公开(公告)号：WO1991007911A1

公开(公告)日：1991-06-13

申请号：PCT/US1990005967

申请日：1990-10-17

Applicant: CONCAT LTD.

Inventor： CONCAT LTD. ,  WINCHELL, Harry, S. ,  KLEIN, Joseph, Y. ,  SIMHON, Elliot, D. ,  CYJON, Rosa, L. ,  KLEIN, Ofer ,  ZAKLAD, Haim

IPC: A61B05/05

CPC classification number: G01R33/5601 ,  A61K49/06 ,  C07F9/6524

Abstract: Polyphosphonate ligands containing three or more phosphonate groups, combined with paramagnetic metal cations and administered in the form of pharmacologically acceptable salts, are useful as MRI contrast enhancement agents, which tend to localize in bone tissue without being conjugated to bone-specific biomolecules. Triazacyclononanes and tetraazacyclododecanes, with dihydroxyphosphorylmethyl or dihydroxyphosphorylethyl groups, optionally substituted at the methyl or ethyl bridges with alkyl, aryl, hydroxyl or amino groups, are particularly preferred.

Abstract translation: 含有三个或更多个膦酸酯基团的多膦酸酯配体与顺磁性金属阳离子组合并以药理学上可接受的盐的形式施用可用作MRI对比度增强剂，其倾向于定位在骨组织中而不与骨特异性生物分子缀合。 三氮杂环壬烷和四氮杂环十二烷与任选在甲基或乙基桥上被烷基，芳基，羟基或氨基取代的二羟基磷酰基甲基或二羟基磷酰基乙基是特别优选的。

公开(公告)号：WO1995005118A1

公开(公告)日：1995-02-23

申请号：PCT/US1994008459

申请日：1994-07-28

Applicant: CONCAT LTD.

Inventor： CONCAT LTD. ,  WINCHELL, Harry, S. ,  KLEIN, Joseph, Y. ,  CYJON, Rosa, L. ,  SIMHON, Elliot, D.

IPC: A61B05/055

CPC classification number: A61K49/06 ,  C07F9/6515 ,  C07F9/6524 ,  Y10T436/24

Abstract: Ligands with three of more nitrogen atoms incorporated into a linear or cyclic backbone structure, with the nitrogen atoms substituted with a combination of phosphonate groups and non-phosphonates groups, of which at least two are phosphonate groups, are disclosed. These ligands are combined with paramagnetic metal cations and administered in the form of pharmacologically acceptable salts, are useful as MRI contrast enhancement agents, which tend to localize in bone tissue without being conjugated to bone-specific biomolecules. Triazacyclononanes and tetraazacyclododecanes, with dihydroxyphosphorylmethyl or dihydroxyphosphorylethyl groups linked to the backbone nitrogens are preferred.

Abstract translation: 公开了具有三个以上氮原子并入线性或环状主链结构的配体，其中氮原子被膦酸酯基团和非膦酸酯基团的组合取代，其中至少两个是膦酸酯基团。 这些配体与顺磁金属阳离子结合并以药理学上可接受的盐的形式施用，可用作MRI对比增强剂，其倾向于定位在骨组织中而不与骨特异性生物分子缀合。 三氮杂环壬烷和四氮杂环十二烷与与骨架氮连接的二羟基磷酰基甲基或二羟基磷酰基乙基是优选的。