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    N.sup.6,N.sup.6 -disubstituted-cyclic adenosine-3',5'-monophosphates and pharmacutical compositions
    5.
    发明授权
    N.sup.6,N.sup.6 -disubstituted-cyclic adenosine-3',5'-monophosphates and pharmacutical compositions 失效
    N6，N6-二取代 - 环腺苷-3'，5'-单磷酸酯和药物组合物

    公开(公告)号：US5246922A

    公开(公告)日：1993-09-21

    申请号：US571188

    申请日：1990-08-23

    申请人： Shigehiro Kataoka ,  Nobuyuki Yamaji ,  Motohiko Kato ,  Shoichi Imai

    发明人： Shigehiro Kataoka ,  Nobuyuki Yamaji ,  Motohiko Kato ,  Shoichi Imai

    IPC分类号： C07H19/213 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7052 ,  A61K31/7076 ,  A61P9/04 ,  C07H19/20

    CPC分类号： C07H19/20 ,  Y02P20/55

    摘要： 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.

    摘要翻译： 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。

    Method for preparing N.sup.6,8-disubstituted 3',5'-cyclic adenosine monophosphate and salt thereof
    7.
    发明授权
    Method for preparing N.sup.6,8-disubstituted 3',5'-cyclic adenosine monophosphate and salt thereof 失效
    制备N6,8-二取代的3'，5'-环腺苷单磷酸及其盐的方法

    公开(公告)号：US4567254A

    公开(公告)日：1986-01-28

    申请号：US652093

    申请日：1984-09-19

    申请人： Shigehiro Kataoka ,  Takashi Nakamura ,  Nobuyuki Yamaji ,  Seiichi Nasuno

    发明人： Shigehiro Kataoka ,  Takashi Nakamura ,  Nobuyuki Yamaji ,  Seiichi Nasuno

    IPC分类号： C07H19/20 ,  C07H15/12 ,  C07H17/00

    CPC分类号： C07H19/20

    摘要： A method for preparing an N.sup.6,8-disubstituted 3',5'-cyclic adenosine monophosphate or a salt thereof represented by the general formula ##STR1## wherein X denotes a halogen atom or ##STR2## N.sub.3, OH or OR, R being an alkyl or aralkyl group; A.sup..sym. denotes a hydrogen ion, alkali metal ion, ammonium ion or organic ammonium ion; and R.sub.1 denotes an alkyl or aromatic group, which method comprises reacting an 8-substituted 3',5'-cyclic adenosine monophosphate or a salt thereof represented by the general formula (II) ##STR3## wherein X and A.sup.61 are as defined above, with an aldehyde represented by the general formulaR.sub.1 --CHO (III)wherein R.sub.1 is as defined above, to form an imine compound represented by the general formula ##STR4## wherein X, R.sub.1 and A.sup..sym. are as defined above, as an intermediate, and then reducing the imine compound.

    摘要翻译： 一种制备由通式（I）表示的N6,8-二取代的3'，5'-环腺苷单磷酸或其盐的方法，其中X表示卤素原子或N 3，OH或OR， R为烷基或芳烷基; A（+）表示氢离子，碱金属离子，铵离子或有机铵离子; 并且R 1表示烷基或芳基，该方法包括使由通式（II）表示的8-取代的3'，5'-环腺苷一磷酸或其盐，其中X和A61为 （IV）表示的亚胺化合物，其中X，R 1和A（+）是如上定义的，其中R 1如上所定义，通式为R1-CHO 如上所定义，作为中间体，然后还原亚胺化合物。

    Process for preparation of N.sup.6 -substituted 3',5'-cyclic adenosine monophosphate and salt thereof
    8.
    发明授权
    Process for preparation of N.sup.6 -substituted 3',5'-cyclic adenosine monophosphate and salt thereof 失效
    制备N6-取代的3'，5'-环腺苷一磷酸及其盐的方法

    公开(公告)号：US4751293A

    公开(公告)日：1988-06-14

    申请号：US727062

    申请日：1985-04-25

    申请人： Shigehiro Kataoka ,  Ayako Nasu ,  Nobuyuki Yamaji ,  Motohiko Kato

    发明人： Shigehiro Kataoka ,  Ayako Nasu ,  Nobuyuki Yamaji ,  Motohiko Kato

    IPC分类号： C07H19/213 ,  C07H1/00 ,  C07H19/20 ,  C07H15/12 ,  C07H17/00

    CPC分类号： C07H19/20

    摘要： A method for the preparation of an N.sup.6 -substituted 3',5'-cyclic adenosine monophosphate or a salt thereof represented by the general formula ##STR1## wherein R.sub.1 represents a straight chain or branched chain alkyl group of 1 to 13 carbon atoms or an aromatic group and B.sym. represents a hydrogen ion or an alkali metal ion, which comprises allowing a 3',5'-cyclic adenosine monophosphate or a salt thereof represented by the general formula ##STR2## wherein A.sym. represents a hydrogen ion, alkali metal ion, organic ammonium ion, or ammonium ion, to react with an aldehyde represented by the general formulaR.sub.1 CHO (III)wherein R.sub.1 is as defined above, under the conditions such that pH is 7.0 or below, the temperature is -10.degree. to 120.degree. C., and the molar ratio of the compound (II) to the compound (III) is 1:1-40, and reducing the resulting compound with a metal hydride or nascent hydrogen.

    摘要翻译： 一种制备由通式（I）表示的N6-取代的3'，5'-环腺苷一磷酸或其盐的方法，其中R 1表示1至13个碳的直链或支链烷基 原子或芳基，B（+）表示氢离子或碱金属离子，其包括使通式（II）表示的3'，5'-环腺苷一磷酸或其盐，其中A （+）表示氢离子，碱金属离子，有机铵离子或铵离子，在通式R 1 CHO（III）表示的醛中，其中R 1如上定义，在pH为7.0或 温度为-10℃〜120℃，化合物（II）与化合物（III）的摩尔比为1:1-40，用金属氢化物或新生氢还原所得化合物。