申请人:Enzo Diagnostics, Inc.
公开号:US05175269A1
公开(公告)日:1992-12-29
A detectable molecule of the formula A.sup.3 --(--X--R.sup.1 --E--Det.sup.b).sub.m where A.sup.3 is A.sup.2 or a polymer, where A.sup.3 has at least one modifiable reactive group selected from the group consisting of amino, hydroxy, cis OH, halides, aryl, imidazoyl, carbonyl, carboxy, thiol or a residue comprising an activated carbon; --X-- is selected from the group consisting of ##STR1## or a C.sub.1 -C.sub.10 branched or unbranched alkyl or aralkyl, which may be substituted by --OH; --Y-- is a direct bond to --E--, or --Y-- is --E--R.sup.2 -- where R.sup.2 is a C.sub.1 -C.sub.10 branched or unbranched alkyl; Z.sub.a is chlorine, bromine or iodine; E is O, NH or an acyclic divalent sulfur atom; Det.sup.b is a chemical moiety capable of being detected, preferably comprising biotin or a metal chelator of the formula: ##STR2## or the 4-hydroxy or acyloxy derivative thereof, where R.sup.3 is C.sub.1 -C.sub.4 alkyl or CH.sub.2 COOM, M is the same or different and selected from the group consisting of hydrogen, a metal or non-metal cation or is C.sub.1 -C.sub.10 alkyl, aryl or aralkyl; and m is an integer from 1 to the total number of modified reactive groups on A.sup.3. The detectable molecules are useful in in vitro or in vivo assays or therapy.
一种可检测的分子,其化学式为A.sup.3--(--X--R.sup.1--E--Det.sup.b).sub.m,其中A.sup.3为A.sup.2或聚合物,A.sup.3具有至少一个可修饰的反应基团,所述反应基团选自氨基、羟基、顺式羟基、卤化物、芳基、咪唑基、羰基、羧基、硫醇或包含活性碳的残基;--X--选自以下组合之一:##STR1## 或C.sub.1-C.sub.10支链或非支链烷基或芳基烷基,其可以被--OH取代;--Y--是直接键连接到--E--,或--Y--是--E--R.sup.2--,其中R.sup.2是C.sub.1-C.sub.10支链或非支链烷基;Z.sub.a是氯、溴或碘;E是O、NH或无环二价硫原子;Det.sup.b是一种可检测的化学基团,优选包括生物素或公式为:##STR2## 或其4-羟基或酰氧衍生物,其中R.sup.3为C.sub.1-C.sub.4烷基或CH.sub.2COOM,M相同或不同,选自氢、金属或非金属阳离子或C.sub.1-C.sub.10烷基、芳基或芳基烷基;m是从1到A.sup.3上修饰反应基团总数的整数。这些可检测的分子在体外或体内检测或治疗中非常有用。