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    Optically active 1,4-hydropyridine compounds
    9.
    发明授权
    Optically active 1,4-hydropyridine compounds 失效
    光学活性的1,4-二氢吡啶化合物

    公开(公告)号：US5395941A

    公开(公告)日：1995-03-07

    申请号：US216216

    申请日：1994-03-22

    申请人： Kunio Isshiki ,  Takashi Nakashima ,  Hiroshi Tanaka ,  Takeo Yoshioka

    发明人： Kunio Isshiki ,  Takashi Nakashima ,  Hiroshi Tanaka ,  Takeo Yoshioka

    IPC分类号： A61K31/455 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/444 ,  A61P9/08 ,  A61P9/12 ,  A61P43/00 ,  C07B53/00 ,  C07D211/90 ,  C07D405/12 ,  C07D405/02

    CPC分类号： C07D405/12 ,  C07D211/90 ,  Y02P20/55

    摘要： Optically active 1,4-dihydropyridine derivatives represented by general formula (I), process for preparing compounds (Ic) (in general formula (I) , R.sup.1 is a lower alkyl group), process for preparing compounds represented by general formula (II) by hydrolyzing the compounds (Ic) under acidic conditions, process for preparing compounds represented by general formula (II) by solvolysis, under basic conditions, of compounds represented by general formula (III); ##STR1## wherein R.sup.1 is H, a lower alkyl group, a cyanoethyl group, a lower alkanoylaminoethyl group, or a lower dialkylaminoethyl group; R.sup.2 is a 2-tetrahydropyranyl group or a lower alkyloxymethyl group; R.sup.3 is a cyano group, a lower dialkylamino group or a lower alkanoylamino group; and R.sup.4 is a lower alkyl group. The compounds of general formula (I) and (II) are intermediate compounds for preparing optically active 1,4-dihydropyridine derivatives which are useful as medicines for circulatory organs. The compounds can be produced efficiently by the process of the present invention.

    摘要翻译： 通式（I）表示的光学活性的1,4-二氢吡啶衍生物，化合物（Ic）的制备方法（通式（I）中，R 1为低级烷基），由通式（II）表示的化合物的制备方法， 通过在酸性条件下水解化合物（Ic），通过在碱性条件下通过通式（III）表示的化合物的溶剂分解来制备由通式（II）表示的化合物的方法; （II）其中R1是H，低级烷基，氰基乙基，低级烷酰基氨基乙基或低级二烷基氨基乙基; R2是2-四氢吡喃基或低级烷氧基甲基; R3是氰基，低级二烷基氨基或低级烷酰氨基; R4为低级烷基。 通式（I）和（II）的化合物是制备用作循环器官药物的光学活性1,4-二氢吡啶衍生物的中间体化合物。 可以通过本发明的方法有效地制备化合物。

    Gene encoding a protein having asymmetric hydrolase activity for 4-substituted 1,4-dihydropyridine derivatives and its expression product
    10.
    发明授权
    Gene encoding a protein having asymmetric hydrolase activity for 4-substituted 1,4-dihydropyridine derivatives and its expression product 失效
    编码具有4-取代的1,4-二氢吡啶衍生物及其表达产物的不对称水解酶活性的蛋白质的基因

    公开(公告)号：US06361987B1

    公开(公告)日：2002-03-26

    申请号：US09514340

    申请日：2000-02-28

    申请人： Akira Arisawa ,  Motoko Matsufuji ,  Takurou Tsuruta ,  Kazuyuki Dobashi ,  Takashi Nakashima ,  Kunio Isshiki ,  Takeo Yoshioka

    发明人： Akira Arisawa ,  Motoko Matsufuji ,  Takurou Tsuruta ,  Kazuyuki Dobashi ,  Takashi Nakashima ,  Kunio Isshiki ,  Takeo Yoshioka

    IPC分类号： C12N914

    CPC分类号： C07D211/88 ,  C07D211/90 ,  C12N9/18 ,  C12N9/78 ,  C12P17/12 ,  C12P41/006

    摘要： This invention provides DNA fragments for efficiently preparing a protein having asymmetric hydrolase activity for 4-substituted 1,4-dihydropyridine derivatives, transformants obtained by using such a DNA fragment, and a process for preparing the aforesaid enzyme. Specifically, an isolated gene derived from the chromosome of Streptomyces viridosporus and encoding a protein having asymmetric hydrolase activity for 4-substituted 1,4-dihydropyridine derivatives, plasmids having the aforesaid gene integrated thereinto, transformants obtained by using such a plasmid, and a process for preparing the aforesaid enzyme by using such a transformant are disclosed. A process for the enzymatic conversion of 4-substituted 1,4-dihydropyridine derivatives by using the aforesaid enzyme is also disclosed.

    摘要翻译： 本发明提供了用于有效制备对4-取代的1,4-二氢吡啶衍生物具有不对称水解酶活性的蛋白质的DNA片段，以及通过使用这样的DNA片段得到的转化体及其制备方法。 具体来说，来源于链球菌链球菌的染色体的分离的基因，编码对4-取代的1,4-二氢吡啶衍生物具有不对称的水解酶活性的蛋白质，将上述基因整合到其中的质粒，使用这样的质粒获得的转化体， 公开了通过使用这种转化体制备上述酶的方法。 还公开了通过使用上述酶酶促转化4-取代的1,4-二氢吡啶衍生物的方法。