公开(公告)号：EP0702014A4

公开(公告)日：1996-08-07

申请号：EP95913398

申请日：1995-03-31

申请人： KYOWA HAKKO KOGYO KK

发明人： AMISHIRO NOBUYOSHI ,  NAGAMURA SATORU ,  SAITO HIROMITSU ,  KOBAYASHI EIJI ,  OKAMOTO AKIHIKO ,  GOMI KATSUSHIGE

IPC分类号： C07D487/04 ,  C07D487/10

CPC分类号： C07D487/04 ,  C07D487/10

摘要： A DC-89 derivative represented by general formula (1) or (2) or a pharmacologically acceptable salt thereof, having an excellent antitumor activity and useful as an antitumor drug, wherein X represents Cl or Br; R represents hydrogen or COR1; and W represents a group of general formula (3) or (4).

摘要翻译： 由通式（1）或（2）表示的DC-89衍生物或其药理学上可接受的盐，具有优异的抗肿瘤活性并且可用作抗肿瘤药物，其中X代表Cl或Br; R代表氢或COR1; W表示通式（3）或（4）的基团。

公开(公告)号：EP1284272A4

公开(公告)日：2003-09-10

申请号：EP01922046

申请日：2001-04-24

申请人： KYOWA HAKKO KOGYO KK

发明人： INO YOJI ,  AMISHIRO NOBUYOSHI ,  MIYATA MAYUMI ,  AGATSUMA TSUTOMU ,  HAYASHI KOZUE ,  TAKAHASHI TAKESHI ,  AKINAGA SHIRO ,  MURAKATA CHIKARA

IPC分类号： A61P5/24 ,  A61P5/32 ,  A61P13/08 ,  A61P15/00 ,  A61P35/00 ,  A61P43/00 ,  C07J41/00 ,  C07J43/00 ,  A61K31/56 ,  A61K31/58

CPC分类号： C07J43/00 ,  C07J41/00

摘要： Steroid sulfatase inhibitors containing as the active ingredient estra-1,3,5(10)-triene derivatives represented by the following general formula (I) or pharmacologically acceptable salts thereof: (I) wherein R?1 and R2¿ are the same or different and each represents hydrogen, lower alkyl, etc.; R3 represents hydrogen, etc.; R4 represents hydrogen, etc.; R5 represents hydrogen, etc.; and R6 represents cyano, amino, COR53 (wherein R53 represents substituted lower alkyl, etc.), optionally substituted aryl, an optionally substituted heterocycle, etc.

公开(公告)号：EP0889042A4

公开(公告)日：1999-10-06

申请号：EP97909629

申请日：1997-10-24

申请人： KYOWA HAKKO KOGYO KK

发明人： INO YOJI ,  AMISHIRO NOBUYOSHI ,  MIYATA MAYUMI ,  MURAKATA CHIKARA ,  OGAWA HARUMI ,  AKIYAMA TADAKAZU ,  AKINAGA SHIRO ,  SOGA SHIROH ,  SHIOTSU YUKIMASA

IPC分类号： C07D313/00 ,  C07D493/04 ,  A61K31/365 ,  A61K31/40 ,  A61K31/44 ,  A61K31/445 ,  A61K31/505 ,  A61K31/535 ,  A61K31/54 ,  A61K31/55 ,  C07F7/10

CPC分类号： C07D493/04 ,  C07D313/00

摘要： Radicicol derivatives having an antityrosine kinase activity and represented by general formula (I) or pharmacologically acceptable salts thereof, wherein R?1 and R2¿ are the same or different and each represents hydrogen, alkanoyl, alkenoyl, tert-butyldiphenylsilyl, or tert-butyldimethylsilyl; R3 represents Y- R5 {where Y represents optionally substituted alkylene, R5 represents CONR6R7 (where R6 represents hydrogen, hydroxy, optionally substituted lower alkyl, optionally substituted higher alkyl, etc. and R7 represents hydroxy, substituted lower alkyl, etc.), CO¿2R?12 (where R12 represents substituted lower alkyl, optionally substituted higher alkyl, etc.), etc.}; X represents halogeno or is bonded to R4 to represent a single bond; and R4 is bonded to X to represent a single bond or represents hydrogen alkanoyl, etc.

公开(公告)号：EP1201668A4

公开(公告)日：2003-05-21

申请号：EP00946296

申请日：2000-07-13

申请人： KYOWA HAKKO KOGYO KK

发明人： KANAI FUMIHIKO ,  AMISHIRO NOBUYOSHI ,  KITAMURA YUSHI ,  MURAKATA CHIKARA ,  AKIYAMA TADAKAZU ,  AKINAGA SHIRO ,  FUSE EIICHI ,  KUWABARA TAKASHI ,  YASOSHIMA KENICHI

IPC分类号： A61K31/553 ,  A61P35/00 ,  A61P43/00 ,  C07D498/22 ,  A61K31/55

CPC分类号： C07D498/22 ,  A61K31/553

摘要： Antitumor agents containing as the active ingredient staurosporin derivatives represented by general formula (I) or pharmacologically acceptable salts thereof wherein R1 is hydrogen, hydroxyl, or lower alkoxy; R?2 and R3¿ are each independently hydrogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkenyl, substituted or unsubstituted lower alkynyl, substituted or unsubstituted aryl, a substituted or unsubstituted heterocyclic group, halogeno, nitro, formyl, or the like; R4 is hydrogen or the like; and R?5 is NR11AR12A¿ (wherein R?11A and R12A¿ are each hydrogen, substituted or unsubstituted lower alkyl, or the like), with the proviso that both R?2 and R3¿ are not 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，R 4表示氢; 等等，R 5表示NR 11A和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 >不是同时氢。

公开(公告)号：EP0786252A4

公开(公告)日：1998-01-07

申请号：EP95932191

申请日：1995-09-20

申请人： KYOWA HAKKO KOGYO KK

发明人： SAITO HIROMITSU ,  AMISHIRO NOBUYOSHI ,  NAGAMURA SATORU ,  KOBAYASHI EIJI ,  OKAMOTO AKIHIKO ,  GOMI KATSUSHIGE ,  YAMASHITA KINYA ,  SATO KIYOSHI ,  NAKAKURA MASASHI ,  HAYAKAWA EIJI

IPC分类号： C07D487/04 ,  C07D487/10 ,  A61K31/40

CPC分类号： C07D487/04 ,  C07D487/10

摘要： An antitumor agent against drug-fast tumors containing a compound represented by general formula (2) or (a) or a pharmacologically acceptable salt thereof as the active ingredient; wherein X represents Cl or Br; and R represents NR1R2 (wherein R?1 and R2¿ represent each independently hydrogen or C¿1?-C4 linear or branched alkyl) or a group of formula (b) (wherein R?3¿ represents CH¿2? or N-CH3). The agent has an excellent antitumor activity against drug-insensitive tumors and is useful as an antitumor agent against drug-fast tumors.

公开(公告)号：EP0705833A4

公开(公告)日：1997-04-02

申请号：EP95916020

申请日：1995-04-20

申请人： KYOWA HAKKO KOGYO KK

发明人： AMISHIRO NOBUYOSHI ,  NAGAMURA SATORU ,  SAITO HIROMITSU ,  KOBAYASHI EIJI ,  OKAMOTO AKIHIKO ,  GOMI KATSUSHIGE

IPC分类号： C07D487/04

CPC分类号： C07D487/04

摘要： A DC-89 derivative represented by general formula (I) or a pharmacologically acceptable salt thereof, wherein X represents Cl or Br; R represents (un)substituted alkyl, (un)substituted aralkyl, COR1 or SO¿2R?7; and Y represents the group (a) or (b). The compound has an excellent antitumor activity and is useful as an antitumor drug.