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    • 6. 发明授权
    • N.sup.6,N.sup.6 -disubstituted-cyclic adenosine-3',5'-monophosphates and
pharmacutical compositions
    • N6,N6-二取代 - 环腺苷-3',5'-单磷酸酯和药物组合物
    • US5246922A
    • 1993-09-21
    • US571188
    • 1990-08-23
    • Shigehiro KataokaNobuyuki YamajiMotohiko KatoShoichi Imai
    • Shigehiro KataokaNobuyuki YamajiMotohiko KatoShoichi Imai
    • C07H19/213A61K31/70A61K31/7042A61K31/7052A61K31/7076A61P9/04C07H19/20
    • C07H19/20Y02P20/55
    • The present invention relates to a N.sup.6,N.sup.6 -disubstituted-cyclic adenosine-3',5'-monophosphate represented by the formula ##STR1## wherein R represents a linear alkyl group having 3 or more carbon atoms or a branched alkyl group having 4 or more carbon atoms, an aralkyl group or an alkenyl group; A.sup..sym. represents a hydrogen ion, an alkali metal ion, an alkaline earth metal ion, an ammonium ion or an organoammonium ion, or a salt thereof, and a cardiac composition comprising it as an effective component, and further includes a process for preparing a compound represented by the formula ##STR2## wherein R.sub.1 represents an alkyl group, an aralkyl group or an alkenyl group and A.sup..sym. has the same meanings as defined above, or a salt thereof, characterized in that a 2'-O-protected-cyclic adenosine-3',5'-monophosphate represented by the formula ##STR3## wherein Y represents a protecting group and A.sup..sym. has the same meanings as defined above, or a salt thereof is reacted with an organic halide represented by the formulaR.sub.1 X (III) wherein X represents a halogen atom and R.sub.1 has the same meanings as defined above, and the protecting group is then removed.
    • 本发明涉及由式(I)表示的N6,N6-二取代环腺苷-3',5'-单磷酸酯,其中R表示具有3个或更多个碳原子的直链烷基或支链烷基 具有4个或更多个碳原子,芳烷基或烯基; A(+)表示氢离子,碱金属离子,碱土金属离子,铵离子或有机铵离子或其盐,以及包含其作为有效成分的心脏组合物,还包括 制备由式(I')表示的化合物,其中R 1表示烷基,芳烷基或烯基,A(+)具有与上述相同的含义或其盐,其特征在于, 或其盐,其中Y表示保护基,A(+)与上述相同的含义,由式(II)表示的2'-O-保护环腺苷-3',5'-单磷酸 与式R1X(III)表示的有机卤化物反应,其中X表示卤素原子,R 1具有与上述相同的含义,然后除去保护基。