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Chelating agents and their metal chelates for treating free radical induced conditions

机译:螯合剂及其金属螯合物用于治疗自由基诱发的疾病

摘要

The invention provides the use of a compound of formula (I) or a metal chelate or salt thereof in the manufacture of a therapeutic agent for use in the treatment of prophylaxis of conditions resulting from the presence of free radicals in the human or non-human animal body (wherein in formula (I): each R1 independently represents hydrogen or CH2COR5; R5 represents hydroxy, optionally hydroxylated alkoxy, amino or alkylamido; each R2 independently represents a group XYR6; X represents a bond, or a C1-3 alkylene or oxoalkylene group optionally substituted by a group R7; Y represents a bond, an oxygen atom or a group NR6; R6 is a hydrogen atom, a group COOR8, an alkyl, alkenyl, cycloalkyl, aryl or aralkyl group optionally substituted by one or more groups selected from COOR8, CONR82, NR82, OR8, NR8, O, OP(O)(OR8)R7 and OSO3M; R7 is hydroxy, an optionally hydroxylated, optionally alkoxylated alkyl or aminoalkyl group; R8 is a hydrogen atom or an optionally hydroxylated, optionally alkoxylated alkyl group; M is a hydrogen atom or one equivalent of a physiologically tolerable cation; R3 represents a C1-8 alkylene group, a 1,2-cycloalkylene group, or a 1,2-arylene group; and each R4 independently represents hydrogen or C1-3alkyl). Such compounds are particularly effective in relieving symptoms associated with reperfusion of ischemic tissue and in treating or preventing radiation-induced injury.
机译:本发明提供了式(I)化合物或其金属螯合物或其盐在制备治疗剂中的用途,所述治疗剂用于预防由人类或非人类中自由基的存在引起的疾病动物体(其中式(I)中:每个R 1 独立地代表氢或CH 2 COR 5 ; R 5 表示羟基,可选地羟基化的烷氧基,氨基或烷基酰胺基;每个R 2 独立地表示基团XYR 6 ; X表示键,或C 1- 3 亚烷基或氧亚烷基,可选地被R 7 基团取代; Y表示键,氧原子或NR 6 基团; R 6 是氢原子,基团COOR 8 ,烷基,烯基,环烷基,芳基或芳烷基,可选地被一个或多个选自COOR 8 的基团取代,CONR 8 2 ,NR 8 2 ,OR 8 ,NR 8 ,O,OP(O)(OR 8 )R 7 和OSO 3 M; R 7 是羟基,是任选羟基化,任选烷氧基化的烷基或氨基烷基; R 8 是氢原子或任选地羟基化,任选地烷氧基化的烷基; M是氢原子或生理学上可接受的阳离子的一个当量; R 3 代表C 1-8 亚烷基,1,2-亚环烷基或1,2-亚芳基;并且每个R 4 独立地代表氢或C 1-3 烷基)。这样的化合物在减轻与缺血组织的再灌注有关的症状以及治疗或预防辐射引起的损伤方面特别有效。 <图像文件=“ US06258828-20010710-C00001.GIF” imgContent =“ undefined” imgFormat =“ GIF” />

著录项

  • 公开/公告号US6258828B1

    专利类型

  • 公开/公告日2001-07-10

    原文格式PDF

  • 申请/专利权人 NYCOMED IMAGING AS;

    申请/专利号US19980213290

  • 申请日1998-12-17

  • 分类号A61K314/40;C07D2136/20;

  • 国家 US

  • 入库时间 2022-08-22 01:03:52

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