K7/08 , A61K38/00 , G01N33/573 , G01N33/57484 , G01N2333/988
摘要： The present invention relates to polypeptides which can be used to target tumours by binding to carbonic anhydrase IX (Ca9), in particular for diagnosis, prognosis and/or treatment of tumours. Further, it relates to methods of identifying such polypeptides.
摘要翻译：本发明涉及可用于通过结合碳酸酐酶IX（Ca9），特别是用于诊断，预后和/或治疗肿瘤来靶向肿瘤的多肽。此外，它涉及鉴定这些多肽的方法。

4. 发明申请

WO2007088129A2 COMPOUNDS USEFUL FOR THE AT LEAST BI-MODAL DIAGNOSTIC IMAGING 审中-公开
标题翻译：适用于至少双模式诊断成像的化合物
公开(公告)号：WO2007088129A2
公开(公告)日：2007-08-09
申请号：PCT/EP2007/050664
申请日：2007-01-23
申请人： DKFZ DEUTSCHES KREBSFORSCHUNGSZENTRUM , RUPRECHT-KARLS-UNIVERSITÄT-HEIDELBERG , KIESSLING, Fabian , BEIJER, Barbro , SCHULZ, Ralf , SEMMLER, Wolfhard , MIER, Walter , WÄNGLER, Björn
发明人： KIESSLING, Fabian , BEIJER, Barbro , SCHULZ, Ralf , SEMMLER, Wolfhard , MIER, Walter , WÄNGLER, Björn
IPC分类号： A61K49/00 , A61K49/08 , A61K51/04
CPC分类号： A61K49/0032 , A61K49/005 , A61K49/085 , A61K49/10 , A61K51/0478 , A61K51/0482 , C09B23/0066 , C09B23/086
摘要： The present invention relates to compounds of formula (I), Ch-L-D (I), wherein D is a cyanine dye, L is a covalent bond or a linker and Ch is a metal chelating moiety or a pharmaceutically acceptable salt thereof, which can be used for the preparation of a contrast agent for the at least bi-modal diagnostic imaging of a biological system as well as a contrast agent prepared from these compounds, their use in multi-modal diagnostic imaging and imaging methods.
摘要翻译：本发明涉及式（I）化合物，Ch-LD（I），其中D为花青染料，L为共价键或连接基，Ch为金属螯合部分或其药学上可接受的盐，其可以用于制备用于生物系统的至少双模态诊断成像的造影剂以及由这些化合物制备的造影剂，其用于多模式诊断成像和成像方法。

5. 发明申请

WO2009092612A1 HYDROPHOBIC MODIFIED PRES-DERIVED PEPTIDES OF HEPATITIS B VIRUS (HBV) AND THEIR USE AS VEHICLES FOR THE SPECIFIC DELIVERY OF COMPOUNDS TO THE LIVER 审中-公开
标题翻译：乙型肝炎病毒（HBV）的疏水性改性预先导入的化合物及其作为特定化合物向肝脏递送的车辆
公开(公告)号：WO2009092612A1
公开(公告)日：2009-07-30
申请号：PCT/EP2009/000477
申请日：2009-01-26
申请人： UNIVERSITÄTSKLINIKUM HEIDELBERG , MIER, Walter , HABERKORN, Uwe , URBAN, Stephan
发明人： MIER, Walter , HABERKORN, Uwe , URBAN, Stephan
IPC分类号： C07K14/02 , A61P33/02 , A61P31/20 , A61P35/04 , A61K38/00
CPC分类号： C07K14/005 , A61K38/162 , A61K2039/6075 , C07K2319/033 , C12N2730/10122 , C12N2810/6036 , Y02A50/41 , Y02A50/412 , Y02A50/423 , Y02A50/463
摘要： The present invention relates to hydrophobic modified preS-derived peptides of hepatitis B virus (HBV) which are versatile vehicles for the specific delivery of compounds to the liver, preferably to hepatocytes, in vitro as well as in vivo. Any kind of compound, but in particular drugs, such as interferons, viral reverse transcriptase inhibitors or core assembly inhibitors, and/or labels can be specifically targeted to the liver and so be enriched in the liver. This liver targeting can further be used for the targeted diagnosis, prevention and/or treatment of liver diseases or disorders, such as hepatitis, malaria, hepatocellular carcinoma (HCC), as well as for the prevention of HAV, HBV, HCV and/or HDV infection. The present invention relates to pharmaceutical compositions comprising said hydrophobic modified preS-derived peptide(s) and the compound(s) to be specifically delivered to the liver. The present invention furthermore relates to a method for the combined treatment of a liver disease and the prevention of HAV, HBV, HCV and/or HDV infection. The present invention relates also to the use of the preS-derived peptides in gene therapy and the delivery of immunogenic epitopes for hepatocyte-mediated antigen presentation to activate liver-directed immunological responses.
摘要翻译：本发明涉及乙型肝炎病毒（HBV）的疏水性修饰的preS-衍生肽，其是用于在体外和体内特异性递送化合物至肝脏，优选肝细胞的通用载体。任何种类的化合物，特别是药物，例如干扰素，病毒逆转录酶抑制剂或核心组装抑制剂和/或标记物可以特异性靶向肝脏，因此富含肝脏。该肝靶向可进一步用于肝病，疟疾，肝细胞癌（HCC）等肝病或疾病的靶向诊断，预防和/或治疗，以及预防HAV，HBV，HCV和/或 HDV感染。本发明涉及包含所述疏水性修饰的preS-衍生的肽和要特异性递送至肝脏的化合物的药物组合物。本发明还涉及一种联合治疗肝脏疾病和预防HAV，HBV，HCV和/或HDV感染的方法。本发明还涉及preS衍生的肽在基因治疗中的用途，以及用于肝细胞介导的抗原呈递的免疫原性表位的递送以激活肝脏免疫应答。

6. 发明申请

WO2005044842A1 PEPTIDE USEFUL FOR DIAGNOSIS AND THERAPY OF TUMORS 审中-公开
标题翻译：有用的诊断和治疗肿瘤的肽
公开(公告)号：WO2005044842A1
公开(公告)日：2005-05-19
申请号：PCT/EP2004/011681
申请日：2004-10-15
申请人： DEUTSCHES KREBSFORSCHUNGSZENTRUM STIFTUNG DES ÖFFENTLICHEN RECHTS , RUPRECHT-KARLS-UNIVERSITÄT , ZITZMANN, Sabine , MIER, Walter , PESCHKE, Sigrid , HABERKORN, Uwe , MAHMUT, Miriam
发明人： ZITZMANN, Sabine , MIER, Walter , PESCHKE, Sigrid , HABERKORN, Uwe , MAHMUT, Miriam
IPC分类号： C07K7/08
CPC分类号： A61K38/00 , C07K2319/01
摘要： Described are the peptide motif FRPNRAQDYNTN and related motifs characterizing peptides which are capable of specifically binding to tumors, e.g., a prostate tumor. Moreover, various diagnostic and therapeutic uses of peptides containing said motif are described.
摘要翻译：描述了肽基序FRPNRAQDYNTN和表征能够特异性结合肿瘤例如前列腺肿瘤的肽的相关基序。此外，描述了含有所述基序的肽的各种诊断和治疗用途。

7. 发明申请

WO2011009539A1 ε-POLYLYSIN-KONJUGATE UND DEREN VERWENDUNG 审中-公开
标题翻译： E-聚赖氨酸结合物及其用途
公开(公告)号：WO2011009539A1
公开(公告)日：2011-01-27
申请号：PCT/EP2010/004198
申请日：2010-07-09
申请人： MERCK PATENT GMBH , KUEBELBECK, Armin , LARBIG, Gregor , MIER, Walter , BEIJER, Barbro , HABERKORN, Uwe
发明人： KUEBELBECK, Armin , LARBIG, Gregor , MIER, Walter , BEIJER, Barbro , HABERKORN, Uwe
IPC分类号： A61K47/48 , A61K49/08 , A61K51/04
CPC分类号： A61K47/48315 , A61K47/542 , A61K47/645 , A61K49/085 , A61K49/146 , A61K51/0497 , A61K51/088 , C07K7/00 , C07K7/06 , C07K7/08 , C07K14/00
摘要： Die vorliegende Erfindung betrifft ε-Polylysin-Konjugate, insbesondere Konjugate von ε-Polylysin mit Carboxylgruppen tragenden Verbindungen, sowie deren Herstellung und Verwendung für das Targeting der Niere.
摘要翻译：本发明涉及的电子聚赖氨酸缀合物，尤其是E-聚赖氨酸与带羧基的化合物的缀合物，以及它们的生产和使用用于靶向肾脏。

8. 发明申请

WO2018065085A1 COATING OF NANOPARTICLE SURFACES WITH CYCLOPEPTIDES FOR IMPROVING DELIVERY OF AGENTS VIA THE ORAL ROUTE 审中-公开
标题翻译：具有环肽的纳米颗粒表面涂层用于改善通过口服途径给药的作用
公开(公告)号：WO2018065085A1
公开(公告)日：2018-04-12
申请号：PCT/EP2017/001119
申请日：2017-09-19
申请人： RUPRECHT-KARLS-UNIVERSITÄT HEIDELBERG
发明人： UHL, Philipp , MIER, Walter , HABERKORN, Uwe , SAUTER, Max
IPC分类号： A61K9/00 , A61K9/19 , A61K9/51
摘要： The present invention relates to a surface-coated nanoparticle comprising biodegradable polymer chains and cyclopeptides, wherein the cyclopeptides are covalently attached to the biodegradable polymer chains forming the nanoparticle, thereby coating the surface of the nanoparticle. The present invention further relates to the use of said surface-coated nanoparticle as a capsule for an agent for improving the oral delivery thereof. In another aspect, the present invention relates to the surface-coated nanoparticle for use in the treatment or prevention of a disorder or disease in a patient, wherein the treatment or prevention is achieved by mucosal uptake of the surface-coated nanoparticle via the oral route.
摘要翻译：本发明涉及包含生物可降解聚合物链和环肽的表面涂布纳米粒子，其中环肽共价连接至形成纳米粒子的生物可降解聚合物链，由此涂布纳米粒子的表面。本发明进一步涉及所述表面涂覆的纳米颗粒作为用于改善其口服递送的药剂的胶囊的用途。另一方面，本发明涉及用于治疗或预防患者病症或疾病的表面包被的纳米颗粒，其中所述治疗或预防通过口服途径通过粘膜摄取表面包被的纳米颗粒来实现

9. 发明申请

WO2017102906A1 CYCLIC NTCP-TARGETING PEPTIDES AND THEIR USES AS ENTRY INHIBITORS 审中-公开
标题翻译：循环的NTCP-靶向肽及其作为进入抑制剂的用途
公开(公告)号：WO2017102906A1
公开(公告)日：2017-06-22
申请号：PCT/EP2016/081117
申请日：2016-12-15
申请人： RUPRECHT-KARLS-UNIVERSITÄT HEIDELBERG
发明人： URBAN, Stephan , NI, Yi , MIER, Walter
IPC分类号： A61K38/12 , C07K7/50 , C07K7/64 , C07K14/005 , A61K51/08 , A61K47/50 , A61K51/04 , A61P31/20
CPC分类号： A61K51/088 , A61K38/00 , A61K49/0056 , C07K7/06 , C07K7/08 , C07K7/50 , C07K7/64 , C07K14/005 , C12N2730/10111 , C12N2730/10141 , Y02A50/409 , Y02A50/411 , Y02A50/423 , Y02A50/463
摘要： The present invention relates to cyclic NTCP targeting peptides which are preS-derived peptides of hepatitis B virus (HBV). The present invention further relates to pharmaceutical compositions comprising at least one cyclic peptide. The present invention further relates to medical uses of said cyclic peptides and the pharmaceutical compositions, such as in the diagnosis, prevention and/or treatment of a liver disease or condition, and/or in the inhibition of HBV and/or HDV infection. The present invention further relates to methods of diagnosis, prevention and/or treatment of a liver disease or condition and/or the inhibition of HBV and/or HDV infection.
摘要翻译：本发明涉及作为乙型肝炎病毒（HBV）的preS衍生肽的环状NTCP靶向肽。本发明进一步涉及包含至少一种环肽的药物组合物。本发明进一步涉及所述环肽和药物组合物的医疗用途，例如用于诊断，预防和/或治疗肝脏疾病或病症，和/或用于抑制HBV和/或HDV感染。本发明还涉及诊断，预防和/或治疗肝脏疾病或病症和/或抑制HBV和/或HDV感染的方法。

10. 发明申请

WO2020165409A1 PROSTATE SPECIFIC MEMBRANE ANTIGEN (PSMA) LIGANDS COMPRISING AN AMYLASE CLEAVABLE LINKER 审中-公开
公开(公告)号：WO2020165409A1
公开(公告)日：2020-08-20
申请号：PCT/EP2020/053891
申请日：2020-02-14
申请人： DEUTSCHES KREBSFORSCHUNGSZENTRUM , RUPRECHT-KARLS-UNIVERSITÄT HEIDELBERG
发明人： EDER, Matthias , KOPKA, Klaus , SCHÄFER, Martin , BAUDER-WUEST, Ulrike , HABERKORN, Uwe , KLIEM, Hans-Christian , MIER, Walter , LINDNER, Thomas
IPC分类号： A61K51/04 , A61P35/00
摘要： In particular, the present invention relates to a PSMA binding ligand comprising an oligosaccharide building block which comprises a bond being cleavable by alpha-amylase. Typically, this PSMA binding ligand further comprises a PSMA binding motif Q and a chelator residue A, wherein the PSMA binding motif Q and the chelator residue A are preferably linked via at least one linker A-L AQ -Q comprising the oligosaccharide building block, the PSMA binding ligand thus preferably having the structure (I) or a pharmaceutically acceptable salt or solvate thereof

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