NMR imaging using paramagnetic chelates having hydroxyalkyl-substituted
amide groups
    1.
    发明授权
    NMR imaging using paramagnetic chelates having hydroxyalkyl-substituted amide groups 失效
    使用具有羟烷基取代的酰胺基团的顺磁螯合物进行NMR成像

    公开(公告)号:US5316756A

    公开(公告)日:1994-05-31

    申请号:US515761

    申请日:1990-04-13

    摘要: Compounds of the general formula I: ##STR1## R.sup.1 signifies a COOX group or the group ##STR2## R.sup.2 and R.sup.3 are the same or different and signify a hydrogen atom, a lower straight- or branched-chain, hydrocarbon radical, a phenyl or benzyl group or either R.sup.2 or R.sup.3 signifies the group ##STR3## or R.sup.2 or R.sup.3 together signify a trimethylene or tetramethylene radical, R.sup.4 represents a straight- or branched-chain mono- or poly-hydroxyalkyl radical, R.sup.5 represents a hydrocarbon atom, a lower straight- or branched-chain, optionally mono- or poly-hydroxylated, hydrocarbon radical, Q signifies an oxygen or sulfur atom or the group ##STR4## wherein j signifies the numbers 1 to 4 and R.sup.x signifies a hydrogen atom, a lower alkoxy group with 1 to 4 carbon atoms, a COOX group, or if j>1, also the group ##STR5## wherein k and m are the same or different and represent the numbers 0 or 2, l signifies the numbers 1 or 2 and n and w are the same or different and signify the numbers 0 or 1,wherein n and w can only represent the number 1, if k and m signify the number 2, andX represents hydrogen atoms and/or metal ion equivalents, and their salts with physiologically harmless organic bases, are valuable complexing agents, complexes and complex salts for NMR imaging.

    摘要翻译: 通式I的化合物:其中R 1表示COOX基团或基团R 2和R 3相同或不同,表示氢原子,低级直链或支链烃基, 苯基或苄基或R 2或R 3表示基团,或R 2或R 3一起表示三亚甲基或四亚甲基,R 4表示直链或支链单 - 或多 - 羟基烷基,R 5表示烃原子 低级直链或支链,任选的单羟基化或多羟基化烃基,Q表示氧或硫原子或基团,其中j表示数字1至4,Rx表示氢原子, 具有1至4个碳原子的低级烷氧基,COOX基团,或者如果j> 1,则基团< IMAGE>其中k和m相同或不同并且表示数字0或2,l表示数字1或2 并且n和w相同或不同并且表示数字0或1,其中n和w只能是 代表数字1,如果k和m表示数字2,X表示氢原子和/或金属离子当量,以及它们与生理无害的有机碱的盐是NMR成像的有价值的络合剂,络合物和络合盐。

    Substituted polyamino, polycarboxy complexing agent dimers for MRI and
X-ray contrast
    7.
    发明授权
    Substituted polyamino, polycarboxy complexing agent dimers for MRI and X-ray contrast 失效
    取代的聚氨基,多羧基络合剂二聚体用于MRI和X射线对比

    公开(公告)号:US5482700A

    公开(公告)日:1996-01-09

    申请号:US269504

    申请日:1994-07-01

    摘要: 1. Compounds of general Formula I ##STR1## wherein n and m in each case mean the numbers 0, 1, 2, 3 and 4,X stands for a hydrogen atom and/or a metal ion equivalent of an element of atomic numbers 21-29, 31, 32, 37-39, 42-44, 49 or 57-83,R.sup.1 and R.sup.2, being different, mean in each case a hydrogen atom or a straight-chain, branched, saturated or unsaturated C.sub.0 -C.sub.20 -alkylene group which optionally contains imino, phenylenoxy, phenylenimino, amido, hydrazido, ester group(s), oxygen, sulfur and/or nitrogen atom(s) and is substituted, if desired, by hydroxy, mercapto, imino, epoxy, oxo, thioxo and/or amino group(s), this alkylene group exhibiting at the end either a second molecule of general Formula I.sub.A or I.sub.B ##STR2## a functional group, or, linked by way of this functional group, a bio- or macromolecule,are valuable diagnostic and therapeutic media.

    摘要翻译: 1.通式I的化合物(I)其中n和m在各种情况下均指数字0,1,2,3和4,X表示氢原子和/或其元素的金属离子当量 原子序数21-29,31,32,37-39,42-44,49或57-83,R1和R2不同,在每种情况下是指氢原子或直链,支链,饱和或不饱和的C0 任选地含有亚氨基,亚苯氧基,亚苯基亚氨基,酰氨基,酰肼基,酯基,氧,硫和/或氮原子的-C 20 - 亚烷基,如果需要,可以被羟基,巯基,亚氨基,环氧基 ,氧代,硫代和/或氨基,该亚烷基末端表示通式IA或IB的第二分子(IA),(IB)官能团,或者由 该功能组的一种生物或大分子是有价值的诊断和治疗媒介。

    Derivatized DTPA complexes, pharmaceutical agents containing these
compounds, their use, and processes for their production
    10.
    发明授权
    Derivatized DTPA complexes, pharmaceutical agents containing these compounds, their use, and processes for their production 失效
    衍生的DTPA复合物,含有这些化合物的药剂,其用途及其生产方法

    公开(公告)号:US6039931A

    公开(公告)日:2000-03-21

    申请号:US319357

    申请日:1994-10-06

    摘要: Compounds of general Formula I ##STR1## wherein Z.sup.1 and Z.sup.2 in each case independently mean the residue--(CH.sub.2).sub.m --(C.sub.6 H.sub.4).sub.q --(O).sub.k --(CH.sub.2).sub.n --(C.sub.6 H.sub.4).sub.l --(O).sub.r --R, whereinm and n means the numbers 0-20,k, l, q and r means the numbers 0 and 1, andR means a hydrogen atom, an optionally OR.sup.1 -substituted C.sub.1 -C.sub.6 -alkyl residue, or a CH.sub.2 COOR.sup.1 group with R.sup.1 meaning it hydrogen atom, a C.sub.1 -C.sub.6 -alkyl residue, or a benzyl group,X means a hydrogen atom and/or a metal ion equivalent of an element of atomic number 21-29, 42, 44 or 57-83,with the provisos that at least two the substituents X stand for a metal ion equivalent; that one of the substituents Z.sup.1 and Z.sup.2 stands for a hydrogen and the other is not H; that--if n and l each mean the number 0--k and r do not simultaneously mean the number 1; that --(O).sub.r --R is not --OH; and that Z.sup.1 and Z.sup.2 are not --CH.sub.2 --C.sub.6 H.sub.4 --O--CH.sub.2 --COOCH.sub.2 C.sub.6 H.sub.5 or --CH.sub.2 --C.sub.6 H.sub.4 --O--(CH.sub.2).sub.5 --COOCH.sub.2 C.sub.6 H.sub.5, as well as their salts with inorganic and/or organic bases, amino acids or amino acid amides, are valuable pharmaceutical agents, e.g., for NMR.

    摘要翻译: 其中Z 1和Z 2在每种情况下独立地表示残基 - (CH 2)m - (C 6 H 4)q - (O)k - (CH 2)n - (C 6 H 4)1 - (O)r R的通式I的化合物,其中m和 n表示数字0-20,k,l,q和r表示数字0和1,R表示氢原子,任选OR 1取代的C 1 -C 6烷基残基或具有R 1的CH 2 COOR 1基团,表示氢 原子,C1-C6烷基残基或苄基,X表示原子序数21-29,42,44或57-83的元素的氢原子和/或金属离子当量,条件是在 至少两个取代基X代表金属离子当量; 取代基Z1和Z2之一代表氢,而另一个不是H; 如果n和l每个意味着数字0-k,r不同时表示数字1; - (O)r-R不是-OH; 并且Z1和Z2不是-CH2-C6H4-O-CH2-COOCH2C6H5或-CH2-C6H4-O-(CH2)5-COOCH2C6H5,以及它们与无机和/或有机碱,氨基酸或氨基酸的盐 酰胺,是有价值的药剂,例如核磁共振。