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    • 4. 发明专利
    • Adenosine derivative
    • 腺苷衍生物
    • JPH11279193A
    • 1999-10-12
    • JP9679998
    • 1998-03-24
    • Akira MatsudaHiroyasu Nakada裕康 中田彰 松田
    • MATSUDA AKIRANAKADA HIROYASUSAITO YOSHIKO
    • C07H19/16G01N33/566
    • C07H19/16Y02P20/55
    • PROBLEM TO BE SOLVED: To obtain the subject new derivative comprising a specific adenosine derivative, having binding properties to purine 3-like receptor, useful for screening the purine 3-like receptor substance, investigating pharmacological and physiological action and mechanism of purine receptor, etc.
      SOLUTION: This new adenosine derivative is shown by formula I (R
      1 and R
      2 are each a hycircxyl group or a lower alkyl; when one of R
      1 and R
      2 is the lower alkyl, the other is a hydroxyl group; when one or R
      1 and R
      2 is the hydroxyl group, the other is the lower alkyl). Since the derivative is selectively bonded to the purine 3-like receptor, the derivative is useful for screening the purine 3-like receptor and a substance having the action of the purine 3-like receptor, investigating pharmacological, biochemical and physiological actions and mechanism of purine receptor and useful as a medicine for a hypotensor, etc. The compound is obtained by reacting an aldehyde derivative of formula II (Bz is benzoyl) with the reaction product of ethyl magnesium bromide and trimethylsilylacetylene or the like at -20°C by dripping the reaction product and eliminating the protective group.
      COPYRIGHT: (C)1999,JPO
    • 要解决的问题:为了获得包含具有与嘌呤3样受体结合的特异性腺苷衍生物的主题新衍生物,可用于筛选嘌呤3样受体物质,研究嘌呤受体的药理和生理作用及机制等 解决方案:这种新的腺苷衍生物由式I表示(R 1和R 2各自为环烷基或低级烷基;当R 1和R 2中的一个为低级烷基时, 另一个是羟基;当一个或R 1和R 2是羟基时,另一个是低级烷基)。 由于衍生物选择性地与嘌呤3样受体结合,该衍生物可用于筛选嘌呤3样受体和具有嘌呤3样受体作用的物质,研究其药理学,生物化学和生理学作用及机制 嘌呤受体并用作低血压药物等。该化合物通过使式II的醛衍生物(Bz是苯甲酰基)与乙基溴化镁和三甲基甲硅烷基乙炔等在-20℃下的反应产物在-20℃下反应而获得 滴加反应产物并除去保护基。
    • 8. 发明专利
    • Dna/rna chimeric oligonucleotide
    • DNA / RNA CHIMERIC OLIGONUCLEOTIDE
    • JP2008125374A
    • 2008-06-05
    • JP2006311103
    • 2006-11-17
    • Geneticlab Co LtdAkira Matsuda彰 松田株式会社ジェネティックラボ
    • KATO YUUKAOGAWA NAOKINAMIKAWA NORIAKIMATSUDA AKIRA
    • C12N15/09
    • PROBLEM TO BE SOLVED: To provide a nucleic acid molecule having resistance to a nuclease without any toxicity in living bodies. SOLUTION: An aptamer is composed of a DNA/RNA chimeric oligonucleotide composed of a purine ribonucleotide and a pyrimidine deoxyribonucleotide. The aptamer exhibits a binding activity comparable to that of a 2'-fluoro-modified RNA for a target and has resistance equal to that of natural DNA to the nuclease. Furthermore, the aptamer is metabolized through a pathway similar to that of usual DNA or RNA without a risk of causing adverse effects due to inadequate metabolism or accumulation of non-natural substances after acting on the target in the body. COPYRIGHT: (C)2008,JPO&INPIT
    • 待解决的问题:提供对生物体没有毒性的对核酸酶具有抗性的核酸分子。 解决方案:适体由由嘌呤核糖核苷酸和嘧啶脱氧核糖核苷酸组成的DNA / RNA嵌合寡核苷酸组成。 适体表现出与目标的2'-氟修饰的RNA相当的结合活性,并具有与天然DNA相当于核酸酶的抗性。 此外,适体通过类似于通常的DNA或RNA的通路代谢,而不会由于非天然物质在身体中的靶标上的代谢或积累不足而引起不良反应的风险。 版权所有(C)2008,JPO&INPIT