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    Vitamin D derivatives, process for producing the same and their use in the differentiation of tumor cells
    1.
    发明授权
    Vitamin D derivatives, process for producing the same and their use in the differentiation of tumor cells 失效
    维生素D衍生物，其制备方法及其在肿瘤细胞分化中的应用

    公开(公告)号：US4891364A

    公开(公告)日：1990-01-02

    申请号：US211096

    申请日：1988-06-13

    申请人： Noboru Kubodera ,  Katsuhito Miyamoto ,  Kiyoshige Ochi ,  Isao Matsunaga ,  Eigoro Murayama

    发明人： Noboru Kubodera ,  Katsuhito Miyamoto ,  Kiyoshige Ochi ,  Isao Matsunaga ,  Eigoro Murayama

    IPC分类号： C07C401/00 ,  C07J7/00 ,  C07J41/00 ,  C07J51/00 ,  C07J71/00

    CPC分类号： C07J7/002 ,  C07C401/00 ,  C07J41/005 ,  C07J51/00 ,  C07J7/007 ,  C07J71/0042

    摘要： Vitamin D derivatives of the formula ##STR1## where R.sub.1, R.sub.2 and R.sub.3 which may be the same or different each represents a hydrogen atom or a hydroxyl group; X is an oxygen atom, the group of the formula OR.sub.4 (where R.sub.4 is either a hydrogen atom or a lower alkyl having 4 to 6 carbon atoms that may or may not be substituted by a hydroxyl group), or the group of the formula=N-OR.sub.5 (where R.sub.5 is either a hydrogen atom or a lower alkyl group having 1 to 5 carbon atoms that may or may not be substituted by a hydroxyl group, an amino group or a lower alkylamino group having 1 to 3 carbon atoms), provided that the carbon atom at 20-position is linked to X by a single bond when X is the group of the formula OR.sub.4, and by a double bond in other cases, and a process for preparing the derivatives are disclosed.The derivatives have both the immunoregulating action and the ability to induce differentiation in tumor cells and hence are useful as medicines such as antiallergic agents, antirheumatic agents and antitumor agents.

    摘要翻译： 其中R1，R2和R3可以相同或不同的维生素D衍生物表示氢原子或羟基; X是氧原子，式OR4（其中R4是氢原子或具有4-6个碳原子的低级烷基，可以被羟基取代或不被羟基取代）的基团，或式= N-OR5（其中R5为氢原子或碳原子数1〜5的低级烷基，可以被羟基，氨基或碳原子数1〜3的低级烷基氨基取代） 条件是当X是式OR4的基团时，20位上的碳原子通过单键与X连接，并且在其它情况下通过双键，并且公开了制备衍生物的方法。 所述衍生物具有免疫调节作用和在肿瘤细胞中诱导分化的能力，因此可用作药物如抗过敏剂，抗风湿剂和抗肿瘤剂。

    Process for preparation of 1.alpha.,25-dihydroxycholecalciferol
    6.
    发明授权
    Process for preparation of 1.alpha.,25-dihydroxycholecalciferol 失效
    制备1 {60,25-二羟基胆钙化甾醇的方法

    公开(公告)号：US4022768A

    公开(公告)日：1977-05-10

    申请号：US657375

    申请日：1976-02-12

    申请人： Isao Matsunaga ,  Kiyoshige Ochi ,  Hiroyuki Nagano ,  Minoru Shindo ,  Masayuki Ishikawa ,  Chikara Kaneko ,  Hector F. DeLuca

    发明人： Isao Matsunaga ,  Kiyoshige Ochi ,  Hiroyuki Nagano ,  Minoru Shindo ,  Masayuki Ishikawa ,  Chikara Kaneko ,  Hector F. DeLuca

    IPC分类号： C07J9/00 ,  C07J71/00

    CPC分类号： C07J71/0042 ,  C07J9/00

    摘要： 1.alpha.,25-dihydroxycholecalciferol is prepared by reacting 1,5,7-trien-3.beta.,25-diol with a 1,2,4-triazoline-dione derivative represented by the formula: ##STR1## wherein R represents an alkyl group or an aryl or substituted-aryl group; reacting the resulting 1,4-cyclic adduct represented by the general formula ##STR2## wherein R is as defined above, with a peroxide to form a 1.alpha.,2.alpha.-epoxide compound represented by the general formula ##STR3## wherein R is as defined above, reducing the so formed compound with a metal hydride to form cholesta-5,7-diene-1.alpha.,3.beta.,25-triol, irradiating the so formed compound with ultraviolet rays to form 1.alpha.,25-dihydroxyprevitamin D.sub.3, isomerizing the so formed previtamin D.sub.3, and recovering 1.alpha.,25-dihydroxycholecalciferol.

    摘要翻译： 1α，25-二羟基胆钙化醇通过使1,5,7-三烯-3β，25-二醇与下式表示的1,2,4-三唑啉二酮衍生物反应制备：其中R表示烷基 或芳基或取代的芳基; 使得到的由通式“IMAGE”表示的所得1,4-环加成物与上述定义相同，与过氧化物反应，形成由通式“IMAGE”表示的1α，2α-环氧化合物，其中R为 用金属氢化物还原形成的化合物以形成胆甾烯-5,7-二烯-1α，3β，25-三醇，用紫外线照射所形成的化合物以形成1α，25-二羟维生素D3， 异构化所形成的维生素D3，并回收1α，25-二羟基胆钙化甾醇。

    Pentaerythritol derivative
    7.
    发明授权
    Pentaerythritol derivative 失效
    季戊四醇衍生物

    公开(公告)号：US4650888A

    公开(公告)日：1987-03-17

    申请号：US721850

    申请日：1985-04-10

    申请人： Kiyoshige Ochi ,  Yoshikazu Hinohara ,  Isao Matsunaga

    发明人： Kiyoshige Ochi ,  Yoshikazu Hinohara ,  Isao Matsunaga

    IPC分类号： A61K31/045 ,  A61K31/255 ,  A61P1/04 ,  C07C305/10 ,  C07F5/06

    CPC分类号： C07F5/069 ,  C07C303/24

    摘要： Complexes of pentaerythritol derivatives such as sulfuric acid ester of pentaerythritol or dipentaerythritol with a basic polyaluminum chloride and process for preparing the same are disclosed. The complex is novel and has a good anti-pepsin activity and therefore it is useful as an anti-ulcer agent.The complex is prepared by reacting pentaerythritol or dipentaerythritol with a sulfating agent and then reacting the resulting sulfate with a basic polyaluminum chloride.

    摘要翻译： 公开季戊四醇衍生物如季戊四醇或二季戊四醇硫酸酯与碱式聚氯化铝的配合物及其制备方法。 该复合物是新颖的，具有良好的抗胃蛋白酶活性，因此可用作抗溃疡剂。 该复合物通过使季戊四醇或二季戊四醇与硫酸化剂反应，然后使得到的硫酸盐与碱性聚氯化铝反应来制备。