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1. 发明申请

US20040053990A1 Radicicol derivatives 审中-公开
标题翻译：蓝霉素衍生物
公开(公告)号：US20040053990A1
公开(公告)日：2004-03-18
申请号：US10629655
申请日：2003-07-30
申请人： KYOWA HAKKO KOGYO CO., LTD
发明人： Yoji Ino , Nobuyoshi Amishiro , Mayumi Miyata , Chikara Murakata , Harumi Ogawa , Tadakazu Akiyama , Shiro Akinaga , Shiro Soga , Yukimasa Shiotsu
IPC分类号： A61K031/695 , A61K031/365 , A61K031/4433 , A61K031/4025 , C07D313/20 , C07D45/02
CPC分类号： C07D493/04 , C07D313/00
摘要： Radicicol derivatives represented by the following formula (I) having tyrosine kinase inhibition activity or pharmacologically acceptable salts thereof: 1 wherein R1 and R2 are the same or different, and each represents hydrogen, alkanoyl, alkenoyl, tert-butyldiphenylsilyl or tert-butyldimethylsilyl; R3 represents YnullR5 nullwherein Y represents substituted or unsubstituted alkylene; and R5 represents CONR6R7 (wherein R6 represents hydrogen, hydroxyl, substituted or unsubstituted lower alkyl, substituted or unsubstituted higher alkyl, and the like; R7 represents hydroxyl, substituted lower alkyl, and the like), CO2R12 (wherein R12 represents substituted lower alkyl, substituted or unsubstituted higher alkyl, and the like), and the likenull and the like; X represents halogen or is combined together with R4 to represent a single bond; and R4 is combined together with X to represent a single bond, or represents hydrogen, alkanoyl, and the like.
摘要翻译：由下式（I）表示的具有酪氨酸激酶抑制活性的衍生物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，各自表示氢，链烷酰基，烯酰基，叔丁基二苯基甲硅烷基或叔丁基二甲基甲硅烷基; R 3表示Y-R 5 {其中Y表示取代或未取代的亚烷基; 并且R 5表示CONR 6 R 7（其中R 6表示氢，羟基，取代或未取代的低级烷基，取代或未取代的高级烷基等; R 7表示羟基，取代的较低级烷基等），CO 2 R 12（其中R 12表示取代的低级烷基，取代或未取代的高级烷基等）等}等; X表示卤素或与R 4结合以表示单键; 和R 4与X一起表示单键，或表示氢，烷酰基等。

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