MACROCYCLIC COMPOUNDS
    71.
    发明授权
    MACROCYCLIC COMPOUNDS 失效
    大环化合物。

    公开(公告)号:EP0346427B1

    公开(公告)日:1995-03-29

    申请号:EP89900628.2

    申请日:1988-12-02

    申请人: FISONS plc

    摘要: Compounds of formula (I), in which [R1 and R2], [R3 and R4] and [R5 and R6] represent a carbon-carbon bond or two hydrogen atoms; R2 additionally represents alkyl; R7, R8 and R9 represent groups including H or OH, R10 has various significances including alkyl and alkenyl; X and Y represent groups including O and (H, OH); R14, R15, R16, R17, R18, R19, R22 and R23 represent H or alkyl; R20 and R21 represent groups including O, (H, OH) and (H, O-alkyl), n is 1, 2 or 3, and in addition, Y, R10 and R23, together with the carbon atoms to which they are attached, may represent a heterocyclic ring, (with certain provisos) are described. Processes for making the compounds and pharmaceutical formulations containing them, e.g. for use as immunosuppressive agents, are also described.

    Novel processes for the production of 13-ether derivatives of milbemycins, and novel intermediates therefor
    73.
    发明公开
    Novel processes for the production of 13-ether derivatives of milbemycins, and novel intermediates therefor 失效
    Verfahren zur Herstellung von 13-Ether-Derivaten von Milbemycinen und Zwischenprodukte。

    公开(公告)号:EP0594291A1

    公开(公告)日:1994-04-27

    申请号:EP93306899.1

    申请日:1993-09-01

    IPC分类号: C07D493/22 C07H19/01

    摘要: 57 An intermediate useful in the synthesis of milbemycin derivatives having an ether bond at the 13-position and which is represented by the general formula (IIId) :

    wherein R represents a methyl group, an ethyl group, an isopropyl group or a sec-butyl group, and R 5 and R 6' each individually represents a hydrogen atom or a protecting group, and related precursors as well as to a process for producing these intermediates.

    摘要翻译: 可用于合成在13位上具有醚键并由通式(IIId)表示的密尔伯霉素衍生物的中间体:其中R表示甲基,乙基,异丙基或秒 丁基,R 5和R 6'各自独立地表示氢原子或保护基,以及相关前体以及制备这些中间体的方法。

    A process for the glycosylation of avermectin compounds at the 14a-position
    77.
    发明公开
    A process for the glycosylation of avermectin compounds at the 14a-position 失效
    Verfahren zur Glycosylierung von Auermectinverbindungen an der 14a-Position。

    公开(公告)号:EP0524687A1

    公开(公告)日:1993-01-27

    申请号:EP92202163.9

    申请日:1992-07-15

    申请人: MERCK & CO. INC.

    CPC分类号: C07H19/01 C12P19/58

    摘要: Avermectin compounds are glycosylated the 14a- position by adding the avermectin compounds to the fermentation medium of Bacillus subtilis  . The 14a-methyl group of the avermectin compound is glycosylated with a glycosyl moiety, specifically a glucose group. The compounds are potent anthelmintic and antiparasite agents, and compositions for such uses are also disclosed.

    摘要翻译: 通过将阿维菌素化合物加入到枯草芽孢杆菌的发酵培养基中,阿维菌素化合物被14位糖基化。 阿维菌素化合物的14a-甲基用糖基部分,特别是葡萄糖基团糖基化。 这些化合物是有效的驱肠虫剂和抗寄生虫剂,并且还公开了用于此类用途的组合物。