Radicicol derivatives
    8.
    发明授权
    Radicicol derivatives 失效
    蓝霉素衍生物

    公开(公告)号:US5977165A

    公开(公告)日:1999-11-02

    申请号:US958285

    申请日:1997-10-27

    IPC分类号: C07D313/00 A61K31/335

    CPC分类号: C07D313/00

    摘要: The present invention relates to radicicol derivatives represented by the following formula (I) or pharmacologically acceptable salts thereof: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and each represents hydrogen, alkanoyl, alkenoyl or tert-butyldimethylsilyl; (1) when X represents halogen, Y represents an oxygen atom or R.sup.4 --O--N (wherein R.sup.4 represents hydrogen or substituted or unsubstituted lower alkyl); and R.sup.3 represents hydrogen, alkanoyl, alkenoyl or the like; and (2) when X and R.sup.3 are combined with each other to represent a single bond; Y represents R.sup.4B --O--N (wherein R.sup.4B has the same meaning as R.sup.4). The radicicol derivatives of the present invention demonstrate tyrosine kinase inhibition activity and pharmacological activities such as antitumor, antimicrobial or immunosuppression effects.

    摘要翻译: 本发明涉及由下式(I)表示的根赤壳菌素衍生物或其药理学上可接受的盐:其中R1和R2相同或不同,各自代表氢,烷酰基,烯酰基或叔丁基二甲基甲硅烷基; (1)当X表示卤素时,Y表示氧原子或R4-O-N(其中R4表示氢或取代或未取代的低级烷基); 和R3表示氢,烷酰基,烯酰基等; 和(2)当X和R 3相互结合以表示单键时; Y表示R4B-O-N(其中R4B与R4相同)。 本发明的根皮霉素衍生物显示出酪氨酸激酶抑制活性和药理活性,如抗肿瘤,抗微生物或免疫抑制作用。