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    TETRAAZA-CYCLOALKANES BASED LIGANDS AND THEIR USE IN NUCLEAR MEDICINE AND MOLECULAR IMAGING
    1.
    发明申请
    TETRAAZA-CYCLOALKANES BASED LIGANDS AND THEIR USE IN NUCLEAR MEDICINE AND MOLECULAR IMAGING 审中-公开
    基于TETRAAZA-CYCLOALKANES的配体及其在核医学和分子成像中的应用

    公开(公告)号：WO2012150302A1

    公开(公告)日：2012-11-08

    申请号：PCT/EP2012/058130

    申请日：2012-05-03

    申请人： TECHNISCHE UNIVERSITÄT MÜNCHEN ,  NOTNI, Johannes ,  WESTER, Hans-Jürgen

    发明人： NOTNI, Johannes ,  WESTER, Hans-Jürgen

    IPC分类号： A61K103/30 ,  A61K103/34 ,  A61K33/34 ,  A61K49/10 ,  G01N24/00 ,  A61B5/055 ,  C07F9/30

    CPC分类号： C07F9/6524 ,  C07F9/65583 ,  C07F9/65586

    摘要： The present invention relates to the field of nuclear medicine and molecular imaging, i.e. radiopharmaceuticals for imaging and targeted radiotherapy, using metal ion radionuclides or paramagnetic metal ions in combination with chelators that are highly functionalized with peptidic or nonpeptidic ligands, or radioactive or non-radioactive signalling units. Formula (II) wherein m, n, o and p are independently of each other selected from the integers 1 and 2; and R', R", R'" and R'" are independently of each other selected from OH or an amide residue -NR 1 R 2 2 .

    摘要翻译： 本发明涉及核医学和分子成像领域，即用于成像和靶向放射治疗的放射性药物，其使用金属离子放射性核素或顺磁金属离子与用肽或非肽配体高度官能化的螯合剂或放射性或非放射性 信号单元。 式（II）其中m，n，o和p彼此独立地选自整数1和2; 和R'，R“，R”“和R”“彼此独立地选自OH或酰胺残基-NR1R2 2。

    CHELATING AGENT
    3.
    发明申请
    CHELATING AGENT 审中-公开
    电话代理

    公开(公告)号：WO2008068516A1

    公开(公告)日：2008-06-12

    申请号：PCT/GB2007/004733

    申请日：2007-12-10

    申请人： TECHNISCHE UNIVERSITÄT MÜNCHEN ,  JONES, Nicholas, Andrew ,  KNÖR, Sebastian ,  MODLINGER, Armin ,  WESTER, Hans-Jürgen ,  KESSLER, Horst

    发明人： KNÖR, Sebastian ,  MODLINGER, Armin ,  WESTER, Hans-Jürgen ,  KESSLER, Horst

    IPC分类号： C07D257/02 ,  A61K31/395 ,  A61P35/00

    CPC分类号： C07D257/02 ,  Y02P20/55

    摘要： A compound of the formula: wherein R 1 is selected from H, methyl, ethyl, carboxyl protecting groups and hydrophilic moieties, R 2 and R 3 are independently selected from H, methyl, ethyl and carboxyl protecting groups, R 4 is selected from H, methyl, ethyl, hydrophilic moieties and carboxyl protecting groups, and R 5 is an aryl, heteroaryl, alkyl or a combination of these groups and is substituted with a carbonyl group, an aminooxy group or a functional group suitable for participating in a cycloaddition reaction. The compounds of the invention maybe useful as bifunctional chelating agents which allow chemoselective attachment to targeting molecules.

    摘要翻译： 下式的化合物：其中R 1选自H，甲基，乙基，羧基保护基和亲水部分，R 2和R 3 >独立地选自H，甲基，乙基和羧基保护基，R 4选自H，甲基，乙基，亲水部分和羧基保护基，R 5， 是芳基，杂芳基，烷基或这些基团的组合，并被羰基，氨基氧基或适于参与环加成反应的官能团取代。 本发明的化合物可用作双功能螯合剂，其允许化学选择性连接靶向分子。

    CYCLOPENTAPEPTIDE DERIVATIVES AND USES THEREOF
    5.
    发明申请
    CYCLOPENTAPEPTIDE DERIVATIVES AND USES THEREOF 审中-公开
    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。

    CYCLOPEPTIDE DERIVATIVES AND USES THEREOF
    7.
    发明申请
    CYCLOPEPTIDE DERIVATIVES AND USES THEREOF 审中-公开
    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。

    CANCER IMAGING AND TREATMENT
    9.
    发明申请
    CANCER IMAGING AND TREATMENT 审中-公开
    癌症成像和治疗

    公开(公告)号：WO2009027706A2

    公开(公告)日：2009-03-05

    申请号：PCT/GB2008/002950

    申请日：2008-09-01

    申请人： TECHNISCHE UNIVERSITÄT MÜNCHEN ,  JONES, Nicholas, Andrew ,  WESTER, Hans-Jürgen, Peter ,  DIJKGRAAF, Ingrid ,  KESSLER, Horst ,  DEMMER, Oliver

    发明人： WESTER, Hans-Jürgen, Peter ,  DIJKGRAAF, Ingrid ,  KESSLER, Horst ,  DEMMER, Oliver

    IPC分类号： C07K7/64 ,  A61K47/48 ,  A61K51/08 ,  A61P35/00 ,  A61K101/02

    CPC分类号： A61K51/08 ,  A61K47/55 ,  A61K51/088

    摘要： A compound, or a pharmaceutically acceptable salt or ester thereof, comprises the structure: [(P1-S1 j ) p - L - (S2 q -P2) r ] t wherein: P1 and P2, which may be the same or different, are cyclic oligopeptide moieties, at least one of P1 and P2 having the motif B-Arg or B-(Me) Arg within the cyclic moiety, wherein B is a basic amino acid, a derivative thereof, or phenylalanine or a derivative thereof; S1 and S2 are spacer groups, which may be the same or different; L is a linker moiety containing at least two functional groups for attachment of the cyclic oligopeptides or spacer groups; n and q are independently 0 or 1; p and r are independently integers of 1 or more; and t is an integer of 1 or more, provided that, when t, p or r is greater than 1, the cyclic oligopeptide moiety, spacer group and/or the value of j or q may be the same or different between the multiple (P1-S1 j ) moieties or multiple (S2 q -P2) moieties.

    摘要翻译： 化合物或其药学上可接受的盐或酯包括以下结构：[（P1-S1j）p -L-（S2q-P2）r] t其中：P1和P2可以相同或不同，为环状 寡肽部分，在环状部分内具有基序B-Arg或B（Me）Arg的P1和P2中的至少一个，其中B是碱性氨基酸，其衍生物或苯丙氨酸或其衍生物; S1和S2是间隔基，其可以相同或不同; L是含有至少两个用于连接环状寡肽或间隔基团的官能团的连接体部分; n和q独立地为0或1; p和r独立地为1或更大的整数; 并且t为1或更大的整数，条件是当t，p或r大于1时，环状寡肽部分，间隔基团和/或j或q的值可以在多个 P1-S1j）部分或多个（​​S2q-P2）部分。