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DERIVATIVES OF CONDENSED 1,2,4-THIADIAZINE AND CONDENSED 1,4-THIAZINE, THEIR SYNTHESIS AND USING
DERIVATIVES OF CONDENSED 1,2,4-THIADIAZINE AND CONDENSED 1,4-THIAZINE, THEIR SYNTHESIS AND USING
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机译:缩合的1,2,4-噻嗪和缩合的1,4-噻嗪的衍生物,其合成和用途
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FIELD: organic chemistry, chemical technology, pharmacy. SUBSTANCE: invention describes novel derivatives of condensed 1,2,4-thiadiazine of the general formula (I) given in the description where B means one of bonds in double bond between atoms 2 and 3 of ring of the formula (I); D means -S(=O)2-; R1 means hydrogen atom; R4 means hydrogen atom; or R4 in common with R5 means one of bonds in double bond between atoms 2 and 3 of the formula (I); or R1 in common with R4 means one of bonds in double bond between atoms 3 and 4 of the formula (I); R2 means hydrogen atom, C1-6-alkyl, C3-6-cycloalkyl, C2-6-alkenyl; R3 means R8, aryl substituted with C1-6-alkyl where R8 means hydrogen atom, C3-6-cycloalkyl or (C3-6-cycloalkyl)-C1-6-alkyl, unbranched or branched C1-18-alkyl, with optionally mono- or polysubstituted hydroxy-group, C3-6-cycloalkyl, aryl, carboxy-group; A in common with 5 and 6 carbon atoms of the formula (I) means 5-membered heterocyclic system containing one or two nitrogen atoms or one sulfur atom being heterocyclic systems are optionally mono- or poly-substituted with halogen atom under condition of excluding the following compounds: 3-aminoimidazo-[4,5-e] -1,2,4-thiadiazine 1,1-dioxide and 3-(benzoylamino)-imidazo-[4,5-e] -1,2,4-thiadiazine 1,1-dioxide or its salt with pharmaceutically acceptable acid or base. New compounds are used as agents opening KATF-regulated potassium channels. Also, invention describes pharmaceutical composition eliciting effect on KATF-regulated potassium channels and method of effect on KATF-regulated channels. EFFECT: improved method of synthesis, valuable medicinal properties of compounds. 18 cl, 23 ex
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机译:领域:有机化学,化学技术,药学。物质:本发明描述了通式(I)的缩合的1,2,4-噻二嗪的新型衍生物。<图像文件=“ 00000001.GIF” he =“ 37” id =“ imag00000001” imgContent =“ undefined” imgFormat =“ GIF说明书中给出的“ wi =“ 51” />,其中B表示式(I)的环的原子2和3之间的双键中的一个键; D表示-S(= O) 2 Sub>-; R 1 Sup>表示氢原子; R 4 Sup>表示氢原子;与R 5 Sup>共同的R 4 Sup>是指式(I)的原子2与原子3之间的双键中的一个键。与R 4 Sup>共同的R 1 Sup>是指式(I)的原子3与原子4之间的双键中的一个键。 R 2 Sup>是指氢原子,C 1-6 Sub>-烷基,C 3-6 Sub>-环烷基,C 2-6 Sub>-烯基; R 3 Sup>表示R 8 Sup>,被C 1-6 Sub>-烷基取代的芳基,其中R 8 Sup>表示氢原子, C 3-6 Sub>-环烷基或(C 3-6 Sub>-环烷基)-C 1-6 Sub>-烷基,直链或支链C 1-18 Sub>-烷基,具有任选地单或多取代的羟基,C 3-6 Sub>-环烷基,芳基,羧基;与式(I)的5和6个碳原子相同的“ A”是指含有一个或两个氮原子或一个硫原子的5元杂环系统,其杂环系统任选在不排除卤素的条件下被卤素原子单取代或多取代。以下化合物:3-氨基咪唑-[4,5-e] -1,2,4-噻二嗪1,1-二氧化物和3-(苯甲酰基氨基)-咪唑-[4,5-e] -1,2,4-噻二嗪1,1-二氧化物或其盐与药学上可接受的酸或碱。新化合物被用作打开K ATF Sub>调节钾通道的试剂。另外,本发明还描述了引起对K ATF Sub>调节的钾通道的作用的药物组合物和对K ATF Sub>调节的通道的作用的方法。效果:改进的合成方法,有价值的化合物药物特性。 18 cl,前23
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