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1. 发明公开

EP0639083A1 COMPLEXING AGENTS AND TARGETING IMMUNOREAGENTS 失效
标题翻译：复合剂和靶向免疫营养素
公开(公告)号：EP0639083A1
公开(公告)日：1995-02-22
申请号：EP92915130.0
申请日：1992-05-07
申请人： STERLING WINTHROP INC.
发明人： TONER, John, L. , HILBORN, David, A. , MURRAY, Bruce, J. , HOUSSAIN, Timothy, Z. , SNOW, Robert, A. , SAHA, Ashis, K. , PHILION, Richard , SHEARMAN, Clyde, W. , SHAH, Chandra West Gate Village, 500
IPC分类号： G01N33 , A61K47 , A61K49 , A61K51 , C07D213 , C07D401 , C07D471 , C07K14 , C07K16
CPC分类号： C07D213/40 , A61K47/6887 , A61K49/0002 , A61K49/0019 , A61K49/0058 , A61K51/10 , A61K51/1093 , A61K2121/00 , C07D213/36 , C07D213/38 , C07D213/42 , C07D471/04 , C07D471/08
摘要： A targeting radioactive immunoreagent comprises a metal radionuclide ion, a complexing agent, and an immunoreactive group covalently bonded to said complexing agent, the complexing agent having the structure (AI), wherein R represents hydrogen, alkyl, alkoxy, alkylthio, alkylamino, alkylformamido, aryl, aryloxy, heterocyclyl or a protein reactive group; R1 represents hydrogen, alkyl, alkoxy, alkylthio, alkylamino, alkylformamido, aryl, aryloxy, heterocyclyl or a protein reactive group; R2 represents hydroxy, carboxy, hydroxyalkyl, thioalkyl, formyl, carbonyliminodiacetic acid, methyleneiminodiacetic acid, methylenethioethyleneiminodiacetic acid, carboxyalkylthioalkyl, hydrazinylidenediacetic acid, or a salt of such acids, or two R2 groups, taken together, represent the atoms necessary to complete a macrocyclic ring structure containing at least one heteroatom coordinating site and at least one, preferably two alkylene groups forming part of the ring structure; R3 represents hydrogen, alkyl, alkoxy, alkylthio, alkylamino, alkylformamido, aryl, aryloxy, heterocyclyl or a protein reactive group; R4 represents hydrogen or a protein reactive group; n is 0 to 4; o is 0 or 1; m is 0 or 1; provided that at least one of n and m is 0 and at least one of R, R?1, R3 and R4¿ is a protein reactive group. In another aspect, this invention provides novel terpyridines, quaterpyridines, quinqepyridines, sexipyridines and phenanthrolines having the structure (AI). Preferred terpyridines have the structure (AI) above wherein n=1, o=1, m=0, and R is a protein reactive group or a phenyl substituted with a protein reactive group. Optionally, the phenyl may also contain one or more substituents selected from alkyl and alkoxy. Preferred phenanthrolines have the structure (AI) above wherein n=0, o=1, m=1 and at least one R4 is a protein reactive group. The targeting radioactive immunoreagents are particularly useful in therapeutic and diagnostic imaging compositions and methods.
摘要翻译：靶向放射性免疫试剂包含金属放射性核素离子，络合剂和与所述络合剂共价结合的免疫反应性基团，所述络合剂具有结构（AI），其中R表示氢，烷基，烷氧基，烷硫基，烷基氨基，烷基甲酰氨基，芳基，芳氧基，杂环基或蛋白质反应性基团; R1表示氢，烷基，烷氧基，烷硫基，烷基氨基，烷基甲酰氨基，芳基，芳氧基，杂环基或蛋白质反应性基团; R2代表羟基，羧基，羟基烷基，硫代烷基，甲酰基，羰基亚氨基二乙酸，亚甲基亚氨基二乙酸，亚甲基硫代亚乙基亚氨基二乙酸，羧基烷基硫代烷基，肼基亚乙基二乙酸或这些酸的盐或两个R2基团一起代表完成大环含有至少一个杂原子配位位点和至少一个，优选两个形成环结构一部分的亚烷基的结构; R3表示氢，烷基，烷氧基，烷硫基，烷基氨基，烷基甲酰氨基，芳基，芳氧基，杂环基或蛋白质反应性基团; R4代表氢或蛋白质反应性基团; n是0至4; o是0或1; m是0或1; 条件是n和m中的至少一个是0且R，R 1，R 3和R 4中的至少一个是蛋白质反应性基团。另一方面，本发明提供了具有结构（AI）的新三联吡啶，四吡啶，五联吡啶，六联吡啶和菲咯啉。优选的三联吡啶具有以上结构（AI），其中n = 1，o = 1，m = 0，并且R是蛋白质反应性基团或被蛋白质反应性基团取代的苯基。任选地，该苯基还可以含有一个或多个选自烷基和烷氧基的取代基。优选的菲咯啉具有以上结构（AI），其中n = 0，o = 1，m = 1且至少一个R 4是蛋白质反应性基团。靶向放射性免疫试剂在治疗和诊断成像组合物和方法中特别有用。

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