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INTRACELLULAR CALCIUM INDUCTIVE CALCIUM RELEASE CHANNEL ACTIVITY REGULATOR

机译:胞内钙诱导性钙释放通道活性调节剂

摘要

PROBLEM TO BE SOLVED: To obtain a regulator which inhibits the increase of the intracellulor calcium concentration due to the opening of intracellular calcium inductive calcium release channel caused by caffeine and, as a result, is effective in the prevention and the treatment of ischemic heart disease and the like by formulating a specific ellipticine derivative as an active ingredient. ;SOLUTION: This regulator includes an ellipticine derivative with a skeleton of formula I or its pharmacologically permissible salt, suitably an ellipticine derivative of formula II (R is H, a lower alkyl, etc.; R2 is H and a lower alkyl) or the like as an active ingredient. It is preferable that the above-stated derivative is 9-hydroxyellipticine or a compound convertible to 9-hydroxyellipticine in vivo. For example, 9-hydroxyellipticine may be reacted with a carboxylic acid derivative in a solvent in the presence of a condensing agent or a deacidification agent and then submitted to the deprotection reaction.;COPYRIGHT: (C)1999,JPO
机译:要解决的问题:获得一种调节剂,该调节剂可抑制由于咖啡因引起的细胞内钙诱导性钙释放通道的开放而引起的细胞内钙浓度的升高,因此可有效预防和治疗缺血性心脏病通过配制特定的玫瑰树碱衍生物作为有效成分等。 ;解决方案:该调节剂包括具有式I骨架的玫瑰树碱衍生物或其药理上允许的盐,合适的是式II玫瑰树碱衍生物(R为H,低级烷基等; R 2 为H和低级烷基)等作为有效成分。上述衍生物优选在体内为9-羟基玫瑰树碱或可转化为9-羟基玫瑰树碱的化合物。例如,可以使9-羟基玫瑰树碱与羧酸衍生物在溶剂中在缩合剂或脱酸剂存在下反应,然后进行脱保护反应。; COPYRIGHT:(C)1999,JPO

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