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    • 9. 发明授权
    • Aminopolycarboxylic acids and derivatives thereof for magnetic resonance
imaging
    • 氨基多羧酸及其衍生物用于磁共振成像
    • US5419893A
    • 1995-05-30
    • US5628
    • 1993-01-19
    • Arne BergTorsten AlmenJo KlavenessPal RongvedTerje Thomassen
    • Arne BergTorsten AlmenJo KlavenessPal RongvedTerje Thomassen
    • A61K49/00A61K47/48A61K49/04A61K51/00A61K51/04C07C227/18C07C229/16C07C229/22C07C229/76C07C237/06C07D257/02C07D273/00C07D285/00C07F5/00C07F11/00C07F15/02C09K3/00A61B5/055
    • A61K51/0482A61K47/48076A61K51/0478C07D257/02C07D273/00C07D285/00C07F5/003Y10S514/836Y10T436/24
    • There are provided chelating agents particularly useful for the preparation of diagnostic and therapeutic agents for magnetic resonance imaging, scintigraphy, ultrasound imaging, radiotherapy and heavy metal detoxification, said agents being compounds of formula IX--CHR.sub.1 NZ--(CHR.sub.1).sub.n --A--(CHR.sub.1).sub.m --NZ--CHR.sub.1 --X (I)(wherein each of the groups Z is a group --CHR.sub.1 X or the groups Z together are a group --(CHR.sub.1).sub.q --A'--(CHR.sub.1).sub.r --, where A' is an oxygen or sulphur atom or a group --N--Y;A is a group --N--Y or A--(CHR.sub.1).sub.m -- represents a carbon-nitrogen bond or, when the groups Z together are a group --(CHR.sub.1).sub.q --A'--(CHR.sub.1).sub.r --, A may also represent an oxygen or sulphur atom;each Y, which may be the same or different, is a group --(CHR.sub.1).sub.p --N(CHR.sub.1 X).sub.2 or a group --CHR.sub.1 X;each X, which may be the same or different, is a carboxyl group or a derivative thereof or a group R.sub.1 ;each R.sub.1, which may be the same or different, is a hydrogen atom, a hydroxyalkyl group or an optionally hydroxylated alkoxy or alkoxyalkyl group;n,m,p,q and r are each 2,3 or 4; with the provisos that at least two nitrogens carry a --CHR.sub.1 X moiety wherein X is a carboxyl group or a derivative thereof, that each --CHR.sub.1 X moiety is other than a methyl group, and that unless A' is oxygen or sulphur or A is N--(CHR.sub.1).sub.p --N(CHR.sub.1 X).sub.2 at least one R.sub.1 is other than hydrogen) and salts thereof.
    • 提供了特别可用于制备用于磁共振成像,闪烁扫描,超声成像,放射治疗和重金属解毒的诊断和治疗剂的螯合剂,所述药剂是式I X-CHR1NZ-(CHR1)nA-(CHR1) m-NZ-CHR1-X(I)(其中基团Z为基团-CHR1X或基团Z一起为基团 - (CHR 1)q -A' - (CHR 1) - ,其中A'为 氧或硫原子或基团-NY; A是基团-NY或A-(CHR1)m-表示碳 - 氮键,或者当基团Z一起为 - (CHR 1)q-A' - ( CHR1)r-,A也可以表示氧或硫原子;每个Y可以相同或不同,是基团 - (CHR1)pN(CHR1X)2或基团-CHR1X;每个X可以是 相同或不同的是羧基或其衍生物或基团R 1;每个R 1可以相同或不同,是氢原子,羟烷基或任选羟基化的烷氧基或烷氧基烷基; n,m, p,q和r 分别为2,3或4; 条件是至少两个氮原子携带-CHR1X部分,其中X是羧基或其衍生物,每个-CHR1X部分不是甲基,除非A'是氧或硫或A是N- (CHR1)pN(CHR1X)2,至少一个R1不是氢)及其盐。