申请人:Nycomed Imaging AS
公开号:US05198208A1
公开(公告)日:1993-03-30
There are provided chelating agents particularly useful for the preparations of diagnostic and therapeutic agents for magnetic resonance imaging, scintigraphy, ultrasound imaging, radiotherapy and heavy metal detoxification, said agents being compounds of formula X--CHR.sub.1 --NZ--(CHR.sub.1).sub.n --A--(CHR.sub.1).sub.m --NZ--CHR.sub.1 --X 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.
提供了螯合剂,特别适用于制备用于磁共振成像、闪烁扫描、超声波成像、放射治疗和重金属解毒的诊断和治疗剂,所述剂为具有以下结构的化合物:X--CHR.sub.1 --NZ--(CHR.sub.1).sub.n --A--(CHR.sub.1).sub.m --NZ--CHR.sub.1 --X,其中(Z组中的每个均为一个--CHR.sub.1 X组,或Z组在一起是一个--(CHR.sub.1).sub.q --A'--(CHR.sub.1).sub.r --组,其中A'是一个氧原子或硫原子或一个--N--Y组;A是一个--N--Y组或A--(CHR.sub.1).sub.m --代表一个碳-氮键或者,当Z组在一起是一个--(CHR.sub.1).sub.q --A'--(CHR.sub.1).sub.r --组时,A也可以表示一个氧原子或硫原子;每个Y(可以相同也可以不同)为一个--(CHR.sub.1).sub.p --N(CHR.sub.1 X).sub.2组或一个--CHR.sub.1 X组;每个X(可以相同也可以不同)为一个羧基或其衍生物或一个R.sub.1组;每个R.sub.1(可以相同也可以不同)为一个氢原子、一个羟基烷基组或一个可选择羟基化的烷氧基或烷氧基烷基组;n、m、p、q和r分别为2、3或4;但至少有两个氮原子携带一个--CHR.sub.1 X基团,其中X是一个羧基或其衍生物,每个--CHR.sub.1 X基团均不是甲基,且除非A'是氧或硫或A为N--(CHR.sub.1).sub.p --N(CHR.sub.1 X).sub.2,否则至少有一个R.sub.1不是氢)及其盐。