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    Immunosuppressive compounds
    4.
    发明公开
    Immunosuppressive compounds 失效
    免疫抑制剂Verbindungen。

    公开(公告)号：EP0444829A2

    公开(公告)日：1991-09-04

    申请号：EP91301431.2

    申请日：1991-02-22

    申请人： FISONS plc ,  FUJISAWA PHARMACEUTICAL CO., LTD.

    发明人： Cooper, Martin Edward ,  Donald, David Keith ,  Tanaka, Hirokazu

    IPC分类号： C07C69/738 ,  C07C213/10 ,  C07C233/10 ,  C07C59/72 ,  C07C59/90 ,  C07D309/30 ,  A61K31/365 ,  A61K31/215

    CPC分类号： C07D309/30 ,  C07C69/734 ,  C07C69/738 ,  C07C235/30 ,  C07C403/20 ,  C07C2601/14

    摘要： Compounds of formula I,

    wherein R¹ represents H, OH, protected OH or alkoxy; R² represents H; R³ represents O or (H,OH); R⁴ represents methyl, ethyl, propyl or allyl; R⁵ represents OH, protected OH or alkoxy; R⁶ represents OH; R⁷ represents OH, alkoxy or NR⁸R⁹ where R⁸ and R⁹ independently represent H, alkyl or aryl; in addition, R¹ and R² may together represent a second bond between the carbon atoms to which they are attached; and R⁶ and R⁷ may together represent O; and pharmaceutically acceptable salts thereof; are useful inter alia as immunosuppressive agents. The invention also provides the novel compounds of formula I.

    摘要翻译： 式I化合物，其中R 1表示H，OH，保护的OH或烷氧基; R 2表示H; R 3表示O或（H，OH）; R 4代表甲基，乙基，丙基或烯丙基; R 5表示OH，保护的OH或烷氧基; R 6表示OH; R 7表示OH，烷氧基或NR 8 R 9，其中R 8和R 9独立地表示H，烷基或芳基; 此外，R 1和R 2可以一起代表它们所连接的碳原子之间的第二键; R 6和R 7可以一起表示O; 及其药学上可接受的盐; 尤其可用作免疫抑制剂。 本发明还提供了新的式I化合物。

    A new antimicrobial compound,WF11605,derivatives therof and processes for preparing the same
    5.
    发明公开
    A new antimicrobial compound,WF11605,derivatives therof and processes for preparing the same 失效
    Antimikrobielle Verbindung，WF 11605，derenAbkömmlingeund Verfahren zu deren Herstellung。

    公开(公告)号：EP0330334A1

    公开(公告)日：1989-08-30

    申请号：EP89301203.9

    申请日：1989-02-08

    申请人： FUJISAWA PHARMACEUTICAL CO., LTD.

    发明人： Okamoto, Masanori ,  Tsujii, Eisaku ,  Kaizu, Tsutomu ,  Hatanaka, Hiroshi ,  Okuhara, Masakuni ,  Sawada, Kozo ,  Tanaka, Hirokazu

    IPC分类号： C07D309/10 ,  C12P17/06 ,  A61K31/71 ,  C07C62/38 ,  C07J63/00

    CPC分类号： C07J63/008 ,  C12P17/06

    摘要： Compounds of the formula:
    wherein R¹ is hydrogen or acyl,
    R² is hydrogen or
    in which
    R⁴, R⁵, R⁶ and R⁷ are hydrogen or acyl,
    R³ is carboxy or protected carboxy,
    and pharmaceutically acceptable salts thereof.
    One of these compounds, designated WF11605, can be prepared by culturing a WF11605 - producing microorganism, such as Agonomycetes strain F-11605, in an aqueous nutrient medium under aerobic conditions. Processes are also provided for the preparation of various synthetic derivatives of WF11605.
    The compound WF11605 and its derivatives possess antimicrobial activity and are useful as antibiotics and as agents for the prevention and treatment of diseases caused by Leukotriene B₄ (LTB₄). Pharmaceutical compositions containing these compounds are described.

    摘要翻译： 其中R 1是氢或酰基，R 2是氢或CHEM，其中R 4，R 5，R 6和R 7分别是 氢或酰基，R 3是羧基或被保护的羧基，及其药学上可接受的盐。 这些化合物中的一种，称为WF11605，可以通过在有氧条件下在水性营养培养基中培养产生WF11605的微生物，例如Agiogretes菌株F-11605来制备。 还提供了制备WF11605的各种合成衍生物的方法。 化合物WF11605及其衍生物具有抗微生物活性，可用作抗生素和预防和治疗由白三烯B4（LTB4）引起的疾病的药剂。 描述含有这些化合物的药物组合物。

    Pyrrolidine derivatives
    6.
    发明公开
    Pyrrolidine derivatives 失效
    吡咯烷衍生物

    公开(公告)号：EP0289911A3

    公开(公告)日：1989-08-16

    申请号：EP88106637.7

    申请日：1988-04-26

    申请人： FUJISAWA PHARMACEUTICAL CO., LTD.

    发明人： Setoi, Hiroyuki ,  Hirai, Hideo ,  Marusawa, Hiroshi ,  Kuroda, Akio ,  Tanaka, Hirokazu ,  Hashimoto, Masashi

    IPC分类号： C07D207/14 ,  A61K31/40

    CPC分类号： C07D207/16 ,  C07D207/12 ,  C07D207/14

    摘要： A compound of the formula :
    wherein
        R¹ is hydrogen or an acyl group,
        R² is an acyl group,
        R³ is carboxy(lower)alkyl, lower alkyl substituted with carboxy and one or more halogen atom(s), protected carboxy(lower)alkyl, carboxyaryl, protected carboxyaryl, carboxy, protected carboxy, hydroxy(lower)­alkyl, sulfino(lower)alkyl, phosphono(lower)alkyl, protected phosphono(lower)alkyl or halo(lower)­alkyl,
        R⁷ is hydrogen or lower alkyl, and
        A is
    (in which R⁸ is hydrogen or lower alkyl),
    and a pharmaceutically acceptable salt thereof, processes for its preparation and pharmaceutical compositions comprising them. The invention also relates to intermediates of the formula
    and process for production thereof.