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    Polyamine-substituted ligands for use as contrast agents
    1.
    发明申请
    Polyamine-substituted ligands for use as contrast agents 审中-公开
    用作造影剂的多胺取代的配体

    公开(公告)号：US20070202047A1

    公开(公告)日：2007-08-30

    申请号：US11649503

    申请日：2007-01-04

    申请人： Markus Wolf ,  Ulrike Bauder-Wust ,  Uwe Haberkorn ,  Michael Eisenhut ,  Walter Mier

    发明人： Markus Wolf ,  Ulrike Bauder-Wust ,  Uwe Haberkorn ,  Michael Eisenhut ,  Walter Mier

    IPC分类号： A61K49/10 ,  C07F5/00 ,  C07D257/02

    CPC分类号： C07D257/02 ,  A61K49/103 ,  A61K49/106

    摘要： The present invention relates to a polyamine-substituted ligand for the preparation of a contrast agent derived from a chelating molecule selected from the group consisting of 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) and diethylentriamine-pentaacetic acid (DTPA), wherein at least one of the carboxylic groups of the chelating molecule is reacted with an amine of formula HNR1R2 to form an amide bond, wherein R1, R2 are independently selected from the group consisting of H; (CH2)n—NR3R4; and R5; R3, R4 are independently selected from the group consisting of H; (CH2)m—NR6R7; and (CH2)m-1—CH3; R6, R7 are independently selected from the group consisting of H; and (CH2)o-1—CH3; n, m, o are independently 2, 3, or 4; R5 is of formula and optionally at least one of the carboxylic groups of the chelating molecule is further reacted with a monoalkylamine having 1 to 18 carbon atoms to form an amide bond; provided that at least one of R1, R2 is other than H. Furthermore, the invention relates to contrast agents for magnetic resonance imaging (MRI) comprising said ligands and in-vivo diagnostic methods based on MRI using said contrast agents.

    摘要翻译： 本发明涉及用于制备衍生自螯合分子的造影剂的多胺取代配体，所述螯合分子选自1,4,7,10-四氮杂环十二烷-1,4,7,10-四乙酸（DOTA ）和二乙基三胺五乙酸（DTPA），其中螯合分子的至少一个羧基与式HNR 1 R 2的胺反应形成 酰胺键，其中R 1，R 2，R 2独立地选自H; （CH 2）n - NR 3 - 3 - - - - - - - 和R 5; R 3，R 4，R 4独立地选自H; （CH 2 CH 2）m -NR 6 R 6 R 7 R 7， 和（CH 2 CH 2）m-1 -CH 3 3; R 6，R 7，R 7独立地选自H; 和（CH 2）2 -O-1 -CH 3; n，m，o分别为2,3或4; R 5是下式，并且任选地，螯合分子的至少一个羧酸基团与具有1至18个碳原子的单烷基胺进一步反应以形成酰胺键; 条件是R 1，R 2和R 2中的至少一个不是H.此外，本发明涉及用于包含所述配体的磁共振成像（MRI）的造影剂，并且在 - 使用所述造影剂的基于MRI的体内诊断方法。

    Hydrophobic Modified Pres-Derived Peptides of Hepatitis B Virus (HBV) and Their Use as Vehicles for the Specific Delivery of Compounds to the Liver
    3.
    发明申请
    Hydrophobic Modified Pres-Derived Peptides of Hepatitis B Virus (HBV) and Their Use as Vehicles for the Specific Delivery of Compounds to the Liver 有权
    乙型肝炎病毒（HBV）的疏水性修饰的预先衍生的肽及其作为将化合物特异性递送至肝脏的载体的用途

    公开(公告)号：US20110027183A1

    公开(公告)日：2011-02-03

    申请号：US12864197

    申请日：2009-01-26

    申请人： Walter Mier ,  Uwe Haberkorn ,  Stephan Urban

    发明人： Walter Mier ,  Uwe Haberkorn ,  Stephan Urban

    IPC分类号： A61K49/00 ,  C07K7/06 ,  C07K7/08 ,  C07K14/00 ,  A61K39/395 ,  A61K38/44 ,  A61K35/76 ,  A61K38/21 ,  A61K31/7105 ,  A61K31/7052 ,  A61K39/00 ,  A61K38/16 ,  A61K38/10 ,  A61K38/08 ,  C12N15/63 ,  G01N33/53 ,  A61P1/16 ,  A61P37/04 ,  A61P31/12

    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。

    HYDROPHOBIC MODIFIED PEPTIDES AND THEIR USE FOR LIVER SPECIFIC TARGETING
    4.
    发明申请
    HYDROPHOBIC MODIFIED PEPTIDES AND THEIR USE FOR LIVER SPECIFIC TARGETING 审中-公开
    疏水性改性肽及其用于肝脏特异性靶向

    公开(公告)号：US20140038886A1

    公开(公告)日：2014-02-06

    申请号：US13984694

    申请日：2012-02-10

    申请人： Walter Mier ,  Stephan Urban ,  Stefan Mehrle ,  Uwe Haberkorn

    发明人： Walter Mier ,  Stephan Urban ,  Stefan Mehrle ,  Uwe Haberkorn

    IPC分类号： C07K7/08 ,  A61K47/48 ,  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。

    Labelling compounds for the simple synthesis of 3'-[18F]fluoro-3'-deoxythymidine and a method for the production thereof
    9.
    发明授权
    Labelling compounds for the simple synthesis of 3'-[18F]fluoro-3'-deoxythymidine and a method for the production thereof 有权
    用于简单合成3' - [18 F]氟-3'-脱氧胸苷的化合物及其制备方法

    公开(公告)号：US06891033B2

    公开(公告)日：2005-05-10

    申请号：US10470817

    申请日：2002-01-28

    申请人： Stefan Johannes Martin ,  Joseph Antonius Maria Eisenbarth ,  Ulrike Wagner-Utermann ,  Michael Eisenhut ,  Walter Mier

    发明人： Stefan Johannes Martin ,  Joseph Antonius Maria Eisenbarth ,  Ulrike Wagner-Utermann ,  Michael Eisenhut ,  Walter Mier

    IPC分类号： C07H19/06 ,  A61K31/7072

    CPC分类号： C07H19/06

    摘要： The application relates to compounds that are suitable as labelable precursors for synthesis of 3′-[18F]fluoro-3′-deoxythymidine and that have formula (1), in which R denotes triphenylmethyl, triphenylmethyl substituted in the phenyl group, trialkylmethyl, triphenylsilyl, triphenylsilyl substituted in the phenyl group, or trialkylsilyl, R′ denotes R1—SO2, where R1 is an unsubstituted or substituted C1 to C5 alkyl or an unsubstituted or substituted phenyl, and R″ denotes C2 to C10 alkyloxycarbonyl, with the exception of 3-N-Boc-1-(3-O-nosyl-5-O-trityl-2-deoxy-β-D-lyxofuranosy The application also relates to a method for preparation of these compounds and to the use of the same for synthesis of 3′-[18F]fluoro-3′-deoxythymidine.

    摘要翻译： 本申请涉及适用于合成3' - [16 F]氟-3'-脱氧胸苷的可标记前体的化合物，其具有式（1），其中R表示三苯基甲基，三苯基甲基取代的 在苯基中，三烷基甲基，三苯基甲硅烷基，苯基取代的三苯基甲硅烷基或三烷基甲硅烷基，R'表示R 1 -SO 2 - ，其中R 1， SUP>是未取代或取代的C 1至C 5烷基或未取代或取代的苯基，R“表示C 2至C 除了3-N-Boc-1-（3-O-壬基-5-O-三苯甲基-2-脱氧-β-D-吡喃葡萄糖醛酸之外），除了3-N-Boc- 1-烷氧基羰基外，本申请还涉及 制备这些化合物的方法及其用于合成3' - [[18 F]氟-3'-脱氧胸苷的方法。

    Hydrophobic modified pres-derived peptides of hepatitis B virus (HBV) and their use as HBV and HDV entry inhibitors
    10.
    发明授权
    Hydrophobic modified pres-derived peptides of hepatitis B virus (HBV) and their use as HBV and HDV entry inhibitors 有权
    乙型肝炎病毒（HBV）的疏水性修饰的前衍生肽及其作为HBV和HDV进入抑制剂的用途

    公开(公告)号：US09562076B2

    公开(公告)日：2017-02-07

    申请号：US12863663

    申请日：2009-01-26

    申请人： Walter Mier ,  Stephan Urban

    发明人： Walter Mier ,  Stephan Urban

    IPC分类号： A61K39/29 ,  C07K7/08 ,  C07K14/02 ,  A61P31/20 ,  C07K14/005 ,  A61K47/48 ,  A61K39/12 ,  A61K38/00

    CPC分类号： C07K14/005 ,  A61K38/00 ,  A61K39/12 ,  A61K39/292 ,  A61K47/54 ,  A61K47/542 ,  A61K47/544 ,  A61K47/554 ,  C12N2730/10122 ,  C12N2730/10134

    摘要： The present invention relates to hydrophobic modified preS-derived peptides of hepatitis B virus (HBV) which are derived from a HBV preS consensus sequence and are N-terminal preferably acylated and optional C-terminal modified. These hydrophobic modified preS-derived peptides of HBV are very effective HBV entry inhibitors as well as HDV entry inhibitors and are, thus, suitable for the inhibition of HBV and/or HDV infection, prevention of primary HBV and/or HDV infection as well as treatment of (chronic) hepatitis B and/or D. The present invention further relates to pharmaceutical and vaccine compositions comprising these hydrophobic modified preS-derived peptides of HBV.

    摘要翻译： 本发明涉及衍生自HBV preS共有序列并且N末端优选酰化并任选C末端修饰的乙型肝炎病毒（HBV）的疏水性修饰的preS-衍生肽。 HBV的这些疏水性修饰的preS-衍生肽是非常有效的HBV进入抑制剂以及HDV进入抑制剂，因此适合于抑制HBV和/或HDV感染，预防原发性HBV和/或HDV感染以及 治疗（慢性）乙型肝炎和/或D.本发明还涉及含有这些疏水性修饰的preS-衍生肽的HBV的药物和疫苗组合物。