Pharmaceutically active compounds
    2.
    发明授权
    Pharmaceutically active compounds 失效
    药物活性化合物

    公开(公告)号:US6153641A

    公开(公告)日:2000-11-28

    申请号:US981003

    申请日:1997-12-18

    摘要: The present invention provides novel compounds of the formula (I):R.sub.20 --(CH.sub.2).sub.n --R (I)wherein:T.sub.20 is a bisindolylmaleimide moiety linked to the --(CH.sub.2).sub.n -group through an indolyl nitrogen,n is 0 or 1,R is a 5 or 6 membered aromatic carbocyclic or heterocyclic ring, the heterocyclic ring containing N or S,R is substituted by R.sub.1 and up to four of R.sub.2, R.sub.3, R.sub.4 and R.sub.5,wherein;R.sub.1 is aminomethyl, (N--(C.sub.1-4 -alkyl)amino)methyl, (N,N-di(C.sub.1-4 -alkyl)amino)methyl or pyridiniummethyl, andR.sub.2, R.sub.3, and R.sub.4 and R.sub.5 (if present), which may be the same or different, are each hydrogen, hydroxy, C.sub.1-4 -alkoxy, C.sub.1-4 -alkoxy) or halogen,or R.sub.2 when in a position contiguous to the bond connecting R to the --(CH.sub.2).sub.n -- group and n is 1 may, together with the 2-carbon atom on the indole to which the --(CH.sub.2) group is attached, form a ring,and pharmaceutically acceptable salts thereof; and the use of such compounds in medical therapy.

    摘要翻译: PCT No.PCT / SE97 / 01504 Sec。 371 1997年12月18日第 102(e)1997年12月18日PCT PCT 1997年9月8日PCT公布。 公开号WO98 / 11102 日期:1998年3月19日本发明提供式(I)的新化合物:R 20 - (CH 2)n R(I)其中:T 20是通过吲哚基氮连接至 - (CH 2)n - 基的双吲哚基马来酰亚胺部分,n 是0或1,R是5或6元芳族碳环或杂环,含有N或S的杂环,R被R 1和多至四个R 2,R 3,R 4和R 5取代,其中: R1是氨基甲基,(N-(C1-4 - 烷基)氨基)甲基,(N,N-二(C1-4 - 烷基)氨基)甲基或吡啶鎓甲基,R2,R3和R4以及R5(如果存在) ,其可以相同或不同,分别为氢,羟基,C 1-4 - 烷氧基,C 1-4 - 烷氧基)或卤素,或者当R 2连接至 - (CH 2)n - 基团和n为1可以与 - (CH 2)基团连接的吲哚上的2-碳原子一起形成环,及其药学上可接受的盐; 以及这些化合物在药物治疗中的应用。