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1. 发明申请

WO2006072336A2 RADIOACTIVE METAL COMPLEXES BASED ON BISPIDINE AND THE DERIVATIVES THEREOF AS CHELATING AGENTS, AND USE THEREOF FOR NUCLEAR MEDICAL DIAGNOSIS AND THERAPY 审中-公开
标题翻译：放射性金属螯合物对Bispidine的基础，它作为螯合剂衍生物及其在核医学诊断和治疗中的应用
公开(公告)号：WO2006072336A2
公开(公告)日：2006-07-13
申请号：PCT/EP2005013171
申请日：2005-12-08
申请人： UNIV HEIDELBERG , ROSSENDORF FORSCHZENT , COMBA PETER , JURAN STEFANIE , KERSCHER MARION , PIETZSCH HANS-JUERGEN , SPIES HARTMUT , STEPHAN HOLGER
发明人： COMBA PETER , JURAN STEFANIE , KERSCHER MARION , PIETZSCH HANS-JUERGEN , SPIES HARTMUT , STEPHAN HOLGER
IPC分类号： C07D471/08 , A61K33/34 , A61K51/04 , A61K103/00 , C07B59/00
CPC分类号： C07D471/08 , C07B59/002
摘要： The invention relates to specific radioactive metal complexes based on bispidine and the derivatives thereof as chelating agents, the use thereof for nuclear medical diagnosis and therapy, and a method for producing such radioactive metal complexes.
摘要翻译：本发明涉及一种基于bispidine特定放射性金属配合物和作为螯合剂和它们对核医学诊断和治疗，以及用于制备这样的放射性金属配合物的方法使用它们的衍生物。

2. 发明申请

WO2010043218A3 TETRATHIOL LIGANDS, METAL COMPLEXES, CONJUGATES, AND KITS, THE USE THEREOF IN NUCLEAR MEDICINE DIAGNOSTICS AND ENDORADIONUCLIDE THERAPY, AND METHOD FOR PRODUCING THE TETRATHIOL LIGANDS AND METAL COMPLEXES 审中-公开
标题翻译： Tetrathiol配体，金属配合物，结合物和试剂盒，它们在核医学诊断和ENDORADIONUKLIDTHERAPIE及其制造方法Tetrathiol配体和金属络合物
公开(公告)号：WO2010043218A3
公开(公告)日：2011-01-27
申请号：PCT/DE2009050056
申请日：2009-10-16
申请人： FORSCHUNGSZENTR DD ROSSENDORF , FOERSTER CHRISTIAN , PIETZSCH HANS-JUERGEN , SUHR MATTHIAS
发明人： FOERSTER CHRISTIAN , PIETZSCH HANS-JUERGEN , SUHR MATTHIAS
IPC分类号： C07D295/185 , A61K51/04 , A61K51/08 , C07D273/01 , C07F1/08 , C07F5/00 , C07F7/22 , C07F13/00
CPC分类号： C07D295/185 , C07D273/01 , C07F13/005
摘要： The invention relates to a ligand of formula (I), where (CH-R1) and (CH-R1') are substituted or non-substituted methylene bridges; the individual R1 and R1', and R3 and R3', are each selected independently of each other from hydrogen, substituted or non-substituted alkyl groups, substituted or non-substituted aryl groups; and m and n are positive whole numbers, where m represents the number of (CH-R1') groups and n represents the number of (CH-R1) groups; wherein the sum of m and n is in the range from 4 to 10; R2 and R2' are selected independently of each other from hydrogen, substituted or non-substituted alkyl groups, substituted or non-substituted carboxyl groups, substituted or non-substituted aryl groups, or Z; X is a substituted or non-substituted methylene bridge having the formula CHR4 or a non-substituted amino group (N-H) or substituted amino group (N-Z); wherein Z stands for -(CH-R5)p-A, where (CH-R5) represents a substituted or non-substituted methylene bridge, and p is a whole number standing for the number of the (CH-R5) groups, wherein p is in the range from 2 through 8; A represents a linkable unit, wherein R4 and the individual R5 are each selected independently of each other from hydrogen, substituted or non-substituted alkyl groups, substituted or non-substituted aryl groups.
摘要翻译：式（I），其中（CH-R 1）和（CH-R1“）代表取代或未取代的亚甲基桥，每个R 1和R 1”是，以及R 3和R 3“的配位体各自独立地选自氢，取代的或未取代的烷基，取代或未取代的芳基，m和n是正整数，其中m表示基团（CH-R1“）的数目，n是基团（CH-R 1）的数量，m，其中与n之和为4的范围内是如图10所示，具有式CHR 4基团或一个取代的氨基取代或未取代的亚甲基桥是R2和R2“独立地选自氢，取代的或未取代的烷基，取代或未取代的羧基，取代或未取代的芳基，或Z，X（NH）或取代的氨基（NZ），其中Z是 - （CH-R5）p，其中（CH-R 5）取代的或未取代的亚甲基表示桥且p为基团（CH-R 5），其中p为2至8的数量的整数，A是一个能够耦合单元，其中，R 4和每个R 5各自独立地选自氢，取代或未取代的烷基，取代或未取代的芳基。

3. 发明申请

WO1996030054A1 99mTc - LABELLED SEROTONIN RECEPTOR BINDING SUBSTANCES 审中-公开
标题翻译： Tc-标记的硒酸铁受体结合物质
公开(公告)号：WO1996030054A1
公开(公告)日：1996-10-03
申请号：PCT/US1996004239
申请日：1996-03-27
申请人： MALLINCKRODT MEDICAL, INC. , JOHANNSEN, Bernd , PIETZSCH, Hans-Juergen , SCHEUNEMANN, Matthias , SPIES, Harmut , BRUST, Peter
发明人： MALLINCKRODT MEDICAL, INC.
IPC分类号： A61K51/04
CPC分类号： C07F13/005 , A61K51/0478 , A61K2123/00
摘要： The invention relates to a zero-charged Tc - labelled substance having a serotonin receptor binding activity, wherein the serotonin receptor binding compound is represented by the general formula (I): L - A - B - E, wherein L is a chelating moiety selected from the group consisting of a tridentate/monodentate chelating combination; A is a 2- to 8-membered hydrocarbon biradical, wherein the carbon atoms may be interrupted by one or two heteroatoms selected from O and S; B is an N-(C1-C4) alkyl group, an NH group, or an optionally substituted piperidin-derived, piperazin-derived, morpholin-derived or pyrrolidin-derived biradical; and E is an aryl or heteroaryl group or wherein E together with B constitutes an optionally substituted 2,4-dihydroquinazolyl group; wherein said serotonin receptor binding compound is labelled with technetium- in the form of oxotechnetium (V), said technetium being attached to said compound by means of said chelating moiety. The invention also relates to a method of preparation of said labelled substance, a radiopharmaceutical composition comprising said labelled substance, a method for detecting and localizing tissues having serotonin receptors with the aid of said labelled substance and a kit for preparing a radiopharmaceutical composition containing said labelled substance.
摘要翻译：本发明涉及具有5-羟色胺受体结合活性的带零电荷的99m Tc标记物质，其中5-羟色胺受体结合化合物由通式（I）表示：L-A-B-E，其中L为选自三齿/单齿螯合组合的螯合部分; A是2-至8-元烃双基，其中碳原子可被一个或两个选自O和S的杂原子间隔; B是N-（C 1 -C 4）烷基，NH基或任选取代的哌啶衍生的哌嗪衍生的吗啉衍生的或吡咯烷衍生的双基; 并且E是芳基或杂芳基，或者其中E与B一起构成任选取代的2,4-二氢喹唑啉基; 其中所述5-羟色胺受体结合化合物用氧化锝（V）形式的锝-99m标记，所述锝通过所述螯合部分连接到所述化合物上。本发明还涉及制备所述标记物质的方法，包含所述标记物质的放射性药物组合物，借助于所述标记物质检测和定位具有5-羟色胺受体的组织的方法和用于制备包含所述标记物质的放射性药物组合物的试剂盒物质。

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