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    Fluorine derivatives of vitamin D3 and cell differentiation-inducing agents containing the same as an active ingredient
    4.
    发明公开
    Fluorine derivatives of vitamin D3 and cell differentiation-inducing agents containing the same as an active ingredient 失效
    氟化物维生素D3-衍生物和Zelldifferenzierung induzierende Mittel，死亡的Wirkstoff呕吐物。

    公开(公告)号：EP0205025A1

    公开(公告)日：1986-12-17

    申请号：EP86107131.4

    申请日：1986-05-26

    申请人： SUMITOMO PHARMACEUTICALS COMPANY, LIMITED ,  Morii, Hirotoshi

    发明人： Morii, Hirotoshi ,  Hamma, Noritaka ,  Saito, Yoshikazu ,  Nishizawa, Toshio ,  Nagata, Akihiko

    IPC分类号： C07C172/00 ,  A61K31/59 ,  C07J9/00

    CPC分类号： C07C401/00 ,  C07J9/00 ,  Y02P20/55

    摘要： Described are novel compounds of the formula (IV)
    wherein R 1 is a hydrogen atom, a nyaroxyl group or a protected hydroxyl group and R 2 is a hydrogen atom or a protecting group,

    a pharmaceutical composition useful as a cell differentiation-inducing agent, which contains an effective amount of a compound of the formula IV (wherein R 2 is H) as an active ingredient and a pharmaceutically acceptable carrier or diluent,
    a method of inducing cell differentiation by administering an effectiveamount of a compound of the formula IV (wherein R 2 is H to a patient,
    and a proceesfor producing a compound of the formula (IV) by subjecting a previtamin D 3 derivative of the formula (III)

    wherein R 1 and R 2 are as defined above, to thermal isomerization to yield a vitamin D 3 derivative of the formula (IV) mentioned above.

    摘要翻译： 描述了式（IV）的化合物：其中R 1是氢原子，羟基或被保护的羟基，R 2是氢原子或保护基，可用作细胞分化诱导剂的药物组合物 ，其含有有效量的式IV化合物（其中R 2为H）作为活性成分和药学上可接受的载体或稀释剂，通过施用有效量的式IV化合物诱导细胞分化的方法（ 其中R 2为H）和通过使式（III）的前维生素D3衍生物（CHEM）（其中R 1和R 2如上所定义）进行热异构化制备式（Ⅳ）化合物的方法， 得到上述式（IV）的维生素D3衍生物。

    Fluorine derivatives of vitamin D3 and process for producing the same
    5.
    发明公开
    Fluorine derivatives of vitamin D3 and process for producing the same 失效
    的维生素D3和其制备方法的氟化的衍生物。

    公开(公告)号：EP0264880A1

    公开(公告)日：1988-04-27

    申请号：EP87115258.3

    申请日：1987-10-19

    申请人： SUMITOMO PHARMACEUTICALS COMPANY, LIMITED

    发明人： Hamma, Noritaka ,  Nishizawa, Toshio ,  Saito, Yoshikazu ,  Katsumata, Takashi

    IPC分类号： C07C401/00 ,  A61K31/59

    CPC分类号： C07C401/00 ,  C07J9/00 ,  C07J71/001 ,  Y02P20/55

    摘要： There are disclosed novel derivatives of 26,26,26,27,27,27-hexafluorovitamin D₃ having a fluorine atom at the 23- and/or 24-position which have an excellent pharmacological activity and a process for production thereof. The novel compounds are represented by the general formula (1).
    wherein R₁ʹ denotes a hydrogen atom, a hydroxyl group or a protected hydroxyl group, R₂ denotes a hydrogen atom or a protecting group for a hydroxyl group, R₃ denotes a hydrogen atom, a fluorine atom, a hydroxyl group or a protected hydroxyl group and R₄ and R₄ʹ each denotes a hydrogen atom, or one of them denotes a hydrogen atom and the other denotes a fluorine atom, hydroxyl group or a protected hydroxyl group or R₄ and R₄ are combined to denote an oxo group, with a proviso that at least one of R₃, R₄ and R₄ʹ denotes a fluorine atom. The process for production thereof comprises subjecting a compound represented by the general formula (3)
    wherein R₁ʹ, R₂, R₃, R₄ and R₄ʹ are the same as defined above, to thermal isomerization and optionally further to a deprotection reaction.

    摘要翻译： 存在具有在23-和/或24位上其具有优异的药理学活性和其制备方法是氟原子26,26,26,27,27,27-hexafluorovitamin D3的游离缺失盘新的衍生物。 的新化合物是由通式（1）表示。 worin R1“表示氢原子，羟基或保护的羟基，R 2表示氢原子或羟基的保护基团，R3表示氢原子，氟原子，羟基或被保护的 羟基和R 4和R 4“各自表示氢原子，或它们中的一个表示氢原子且另一个表示氟原子，羟基或保护的羟基基团或R 4和R 4结合，以表示于氧代基团，具有 条件没有R3，R4和R4“中的至少一个表示氟原子。 生产过程中其包括使由通式（3） worin R1，R2，R3，R4和R4“表示的化合物是相同的如上述所定义，热异构化并任选地进一步脱保护反应。

    Process for preparation of sulfone derivatives
    7.
    发明公开
    Process for preparation of sulfone derivatives 失效
    Verfahren zur Herstellung von Sulfon-Derivaten。

    公开(公告)号：EP0322800A1

    公开(公告)日：1989-07-05

    申请号：EP88121599.0

    申请日：1988-12-23

    申请人： SUMITOMO PHARMACEUTICALS COMPANY, LIMITED

    发明人： Ohashi, Naohito ,  Fujimoto, Koji ,  Mori, Kazuo ,  Tanaka, Yoshihiro ,  Saji, Ikutaro ,  Nishizawa, Toshio

    IPC分类号： C07D249/08 ,  C07D233/60

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08

    摘要： A process for preparing sulfone derivatives of the formula:
    wherein R¹ and R² are each a hydrogen atom, a lower alkyl group or a substituted or unsubstituted cyclo(lower)alkyl, cyclo(lower)alkylmethyl, lower alkenyl, heterocyclic, aryl or ar(lower)alkyl group, R⁴, R⁵, R⁶ and R⁷ are each a hydrogen atom, a lower alkyl group, a lower alkenyl group or a substituted or unsubstituted aryl grcup and Az is a 1,2,4- or 1,3,4-triazole or imidazole ring, which comprises subjecting a sulfide or sulfoxide compound of the formula:
    wherein R¹, R², R⁴, R⁵, R⁶, R⁷ and Az are each as defined above and n is an integer of 0 or 1 to oxidation with an oxidizing agent in the presence of a metal catalyst.

    摘要翻译： 制备下式的砜衍生物的方法：其中R 1和R 2各自为氢原子，低级烷基或取代或未取代的环（低级）烷基，环（低级）烷基甲基， 低级烯基，杂环，芳基或芳（低级）烷基，R 4，R 5，R 6和R 7各自为氢原子，低级烷基，低级烯基或 取代或未取代的芳基基团，并且Az是1,2,4-或1,3,4-三唑或咪唑环，其包括使下式的硫化物或亚砜化合物：其中R 1， R 2，R 4，R 5，R 6，R 7和A 11各自如上所定义，n是0或1的整数，在金属存在下用氧化剂氧化 催化剂。