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1. 发明申请

WO1991010655A1 1,4,10,13-TETRAOXA-7,16-DIAZACYCLOOCTADECANE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND THEIR USE FOR THE REMOVAL OF TOXIC METAL IONS AND RADIOACTIVE ISOTOPES FROM THE LIVING ORGANISM 审中-公开
标题翻译： 1,4,10,13-四氮杂-7,16-二氮杂十八烷衍生物，含有它们的药物组合物及其用于从生活有机体中去除毒性金属离子和放射性同位素
公开(公告)号：WO1991010655A1
公开(公告)日：1991-07-25
申请号：PCT/HU1990000070
申请日：1990-11-07
申请人： ORSZAGOS "e;FREDERIC JOLIOT-CURIE"e; SUGARBIOLOGIAI ... , KOSSUTH, Lajos, Tudományegyetem , EMRI, József , GYORI, Béla , KOVACS, Zoltán , BRÜCHER, Erno , SZTANYIK, László, B. , VARGA, László , KIRALY, Ödön , KANYAR, Béla
发明人： ORSZAGOS "e;FREDERIC JOLIOT-CURIE"e; SUGARBIOLOGIAI ... , KOSSUTH, Lajos, Tudományegyetem
IPC分类号： C07D273/08
CPC分类号： C07D273/00
摘要： The invention relates to partially novel metal complexes, salts and double salts of 1,4,10,13-tetraoxa-7,16-diazacyclooctadecane compounds of formula (I), wherein Q and Q mean hydrogen or a group of formula (III), in the groups of formula (III) the R substituents independently represent hydrogen, a C1-5 straight or branched chain alkyl group, a C2-5 straight or branched chain alkenyl group, phenyl or phenyl-C1-5alkyl group, the two latter ones optionally being substituted on their aromatic part by one or more halogen(s), C1-5alkyl, C1-5alkoxy, cyano or nitro group(s), with the proviso that at least one of Q and Q is other than hydrogen; Me stands for an alkaline metal or alkaline earth metal or transition metal ion; q is 0 or 1; M and N, independently from each other, stand for hydrogen or an alkaline metal, alkaline earth metal or optionally substituted ammonium ion; m, n and p are integers each being equal to the charge of M, N or Me, respectively; s and r are, independently from each other, 0, 1, 2, 3 or 4, with the proviso that (i) r, s and q cannot simultaneously be 0; and (ii) the number of hydrogens in the meaning of M or N may be 0, 1 or 2, as well as pharmaceutical compositions containing these compounds. The compounds and compositions according to the invention can be used for the decorporation of metal ions, mainly radioactive isotopes such as radioactive strontium or cerium being harmful to the living organism. The active agents according to the invention exert their effects either in intravenous or local, transdermal or rectal route of administration.
摘要翻译：本发明涉及式（I）的1,4,10,13-四氧杂-7,16-二氮杂环十八烷化合物的部分新型金属络合物，盐和双盐，其中Q 1和Q 2表示氢或式（III）的基团，在式（III）的基团中，R取代基独立地表示氢，C1-5直链或支链烷基，C2-5直链或支链烯基，苯基或苯基C1- 5个烷基，后两个可选地在其芳族部分被一个或多个卤素，C 1-5烷基，C 1-5烷氧基，氰基或硝基取代，条件是Q 1中的至少一个 >和Q 2不是氢; 我代表碱金属或碱土金属或过渡金属离子; q为0或1; M和N彼此独立地代表氢或碱金属，碱土金属或任选取代的铵离子; m，n和p分别是分别等于M，N或Me电荷的整数; s和r彼此独立地为0,1,2,3或4，条件是（i）r，s和q不能同时为0; 和（ii）M或N含义中的氢的数目可以是0,1或2，以及含有这些化合物的药物组合物。根据本发明的化合物和组合物可用于金属离子的析出，主要是放射性同位素，例如对活生物体有害的放射性锶或铈。根据本发明的活性剂在静脉内或局部，经皮或直肠给药途径中发挥其作用。

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