DC107 DERIVATIVES
    12.
    发明公开
    DC107 DERIVATIVES 失效
    推出冯DC 107

    公开(公告)号:EP0786462A1

    公开(公告)日:1997-07-30

    申请号:EP96917696.5

    申请日:1996-06-14

    IPC分类号: C07D513/08 A61K31/425

    CPC分类号: C07D513/08

    摘要: DC107 derivatives represented by the formula (I):
    or pharmacologically acceptable slats thereof,
    [wherein R 1 is hydrogen, lower alkoxyalkyl, aralkyloxyalkyl, lower alkoxyalkoxyalkyl, lower alkoxyalkoxyalkoxyalkyl, aralkyl, tetrahydropyranyl, COR 4 or the like; R 2 represents hydrogen or COR 5 ; R 3 represents lower alkyl, lower alkenyl, aralkyl which may be substituted with substituted or unsubstituted aryl, lower alkoxyalkyl, aralkyloxyalkyl, substituted or unsubstituted aryloxyalkyl, lower alkoxycarbonylalkyl, lower alkanoyloxyalkyl, alicyclic alkanoyloxyalkyl or the like, or bonds to Y to represent a single bond; Y bonds to R 3 to represent a single bond, or bonds to Z to represent a single bond; Z represents hydrogen or bonds to Y to represent a single bond; W represents oxygen or NR 6 , with the proviso that the compound wherein R 1 , R 2 and Z each represents hydrogen, R 3 bonds to Y to represent a single bond, and W represents oxygen (DC107) is excluded.]

    摘要翻译: 由式(I)代表的DC107衍生物:其或其药理学上可接受的板条,其中R 1是氢,低级烷氧基烷基,芳烷氧基烷基,低级烷氧基烷氧基烷基,低级烷氧基烷氧基烷氧基烷基,芳烷基,四氢吡喃基,COR 4等; R 2表示氢或COR 5; R 3表示低级烷基,低级烯基,可被取代或未取代的芳基取代的芳烷基,低级烷氧基烷基,芳烷氧基烷基,取代或未取代的芳氧基烷基,低级烷氧基羰基烷基,低级烷酰氧基烷基,脂环族烷酰氧基烷基等,或与Y键合以表示 单一债券 Y与R 3键合以表示单键,或与Z键合以表示单键; Z表示氢或与Y键合以表示单键; W表示氧或NR 6,条件是其中R 1,R 2和Z各自表示氢,R 3与Y键合以表示单键,W表示氧(DC107 )被排除在外

    PYRROLOCARBAZOLE DERIVATIVES
    13.
    发明公开
    PYRROLOCARBAZOLE DERIVATIVES 失效
    吡咯卡拉巴唑衍生物

    公开(公告)号:EP0768311A1

    公开(公告)日:1997-04-16

    申请号:EP96905022.8

    申请日:1996-03-07

    CPC分类号: C07D487/04

    摘要: A pyrrolocarbazole derivative and a pharmaceutically acceptable salt thereof having the following formula (I):
    wherein R 1 is lower alkyl or aralkyl; R 2 is hydrogen, substituted or unsubstituted lower alkyl, lower alkenyl, or substituted or unsubstituted aralkyl; R 3 , R 4 , R 5 , R 6 and R 7 may be the same or different, and are hydrogen, halogen, nitro, substituted or unsubstituted lower alkanoyl, NR 9 R 10 , or OR 11 ; R 8 is hydrogen or is combined with R 3 to form -CONR 12 -; and when R 1 is benzyl; R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and R 8 are not simultaneously hydrogen.
    A compound of the present invention stimulates platelet production and is useful for treatment of thrombocytopenia.

    摘要翻译: 具有下式(I)的吡咯并咔唑衍生物及其药学上可接受的盐:其中R1为低级烷基或芳烷基; R2是氢,取代或未取代的低级烷基,低级链烯基或取代或未取代的芳烷基; R3,R4,R5,R6和R7可以相同或不同,为氢,卤素,硝基,取代或未取代的低级烷酰基,NR9R10或OR11; R8是氢或与R3结合形成-CONR12-​​; 当R1是苄基时; R2,R3,R4,R5,R6,R7和R8不同时为氢。 本发明的化合物刺激血小板产生并可用于治疗血小板减少症。

    RADICICOL DERIVATIVES
    18.
    发明公开
    RADICICOL DERIVATIVES 失效
    DERIVATE DES RADICICOLS

    公开(公告)号:EP0823429A1

    公开(公告)日:1998-02-11

    申请号:EP96912263.9

    申请日:1996-04-26

    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:
    wherein R 1 and R 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 4 -O-N (wherein R 4 represents hydrogen or substituted or unsubstituted lower alkyl); and R 3 represents hydrogen, alkanoyl, alkenoyl or the like; and (2) when X and R 3 are combined with each other to represent a single bond; Y represents R 4B -O-N (wherein R 4B has the same meaning as R 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R 1和R 2相同或不同,各自代表氢,链烷酰基,烯酰基或叔 - 甲基硅烷基; (1)当X表示卤素时,Y表示氧原子或R 4 -O-N(其中R 4表示氢或取代或未取代的低级烷基); 和R 3代表氢,烷酰基,烯酰基等; 和(2)当X和R 3彼此结合以表示单键时; Y表示R 4B-N-N(其中R 4具有与R 4相同的含义)。 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。