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Dipyridoxyl chelating agents and their metal chelates for treating free radicals induced conditions

机译:双吡啶氧基螯合剂及其金属螯合物用于治疗自由基诱发的疾病

摘要

This use of the chelating agents of the formula (I) or metal chelates thereof is in the manufacture of a therapeutic agent for use in the treatment or prophylaxis of conditions resulting from the presence of free radicals in the human or non-human animal body, particularly in relieving symptoms associated with reperfusion of ischemic tissue and in treating or preventing radiation-induced injury. The moieties of the compounds of formula (I) are defined as: 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 C1-3 alkyl).
机译:式(I)的螯合剂或其金属螯合物的这种用途是用于制造治疗剂,该治疗剂用于治疗或预防由于人类或非人类动物体内自由基的存在而引起的疾病,特别是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诱发的损伤。式(I)化合物的部分定义为:每个R 1独立地代表氢或-CH 2 COR 5; R5代表羟基,任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代表键,或C1-3的亚烷基或氧代亚烷基任选地被基团R7取代; Y表示键,氧原子或NR 6基团; R6是氢原子,基团COOR8,烷基,烯基,环烷基,芳基或芳烷基,其任选地被一个或多个选自以下的基团取代:COOR8,CONR82,NR82,OR8,= NR8,= O,OP(O) )R7和OSO3M; R7是羟基,是任选羟基化,任选烷氧基化的烷基或氨基烷基; R8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表示碳数1〜8的亚烷基,1,2-亚环烷基或1,2-亚芳基。并且每个R 4独立地表示氢或C 1-3烷基。

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