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    Composition of a n-carboxymethylated tetraazacyclododecane chelating agent, a paramagnetic metal and excess calcium ions for MRI
    2.
    发明授权
    Composition of a n-carboxymethylated tetraazacyclododecane chelating agent, a paramagnetic metal and excess calcium ions for MRI 失效
    N-羧甲基化四氮杂环十二烷螯合剂，顺磁金属和过量钙离子的组成

    公开(公告)号：US5219553A

    公开(公告)日：1993-06-15

    申请号：US743212

    申请日：1991-08-09

    申请人： Karl F. Kraft ,  Steven C. Quay ,  Scott M. Rocklage ,  Dilip Worah

    发明人： Karl F. Kraft ,  Steven C. Quay ,  Scott M. Rocklage ,  Dilip Worah

    IPC分类号： A61K49/06 ,  C07D259/00 ,  C07F5/00 ,  C07F9/38 ,  C07F13/00 ,  G01R33/28

    CPC分类号： G01R33/5601 ,  A61K49/06 ,  C07D259/00 ,  C07F13/005 ,  C07F5/003 ,  C07F9/3817 ,  Y10S424/90 ,  Y10S436/806 ,  Y10S514/836 ,  Y10S514/922 ,  Y10T436/24

    摘要： Magnetic resonance imaging contrast media used to affect the relaxation times of atoms in body tissues undergoing NMR diagnosis are disclosed. Such media comprise (1) a paramagnetic, physiologically compatible complex of (a) a chelant consisting of a N-carboxy methylated tetraazacyclododecane, and (b) a paramagnetic ion of a lanthanide element of atomic numbers 59-70, or of a transition metal of atomic numbers 21-29, 42 or 44, or a physiologically compatible salt of such a complex, and (2) a toxicity-reducing amount of labile calcium ions. The labile calcium ions can be derived from a source other than a salt of said chelant, e.g. an inorganic or organic calcium salt. NMR image-enhancing compositions comprising NMR image-enhancing effective amounts of said contrast media and pharmaceutically acceptable diluents are also disclosed.

    摘要翻译： 公开了用于影响经历NMR诊断的身体组织中的原子的弛豫时间的磁共振成像造影剂。 这种培养基包括（1）由（a）由N-羧基甲基化四氮杂环十二烷组成的螯合剂和（b）原子序数59-70的镧系元素的顺磁离子或过渡金属 的原子序数21-29,42或44，或这种络合物的生理上相容的盐，和（2）不稳定的钙离子的毒性减少量。 不稳定的钙离子可以衍生自除所述螯合剂的盐之外的来源，例如， 无机或有机钙盐。 还公开了包含NMR图像增强有效量的所述造影剂和药学上可接受的稀释剂的NMR图像增强组合物。

    Dipyridoxyl phosphate NMRI contrast agent compositions
    3.
    发明授权
    Dipyridoxyl phosphate NMRI contrast agent compositions 失效
    磷酸二吡啶酯NMRI造影剂组成

    公开(公告)号：US5091169A

    公开(公告)日：1992-02-25

    申请号：US370429

    申请日：1989-06-23

    申请人： Scott M. Rocklage ,  Steven C. Quay

    发明人： Scott M. Rocklage ,  Steven C. Quay

    IPC分类号： A61K49/06 ,  C07F9/58 ,  C07F13/00 ,  G01R33/28

    CPC分类号： C07F13/005 ,  A61K49/06 ,  C07F9/582 ,  G01R33/5601 ,  Y10T436/24

    摘要： N,N'-bis-(pyridoxal-5-phosphate)-alkylenediamine-N,N'-diacetic acids, N,N'-bis-(pyridoxal-5-phosphate)-1,2-cycloalkylenediamine-N,N'-diacetic acids, and N,N'-bis-(pyridoxal-5-phosphate)-1,2-arylenediamine-N,N'-diacetic acids, the corresponding monophosphate compounds and monoacetic acid compounds, and their salts and esters form stable, highly soluble chelates with paramagnetic metal ions, and are highly effective NMRI contrast agents. Preferred contrast agents are paramagnetic ion chelates of N,N'-bis-(pyridoxal-5-phosphate)ethylenediamine-N,N'-diacetic acid, N,N'-bis-(pyridoxal-5-phosphate)trans-1,2-cyclohexylenediamine-N,N'diacetic acid, N,N'-bis-(pyridoxal-5-phosphate)trans-1,2-arylenediamine-N,N'-diacetic acid, and the soluble calcium salts thereof.Novel intermediates for forming these compounds are N,N'-bis(pyridoxal-5-phosphate)alkylenediimines, N,N'-bis(pyridoxal-5-phosphate)alkylenediamines, N,N'-bis(pyridoxal-5-phosphate)-1,2-cycloalkylenediimines, N,N'-bis(pyridoxal-5-phosphate)-1,2-cycloalkylenediamines, N,N'-bis(pyridoxal-5-phosphate)-1,2-arylenediamines, and the corresponding monophosphate compounds.

    摘要翻译： N，N'-二 - （吡哆醛-5-磷酸） - 亚烷基二胺-N，N'-二乙酸，N，N'-双 - （吡哆醛-5-磷酸酯）-1,2-环烷二胺-N，N' - 二乙酸和N，N'-二 - （吡哆醛-5-磷酸）-1,2-芳基二胺-N，N'-二乙酸，相应的单磷酸酯化合物和单乙酸化合物，其盐和酯形成稳定 ，具有顺磁金属离子的高度可溶性螯合物，是高效的NMRI造影剂。 优选的造影剂是N，N'-双 - （吡哆醛-5-磷酸）乙二胺-N，N'-二乙酸，N，N'-双 - （吡哆醛-5-磷酸）反式-1的顺磁离子螯合物， 2-环己二胺-N，N'dia cetic酸，N，N'-双 - （吡哆醛-5-磷酸）反式-1,2-芳基二胺-N，N'-二乙酸及其可溶性钙盐。 用于形成这些化合物的新型中间体是N，N'-双（吡哆醛-5-磷酸）亚烷基二亚胺，N，N'-双（吡哆醛-5-磷酸）亚烷基二胺，N，N'-双（吡哆醛-5-磷酸酯） 1,2-环烷基二亚胺，N，N'-双（吡哆醛-5-磷酸）-1,2-环烷基二胺，N，N'-双（吡哆醛-5-磷酸）-1,2-亚芳基二胺，和相应的 单磷酸盐化合物。

    Dipyriodoxyl phosphate chelating compound intermediates
    5.
    发明授权
    Dipyriodoxyl phosphate chelating compound intermediates 失效
    二硫代磷酸酯螯合化合物中间体

    公开(公告)号：US5130431A

    公开(公告)日：1992-07-14

    申请号：US550128

    申请日：1990-07-06

    申请人： Scott M. Rocklage ,  Steven C. Quay

    发明人： Scott M. Rocklage ,  Steven C. Quay

    IPC分类号： A61K49/06 ,  C07F9/58 ,  C07F13/00 ,  G01R33/28

    CPC分类号： G01R33/5601 ,  A61K49/06 ,  C07F13/005 ,  C07F9/582

    摘要： N,N'-bis-(pyridoxal-5-phosphate)-alkylenediamine-N,N'-diacetic acids, N,N'-bis-(pyridoxal-5-phosphate)-1,2-cycloalkylenediamine-N,N'-diacetic acids, and N,N'-bis-(pyridoxal-5-phosphate)-1,2-arylenediamine-N,N'-diacetic acids, the corresponding monophosphate compounds and monoacetic acid compounds, and their salts and esters form stable, highly soluble chelates with paramagnetic metal ions, and are highly effective NMRI contrast agents. Preferred contrast agents are paramagnetic ion chelates of N,N'-bis-(pyridoxal-5-phosphate)ethylenediamine-N,N'-diacetic acid, N,N'-bis-(pyridoxal-5-phosphate)trans-1,2-cyclohexylenediamine-N,N'-diacetic acid, N,N'-bis-(pyridoxal-5-phosphate)trans-1,2-arylenediamine-N,N'-diacetic acid, and the soluble calcium salts thereof.Novel intermediates for forming these compounds are N,N'-bis(pyridoxal-5-phosphate)alkylenediimines, N,N'-bis(pyridoxal-5-phosphate)alkylenediamines, N,N'-bis(pyridoxal-5-phosphate)-1,2-cycloalkylenediimines, N,N'-bis(pyridoxal-5-phosphate)-1,2-cycloalkylenediamines, N,N'-bis(pyridoxal-5-phosphate)-1,2-arylenediamines, and the corresponding monophosphate compounds.

    摘要翻译： N，N'-二 - （吡哆醛-5-磷酸） - 亚烷基二胺-N，N'-二乙酸，N，N'-双 - （吡哆醛-5-磷酸酯）-1,2-环烷二胺-N，N' - 二乙酸和N，N'-二 - （吡哆醛-5-磷酸）-1,2-芳基二胺-N，N'-二乙酸，相应的单磷酸酯化合物和单乙酸化合物，其盐和酯形成稳定 ，具有顺磁金属离子的高度可溶性螯合物，是高效的NMRI造影剂。 优选的造影剂是N，N'-双 - （吡哆醛-5-磷酸）乙二胺-N，N'-二乙酸，N，N'-双 - （吡哆醛-5-磷酸）反式-1的顺磁离子螯合物， 2-环己二胺-N，N'-二乙酸，N，N'-双 - （吡哆醛-5-磷酸）反式-1,2-芳基二胺-N，N'-二乙酸及其可溶性钙盐。 用于形成这些化合物的新型中间体是N，N'-双（吡哆醛-5-磷酸）亚烷基二亚胺，N，N'-双（吡哆醛-5-磷酸）亚烷基二胺，N，N'-双（吡哆醛-5-磷酸酯） 1,2-环烷基二亚胺，N，N'-双（吡哆醛-5-磷酸）-1,2-环烷基二胺，N，N'-双（吡哆醛-5-磷酸）-1,2-亚芳基二胺，和相应的 单磷酸盐化合物。

    Preparation of oxamine complexes
    6.
    发明授权
    Preparation of oxamine complexes 失效
    制备恶木复合物

    公开(公告)号：US5089644A

    公开(公告)日：1992-02-18

    申请号：US61933

    申请日：1987-06-11

    申请人： Steven C. Quay ,  Scott M. Rocklage

    发明人： Steven C. Quay ,  Scott M. Rocklage

    IPC分类号： A61K49/06 ,  C07F13/00 ,  C07F15/02

    CPC分类号： C07F13/005 ,  A61K49/06 ,  C07F15/025 ,  Y10T436/24

    摘要： A process for making a solution of a complex of an oxamine and a polyvalent paramagnetic metal comprising contacting a solution of the oxamine with (a) the insoluble hydroxide of the polyvalent paramagnetic metal in water, or (b) an alkoxide of the metal is a non-aqueous solvent, thereby to form a solution of a complex of the oxamine and the metal. The complex, preferably ferrioxamine, is an improved NMR image enhancer compared even with ferrioxamine made conventionally, characterized by a high LD.sub.50.

    摘要翻译： 制备含有胺和多价顺磁性金属络合物的方法，包括将该胺的溶液与（a）多价顺磁金属的不溶性氢氧化物在水中接触，或（b）金属的醇盐是 非水溶剂，从而形成了木胺和金属络合物的溶液。 复合物，优选铁草胺，是一种改进的NMR图像增强剂，与常规制备的铁三胺相比，其特征在于高LD 50。

    Dipyridoxyl phosphate NMRI contrast agents
    7.
    发明授权
    Dipyridoxyl phosphate NMRI contrast agents 失效
    磷酸二吡啶酯NMRI造影剂

    公开(公告)号：US4933456A

    公开(公告)日：1990-06-12

    申请号：US47614

    申请日：1987-05-08

    申请人： Scott M. Rocklage ,  Steven C. Quay

    发明人： Scott M. Rocklage ,  Steven C. Quay

    IPC分类号： A61K49/00 ,  A61B5/055 ,  A61B10/00 ,  A61K49/06 ,  C07F1/00 ,  C07F1/08 ,  C07F5/00 ,  C07F9/58 ,  C07F11/00 ,  C07F13/00 ,  C07F15/00 ,  C07F15/02 ,  C07F15/04 ,  C07F15/06 ,  G01R33/28

    CPC分类号： G01R33/5601 ,  A61K49/06 ,  C07F13/005 ,  C07F9/582

    摘要： N,N'-bis-(pyridoxal-5-phosphate)-alkylenediamine-N,N'-diacetic acids, N,N'-bis-(pyridoxal-5-phosphate)-1,2-cycloalkylenediamine-N,N'-diacetic acids, and N,N'-bis-(pyridoxal-5-phosphate)-1,2-arylenediamine-N,N'-diacetic acids, the corresponding monophosphate compounds and monoacetic acid compounds, and their salts and esters form stable, highly soluble chelates with paramagnetic metal ions, and are highly effective NMRI contrast agents. Preferred contrast agents are paramagnetic ion chelates of N,N'-bis-(pyridoxal-5-phosphate)ethylene-diamine-N,N'-diacetic acid, N,N'-bis-(pyridoxal-5-phosphate)trans-1,2-cyclohexylenediamine-N,N'-diacetic acid, N,N'-bis-(pyridoxal-5-phosphate)trans-1,2-arylenediamine-N,N'-diacetic acid, and the soluble calcium salts thereof.Novel intermediates for forming these compounds are N,N'-bis(pyridoxal-5-phosphate)alkylenediimines, N,N'-bis(pyridoxal-5-phosphate)alkylenediamines, N,N'-bis(pyridoxal-5-phosphate)-1,2-cycloalkylenediimines, N,N'-bis(pyridoxal-5-phosphate)-1,2-cycloalkylenediamines, N,N'-bis(pyridoxal-5-phosphate(-1,2-arylenediamines, and the corresponding monophosphate compounds.

    Radioactive metal chelates for dipyridoxyl phosphate
    8.
    发明授权
    Radioactive metal chelates for dipyridoxyl phosphate 失效
    磷酸二吡啶酯的放射性金属螯合物

    公开(公告)号：US4842845A

    公开(公告)日：1989-06-27

    申请号：US47616

    申请日：1987-05-08

    申请人： Scott M. Rocklage ,  Steven C. Quay

    发明人： Scott M. Rocklage ,  Steven C. Quay

    IPC分类号： A61K51/00 ,  A61B5/055 ,  A61K51/04 ,  C07B59/00 ,  C07F1/00 ,  C07F9/58 ,  C07F13/00

    CPC分类号： C07F13/005 ,  A61K51/0478 ,  C07F9/582 ,  A61K2123/00

    摘要： Radioactive metal ion chelates of N,N'-bis-(pyridoxal-5-phosphate)-alkylenediamine-N,N'-diacetic acids, N,N'-bis-(pyridoxal-5-phosphate)-1,2-cycloalkylenediamine-N,N'-diacetic acids, and N,N'-bis-(pyridoxal-5-phosphate)-1,2-arylenediamine-N,N'-diacetic acids, the corresponding monophosphate compounds and monoacetic acid compounds, and their salts and esters form stable, highly soluble chelates with paramagnetic metal ions, and are highly effective agents for radiopharmaceutical imaging. Preferred contrast agents are radioactive metal ion such as technetium-99m and indium-111 ion chelates of N,N'-bis-(pyridoxal-5-phosphate)ethylenediamine-N,N'-diacetic acid, N,N'-bis-(pyridoxal-5-phosphate)trans-1,2-cyclohexylene-diamine-N,N'-diacetic acid, N,N'-bis-(pyridoxal-5-phosphate)trans-1,2-arylenediamine-N,N'-diacetic acid, and the soluble calcium salts thereof.

    NMR imaging with paramagnetic polyvalent metal salts of poly-(acid-alkylene-amino)-alkanes
    9.
    发明授权
    NMR imaging with paramagnetic polyvalent metal salts of poly-(acid-alkylene-amino)-alkanes 失效
    聚（亚烷基 - 氨基） - 烷烃的顺磁多价金属盐的NMR成像

    公开(公告)号：US5039512A

    公开(公告)日：1991-08-13

    申请号：US057709

    申请日：1987-06-15

    申请人： Karl F. Kraft ,  Steven C. Quay ,  Scott M. Rocklage ,  Dilip Worah

    发明人： Karl F. Kraft ,  Steven C. Quay ,  Scott M. Rocklage ,  Dilip Worah

    IPC分类号： A61K49/06 ,  C07D259/00 ,  C07F5/00 ,  C07F9/38 ,  C07F13/00 ,  G01R33/28

    CPC分类号： G01R33/5601 ,  A61K49/06 ,  C07D259/00 ,  C07F13/005 ,  C07F5/003 ,  C07F9/3817 ,  Y10S424/90 ,  Y10T436/24

    摘要： In a method of imaging body tissue in a patient, comprising administering to the patient an effective amount of a pharmaceutical agent for effecting the relaxation times of atoms in body tissues undergoing NMR diagnosis, whereby image contrast is enhanced, said agent comprising an amount, effective to effect such relaxation times, of a paramagnetic, physiologically compatible salt of a physiologically compatible chelate complex of an ion of a lanthanide element of atomic numbers 57-70, or of a transition metal of atomic numbers 21-29, 42, or 44; and a pharmaceutically acceptable carrier, and subjecting the patient to NMR tomography, the improvement wherein said salt of said chelate complex is the calcium or magnesium salt. Such salts are new as are some of the complexing chelates.

    摘要翻译： 在患者体内成像身体组织的方法中，包括向患者施用有效量的用于进行经历核磁共振诊断的身体组织中的原子的松弛时间的药剂，由此增强图像对比度，所述药剂包含有效量 实现这样的松弛时间，原子序数为57-70的镧系元素离子的生理上相容的螯合络合物的顺磁性生理上相容的盐或原子序数21-29,42或44的过渡金属; 和药学上可接受的载体，并对患者进行NMR层析成像，其中所述螯合络合物的所述盐是钙盐或镁盐。 这些盐是一些新的络合螯合物。