利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

5 条记录 (耗时 0.012 秒)

    Vincaleukoblastine derivatives, a process for their preparation, pharmaceutical formulations containing them and the derivatives for use as antimitotic agents
    3.
    发明公开
    Vincaleukoblastine derivatives, a process for their preparation, pharmaceutical formulations containing them and the derivatives for use as antimitotic agents 失效
    Vincaleukoblastinderivate，它们的制备方法，含有它们的药物组合物和这些衍生物用作抗有丝分裂剂。

    公开(公告)号：EP0001920A1

    公开(公告)日：1979-05-16

    申请号：EP78300580.4

    申请日：1978-11-02

    申请人： ELI LILLY AND COMPANY

    发明人： Wright, Ian Glaisby ,  Neuss, Norbert ,  Thompson, Gerald Lee

    IPC分类号： C07D519/04 ,  A61K31/435

    CPC分类号： C07D519/04

    摘要： Vincaleukoblastine derivates of the formula
    wherein

    R 2 is CH 3 or CHO;
    when taken singly, R 5 is H and one of R 3 and R 4 is OH or H and the other is C 2 H 5 and when R 4 and R 5 are taken together, they form an a-epoxide ring R 3 is C 2 H 5 , when taken singly R 6 is H and R' is OR' and when R 6 and R' are taken together they are =0;
    R 1 is H or acetyl; and
    R is OCH, or NH-NH 2 with the proviso that if R is -NH-NH 2 , R 1 is H; or a pharmaceutically acceptable acid addition saft thereof, are prepared by reduction of the corresponding 4-desacetoxy-4-oxo derivatives which in turn were prepared by the oxidation of the corresponding 4- desacetyl-4β-hydroxy derivatives.

    The compounds are useful as antimitotic agents.

    摘要翻译： 式的长春花碱衍生物... ... worin ...... [R <2>是CH 3或CHO; ...当单独采取，R <5>为H，R <3>中的一个和R <4>是OH或H，并且 另一个是C 2 H 5且当R <4>和R <5>合在一起时，它们形成的α-环氧化物的环R <3>是C2H5，当单独使用采取ř<6>为H，R <7>是OR <1 >且当R <6>和R <7>合在一起它们是= 0; ... [R <1>为H或乙酰基; 和... R是OCH 3或NH-NH 2，其条件做如果R是-NH-NH 2，R <1>为H; 或其药学上可接受的酸加成盐，通过还原而后者又是通过相应的4-去乙酰基 - 4β-羟基衍生物的氧化制得的相应的4-脱乙酰基-4-氧代衍生物的制备。 ... 的化合物作为抗有丝分裂剂是有用的。