首页> 外国专利> Heterocyclic compounds having an inhibitory activity on calpains or a trapping activity on reactive oxygen species (ROS's) and their use as medicines

Heterocyclic compounds having an inhibitory activity on calpains or a trapping activity on reactive oxygen species (ROS's) and their use as medicines

机译:对钙蛋白酶具有抑制活性或对活性氧具有捕获活性的杂环化合物及其药物用途

摘要

Heterocyclic derivatives having a calpain inhibiting activity and/or an activity trapping reactive oxygen species, of formula (I) are disclosed, wherein A, X, Y, R1, R2 and Het represent variable groups as described in the specification, with the exception that when Het represents tetrahydrofuran or tertahydropyran, R1 represents the OR3 radical wherein R3 is H, alkyl, arylalkyl, heterocycloalkylcarbonyl radical the heterocycloalkyl radical of which is connected by a carbon atom, alkylcarbonyl, arylcarbonyl or aralkylcarbonyl radical, R2 is H and Y is (CH2)p with p=0, then X is CO-N(R45)-CR46R47)- CO with R45 and R46 being H and R47 is H alkyl, aryl, or aralkyl radical the alkyl and aryl groups of which are optionally substituted. Methods for preparing these compounds, pharmaceutical preparations containing them and their therapeutic use, in particular as calpain inhibitors and/or as trapping agents for reactive oxygen species, whether selectively or not is also disclosed.
机译:公开了具有钙蛋白酶抑制活性和/或捕获活性氧的活性的式(I)的杂环衍生物,其中A,X,Y,R 1,R 2和Het表示说明书中所述的可变基团,除了当Het代表四氢呋喃或四氢呋喃时,R1代表OR3基团,其中R3为H,烷基,芳基烷基,杂环烷基羰基通过碳原子连接的烷基,烷基羰基,芳基羰基或芳烷基羰基,R2为H且Y为(CH2 ),其中p = 0,则X是CO-N(R 45)-CR 46 R 47)-CO,R 45和R 46是H,R 47是H烷基,芳基或芳烷基,其烷基和芳基任选被取代。还公开了制备这些化合物的方法,含有它们的药物制剂及其治疗用途,特别是作为钙蛋白酶抑制剂和/或作为活性氧的捕集剂,无论是否选择性地。

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