公开(公告)号：EP0887351A4

公开(公告)日：2001-06-06

申请号：EP97947917

申请日：1997-12-12

申请人： KYOWA HAKKO KOGYO KK

发明人： KANDA YUTAKA ,  ARAI HITOSHI ,  YAMAGUCHI HIROYUKI ,  ASHIZAWA TADASHI ,  IKEDA SHUN-ICHI ,  MURAKATA CHIKARA ,  TAMAOKI TATSUYA

IPC分类号： C07D513/08 ,  C07D513/18 ,  C07D513/20 ,  C07H15/26 ,  C07H17/02 ,  A61K31/425 ,  A61K31/70 ,  C07D519/00 ,  C07H17/00

CPC分类号： C07D513/08 ,  C07H15/26 ,  C07H17/02

摘要： DC 107 derivatives represented by general formula (I) or pharmacologically acceptable salts thereof, each having antibacterial and antitumor activities, wherein R1 represents CO(CR4AR4B)n1[O(CH2)p1]n2OR5, wherein n1 represents an integer of 1 or 2; R?4A and R4B¿ are the same or different and each represents hydrogen or lower alkyl; p1 and n2 are each an integer of 1 to 10; and R5 represents hydrogen, lower alkyl, etc.; or formula (II), (wherein A?1, A2, A3 and A4¿ are the same or different and each represents hydrogen, hydroxy, etc.); R2 represents hydrogen or COR6 (wherein R6 represents lower alkyl, aralkyl, optionally substituted aryl, etc.); R3 represents lower alkyl, lower alkenyl, aralkyl having optionally substituted aryl, alicyclic alkanoyloxy-alkyl, -CH¿2OCOR?7, etc., or R3 may form a bond together with Y; Y forms a bond together with R3 or Z; Z represents hydrogen or may form a bond together with Y; and W represents oxygen or NR8.

公开(公告)号：EP1110960A4

公开(公告)日：2001-12-12

申请号：EP99940590

申请日：1999-08-31

申请人： KYOWA HAKKO KOGYO KK

发明人： HARA MITSUNOBU ,  NAKASHIMA TAKAYUKI ,  KANDA YUTAKA ,  HAMANO MASAMI ,  IKEDA SHUN-ICHI ,  UOSAKI YUKO ,  MIIKE YOKO ,  KANAZAWA JUNJI

IPC分类号： A61K31/00 ,  A61K31/365 ,  C07D407/14 ,  C07H17/08 ,  C07D307/93 ,  A61K31/34 ,  A61K31/70 ,  C07D307/94 ,  C07D407/12 ,  C07D493/08

CPC分类号： C07D407/14 ,  A61K31/00 ,  A61K31/365 ,  C07H17/08

摘要： Apoptosis inducing agents which contain as the active ingredient tetrocarcin derivatives represented by general formula (I) or salts thereof. These agents are useful as drugs for preventing and/or treating diseases caused by the accelerated expression of proteins of the Bc1-2 family such as cancer and AIDS; wherein --- represents a single or double bond; j and k are each 0 or 1; R?1 to R3, R7 to R10 and R14¿ represent each hydrogen, lower alkyl, etc.; R?4, R11, R12, R13 and R15 to R18¿ represent each hydrogen, hydroxy, lower alkyl, etc.; R?5 and R6¿ represent each hydrogen, hydroxy, lower alkyl or (B) (wherein R32 represents formyl, etc.; and R?33 to R35¿ represent each hydrogen, hydroxy, lower alkyl, etc.); and R19 represents hydroxy, lower alkoxy, lower alkanoyloxy, etc.

公开(公告)号：EP1097934A4

公开(公告)日：2001-10-04

申请号：EP99929753

申请日：1999-07-08

申请人： KYOWA HAKKO KOGYO KK

发明人： AKAMA TSUTOMU ,  NAGATA HIROYUKI ,  HASEGAWA ATSUHIRO ,  UE HARUMI ,  TAKAHASHI ISAMI ,  SAITOH YUTAKA ,  MOCHIDA KENICHI ,  IKEDA SHUN-ICHI ,  KANDA YUTAKA

IPC分类号： A61P37/06 ,  C07D471/06 ,  A61K31/47

CPC分类号： C07D471/06

摘要： LK6-A derivatives represented by general formula (I) and pharmacologically acceptable salts thereof, which exhibit immunosuppressive, cytostatic and antitumor effects and so on, wherein R1 is a lower alkanoyl or acryloyl group which may be substituted with, e.g., lower alkoxy, or the like; R2 is hydrogen, halogeno or the like; R2' is hydrogen, or R2' together with R3 forms a bond; R3 is optionally substituted lower alkanoyl, or R3 together with R2' forms a bond; R?4 and R5¿ are each hydrogen, optionally substituted lower alkanoyl or the like; R6 is hydrogen or the like; and R?7 and R8¿ are each hydrogen, optionally substituted lower alkanoyl or the like, with the proviso that LK6-A corresponding to a compound of general formula (I) where R1 is (E)-methoxyacryloyl; R?2, R4, R5, R6 and R7¿ are each hydrogen; R8 is acetyl; and R?2' and R3¿ together form a bond is excepted.

公开(公告)号：EP1227097A4

公开(公告)日：2003-04-02

申请号：EP00969907

申请日：2000-10-19

申请人： KYOWA HAKKO KOGYO KK

发明人： AKAMA TSUTOMU ,  ASAI AKIRA ,  AGATSUMA TSUTOMU ,  NARA SHINJI ,  YAMASHITA YOSHINORI ,  MIZUKAMI TAMIO ,  IKEDA SHUN-ICHI ,  SAITOH YUTAKA ,  KANDA YUTAKA

IPC分类号： A61P31/04 ,  A61P35/00 ,  C07D487/04 ,  C07D487/14 ,  C07D487/16 ,  C07D491/14 ,  C07D491/147 ,  C07D491/16 ,  C07D498/08 ,  A61K31/407 ,  A61K31/4162 ,  A61K31/4439

CPC分类号： C07D487/04 ,  C07D487/14 ,  C07D491/14

摘要： UCS1025 derivatives represented by general formula (I) which have an antitumor activity or an antibacterial activity or pharmacologically acceptable salts thereof, (I) wherein R1 represents hydrogen, lower alkyl, etc.; R2 represents hydrogen, or forms a bond, etc. together with R3 or forms -O(C=O)-, etc. together with R4; R3 represents hydrogen or forms a bond, etc. together with R2; R4 represents hydrogen or forms -(C=O)O-, etc. together with R2; R5 represents hydrogen, or forms a bond together with R6; R6 represents hydroxy, or forms a bond together with R5; R7 represents hydrogen, or forms =O together with R8; R8 represents hydroxy or forms =O together with R7; --- represents a single or double bond; and a represents a single bond (i.e., the two carbon atoms bonded to a form a single bond to each other) or an oxygen atom.

公开(公告)号：EP0755928A4

公开(公告)日：1997-05-28

申请号：EP96901492

申请日：1996-01-31

申请人： KYOWA HAKKO KOGYO KK

发明人： AKAMA TSUTOMU ,  IKEDA SHUN-ICHI ,  ISHIDA HIROYUKI ,  KIMURA UICHIRO ,  GOMI KATSUSHIGE ,  SAITO HIROMITSU

IPC分类号： C07D311/30 ,  A61K31/35

CPC分类号： C07D311/30

摘要： 5-Aminoflavone derivatives represented by general formula (I) or pharmaceutically acceptable salts thereof, wherein X represents substituted lower alkyl, (un)substituted lower alkoxy, or NR1R2 (wherein R?1 and R2¿ represent each independently hydrogen or (un)substituted lower alkyl, or are combined together with N to represent an (un)substituted heterocyclic group); and Y?1 and Y2¿ represent each independently hydrogen, halogeno or lower alkyl.

摘要翻译： 其中X代表取代的低级烷基，（未）取代的低级烷氧基或NR 1 R 2（其中R 1和R 2各自独立地代表氢或（未）取代的），通式（I）代表的5-氨基黄酮衍生物或其药学上可接受的盐， 低级烷基，或者与N一起表示（未）取代的杂环基）。 Y 1和Y 2各自独立地代表氢，卤代或低级烷基。

公开(公告)号：EP0918058A4

公开(公告)日：2001-05-09

申请号：EP97947916

申请日：1997-12-12

申请人： KYOWA HAKKO KOGYO KK

发明人： ARAI HITOSHI ,  KANDA YUTAKA ,  YAMAGUCHI HIROYUKI ,  ASHIZAWA TADASHI ,  MURAKATA CHIKARA ,  IKEDA SHUN-ICHI ,  TAMAOKI TATSUYA

IPC分类号： C07D513/18 ,  C07H15/26 ,  A61K31/425 ,  A61K31/70 ,  C07D519/00

CPC分类号： C07D513/18 ,  C07H15/26

摘要： DC 107 derivatives represented by general formula (I) or pharmacologically acceptable salts thereof, each having antibacterial and antitumor activities, wherein R1 represents hydrogen, lower alkoxyalkyl, aralkyloxyalkyl, lower alkoxyalkoxyalkyl, lower alkoxyalkoxyalkoxyalkyl, aralkyl, tetrahydropyranyl, COR4, etc.; R2 represents hydrogen or COR6; R3 represents -CH¿2COOR?7, phthalimidomethyl, etc.; and W represents oxygen or NR8 (wherein R8 represents hydroxy, lower alkoxy, lower alkenyloxy, aralkyloxy, optionally substituted arylsulfonylamino or lower alkoxycarbonylamino).

公开(公告)号：EP0680950A4

公开(公告)日：1996-02-28

申请号：EP95900905

申请日：1994-11-16

申请人： KYOWA HAKKO KOGYO KK

发明人： IKEDA SHUN-ICHI ,  KIMURA UICHIRO ,  ASHIZAWA TADASHI ,  GOMI KATSUSHIGE ,  SAITO HIROMITSU ,  KASAI MASAJI

IPC分类号： C07D209/12 ,  C07D209/30 ,  C07D401/06 ,  C07D405/06 ,  A61K31/40 ,  A61K31/44

CPC分类号： C07D401/06 ,  C07D209/12 ,  C07D209/30 ,  C07D405/06

摘要： A propenone derivative represented by general formula (I) and a pharmacologically acceptable salt thereof, wherein R1 represents hydrogen, lower alkyl, lower alkanoyl, lower alkoxycarbonyl, lower alkylsulfonyl, aralkyl, (un)substituted aroyl, (un)substituted arylsulfonyl, (un)substituted heteroarylcarbonyl, (un)substituted heteroarylsulfonyl, diglycolyl or a group of formula (a), R2 represents hydrogen, lower alkyl, halogen, (un)substituted aryl or (un)substituted heteroaryl; R3 represents hydrogen, lower alkyl or (un)substituted aryl; and R?4, R5, R6 and R7¿ represent each independently hydrogen, lower alkyl, lower alkoxy, aralkyloxy, hydroxy, nitro, halogen, trifluoromethyl or -NR8R9, wherein R?8 and R9¿ represent each independently hydrogen, lower alkyl, lower alkanoyl, lower alkoxycarbonyl or (un)substituted aroyl.

公开(公告)号：EP0990439A4

公开(公告)日：2004-01-28

申请号：EP98921757

申请日：1998-05-21

申请人： KYOWA HAKKO KOGYO KK ,  FUJI PHOTO FILM CO LTD

发明人： YONETANI YOSHIYUKI ,  TAKAHASHI TAKESHI ,  KANDA YUKO ,  MIZUKAMI TAMIO ,  TAMAOKI TATSUYA ,  IKEDA SHUN-ICHI ,  TAKASHIMA MASANOBU ,  ASANUMA NAOKI ,  INABA TADASHI ,  TAKEUCHI HIROSHI ,  KAWAMOTO HIROSHI ,  TSUKADA YOSHIHISA ,  SATOMURA MASATO ,  KITAGUCHI HIROSHI

IPC分类号： A61P35/00 ,  C07C323/16 ,  C07C323/25 ,  C07C323/40 ,  C07D207/08 ,  C07D211/58 ,  C07D211/60 ,  C07D213/32 ,  C07D215/06 ,  C07D233/54 ,  C07D233/61 ,  C07D239/42 ,  C07D239/58 ,  C07D251/38 ,  C07D277/44 ,  C07D277/56 ,  C07D309/38 ,  C07D317/22 ,  C07D317/28 ,  C07D319/06 ,  C07H5/06 ,  C07H15/18 ,  A61K31/10

CPC分类号： C07D207/08 ,  C07C323/16 ,  C07C323/25 ,  C07C323/40 ,  C07D211/58 ,  C07D211/60 ,  C07D213/32 ,  C07D215/06 ,  C07D233/64 ,  C07D239/42 ,  C07D239/58 ,  C07D251/38 ,  C07D277/56 ,  C07D309/38 ,  C07D317/22 ,  C07D317/28 ,  C07D319/06 ,  C07H5/06 ,  C07H15/18

摘要： Cancer remedies, each containing a compound of the following general formula (I): Ar?1-S-R1-S-Ar2¿ [wherein RP represents a non-metallic connecting group; Ar?1 and Ar2¿ each independently represents aryl or heteroaryl having 1 to 3 hydroxyls which may be substituted with a monovalent group on the ring thereof (and optionally having 1 to 3 substituents other than the hydroxyl on the ring thereof)] or a physiologically acceptable salt thereof; and compounds of the following general formula (XII): Ar?23-S-R22-N(R24)-R23-S-Ar24¿ [wherein R?22 and R23¿ each independently represents a divalent group; R24 represents a monovalent group or atom, or R24 may be bonded to R22 and/or R23 to form a cyclic structure and further bonded to one or two C¿1-4? alkylene groups to form a divalent group; and Ar?23 and Ar24¿ each independently represents aryl or heteroaryl (optionally having 1 to 3 substituents other than hydroxyl on the ring thereof) having 1 to 3 hydroxyls which may be substituted with a monovalent group; excluding specified compounds] and salts thereof.

公开(公告)号：EP1166781A4

公开(公告)日：2002-08-21

申请号：EP00900834

申请日：2000-01-20

申请人： KYOWA HAKKO KOGYO KK

发明人： YAMAGUCHI HIROYUKI ,  ASAI AKIRA ,  MIZUKAMI TAMIO ,  YAMASHITA YOSHINORI ,  AKINAGA SHIRO ,  IKEDA SHUN-ICHI ,  KANDA YUTAKA

IPC分类号： A61K38/00 ,  A61P35/00 ,  A61P43/00 ,  C07C229/46 ,  C07C237/22 ,  C07C271/22 ,  C07C327/22 ,  C07C327/28 ,  C07D305/12 ,  C07K5/06 ,  A61K31/215 ,  A61K31/27 ,  A61K31/337 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  C07C237/10

CPC分类号： C07K5/06026 ,  A61K38/00 ,  C07C229/46 ,  C07C237/22 ,  C07C271/22 ,  C07C327/22 ,  C07C327/28 ,  C07C2601/02 ,  C07D305/12 ,  C07K5/06191

摘要： Proteasome inhibitors containing as the active ingredient carboxylic acid derivatives represented by general formula (I) or pharmacologically acceptable salts thereof: wherein m and n are each independently an integer of 0 to 10; p is 0 or 1; R1 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, or the like; and R2 is hydrogen, COR13 or CH¿2OR?3a, or alternatively R?1 and R2¿ together represent formula (II), wherein X1 is a linkage, substituted or unsubstituted alkylene, substituted or unsubstituted cycloalkylene, or the like; X2 is oxygen, sulfur, or NR17; R3 is as defined for R?3a; and R4¿ is hydroxyl, mercapto, substituted or unsubstituted alkoxy, or the like, or alternatively R?3 and R4 ¿together represent a linkage; and R5 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or the like.

公开(公告)号：EP0812825A4

公开(公告)日：1999-04-07

申请号：EP96940153

申请日：1996-11-29

申请人： KYOWA HAKKO KOGYO KK

发明人： IKEDA SHUN-ICHI ,  KANAZAWA JUNJI ,  SASAKI KIMIHITO ,  NUKUI ETSUKO ,  OKABE MASAMI ,  GOMI KATSUSHIGE ,  SAITO HIROMITSU ,  SATO SOICHIRO

IPC分类号： C07D209/12 ,  C07F7/08 ,  C07H15/24 ,  A61K31/40 ,  A61K31/70 ,  C07F7/10 ,  C07H15/26

CPC分类号： C07F7/0812 ,  C07D209/12 ,  C07H15/24

摘要： Propenone derivatives represented by general formula (I) or pharmacologically acceptable salts thereof: wherein R1 represents substituted lower alkyl or YR5 (where Y represents S or O and R5 represents optionally substituted lower alkyl, optionally substituted aryl, optionally substituted aromatic heterocyclic group, or optionally substituted cyclic ether residue); R?2 and R3¿ may be the same or different and each represents hydrogen, lower alkyl, or optionally substituted aralkyl, or R?2 and R3¿ may be bonded to each other to thereby form optionally substituted methylene or ethylene; R4 represents hydrogen, hydroxy, lower alkyl, optionally substituted aralkyl, lower alkoxy, optionally substituted aralkyloxy, or halogeno; and X represents optionally substituted indolyl.