公开(公告)号：US06806266B1

公开(公告)日：2004-10-19

申请号：US10030618

申请日：2002-01-11

申请人： Fumihiko Kanai ,  Nobuyoshi Amishiro ,  Yushi Kitamura ,  Chikara Murakata ,  Tadakazu Akiyama ,  Shiro Akinaga ,  Eiichi Fuse ,  Takashi Kuwabara ,  Kenichi Yasoshima

发明人： Fumihiko Kanai ,  Nobuyoshi Amishiro ,  Yushi Kitamura ,  Chikara Murakata ,  Tadakazu Akiyama ,  Shiro Akinaga ,  Eiichi Fuse ,  Takashi Kuwabara ,  Kenichi Yasoshima

IPC分类号： C07D49822

CPC分类号： C07D498/22 ,  A61K31/553

摘要： The present invention provides an antitumor agent comprising a staurosporin derivative or a pharmaceutically acceptable salt thereof, as an active ingredient, which is represented by the general formula (I): wherein R1 represents hydrogen, hydroxy or lower alkoxy, R2 and R3 are the same or different and represent hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted lower alkenyl, substituted or unsubstituted lower alkynyl, substituted or unsubstituted aryl, a substituted or unsubstituted heterocyclic group, halogen, nitro, formyl, etc., R4 represents hydrogen, etc., R5 represents NR11AR12A (wherein R11A and R12A represent hydrogen, substituted or unsubstituted lower alkyl, etc.), provided that R2 and R3 are not simultaneously hydrogen.

摘要翻译： 本发明提供包含星形孢菌素衍生物或其药学上可接受的盐作为活性成分的抗肿瘤剂，其由通式（I）表示：其中R 1表示氢，羟基或低级烷氧基，R 2 和R 3相同或不同，表示氢，取代或未取代的烷基，取代或未取代的低级烯基，取代或未取代的低级炔基，取代或未取代的芳基，取代或未取代的杂环基，卤素，硝基，甲酰基， 等等，R 4表示氢等，R 5表示NR 11A R 12A（其中R 11A和R 12A表示氢，取代或未取代的低级烷基等）， 条件是R 2和R 3不同时为氢。