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公开(公告)号：EP0755928B1
公开(公告)日：2002-04-10
申请号：EP96901492.7
申请日：1996-01-31
发明人： AKAMA, Tsutomu , IKEDA, Shun-ichi , ISHIDA, Hiroyuki Oakwood Apartments D205 , KIMURA, Uichiro , GOMI, Katsushige , SAITO, Hiromitsu
IPC分类号： C07D311/30 , A61K31/35
CPC分类号： C07D311/30
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公开(公告)号：EP0755928A1
公开(公告)日：1997-01-29
申请号：EP96901492.7
申请日：1996-01-31
发明人： AKAMA, Tsutomu , IKEDA, Shun-ichi , ISHIDA, Hiroyuki Oakwood Apartments D205 , KIMURA, Uichiro , GOMI, Katsushige , SAITO, Hiromitsu
IPC分类号： C07D311/30 , A61K31/35
CPC分类号： C07D311/30
摘要： The present invention relates to a 5-aminoflavone derivative represented by the formula (I):
wherein X represents substituted lower alkyl, unsubstituted or substituted lower alkoxy, or NR 1 R 2 (wherein R 1 and R 2 are the same or different and represent hydrogen, unsubstituted or substituted lower alkyl, or R 1 and R 2 are taken together to form an unsubstituted or substituted heterocyclic group containing the sandwiched nitrogen atom in the ring), and Y 1 and Y 2 are the same or different and represent hydrogen, halogen, or lower alkyl, or a pharmaceutically acceptable salt thereof.摘要翻译： 本发明涉及由式（I）表示的5-氨基黄酮衍生物：其中X代表取代的低级烷基，未取代或取代的低级烷氧基或NR 1 R 2（其中R 1和R 2相同或不同，代表氢，未取代或取代的 低级烷基或R 1和R 2一起形成在环中含有夹心的氮原子的未取代或取代的杂环基），并且Y 1和Y 2相同或不同且表示氢，卤素或低级烷基或其药学上可接受的盐 其可接受的盐。
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公开(公告)号：EP1097934B1
公开(公告)日：2004-10-13
申请号：EP99929753.4
申请日：1999-07-08
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： C07D471/06 , A61K31/47
CPC分类号： C07D471/06
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公开(公告)号：EP1373243A1
公开(公告)日：2004-01-02
申请号：EP01923228.9
申请日：2001-04-06
申请人： THE GOVERNMENT OF THE UNITED STATES OF AMERICA, as represented by THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES , KYOWA HAKKO KOGYO CO., LTD.
IPC分类号： C07D311/30 , A61K31/35 , A61P35/00
CPC分类号： C07D311/30
摘要： The invention provides an aminoflavone having formula (I), wherein each of R?1 and R2¿ is H, COCH¿2-R?7, wherein R7 is amino, alkylamino, dialkylamino, or alkyl- or dialkylaminoalkyl, or an α-amino acid residue, provided that at least one of R1 or R2 is other than H, and R3 is H, branched or straight-chain alkyl, hydroxyalkyl, alkanoyloxyalkyl, alkanoyloxy, alkoxy, or alkoxyalkyl, or pharmaceutically acceptable salts thereof. The present invention also provides a pharmaceutical composition comprising an aminoflavone as described above, and a method of inhibiting the growth of a tumor in a host by administering a tumor growth-inhibiting amount of an aminoflavone compound having the formula as described above.
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公开(公告)号：EP1109796A1
公开(公告)日：2001-06-27
申请号：EP00950282.4
申请日：2000-06-30
发明人： CHIN, Allison, C. , HOLCOMB, Ryan , PIATYSZEK, Mieczyslaw, A. , SINGH, Upinder , TOLMAN, Richard, L. , AKAMA, Tsutomu , KANDA, Yutaka , ASAI, Akira , YAMASHITA, Yoshinori , ENDO, Kaori , YAMAGUCHI, Hiroyuki
IPC分类号： C07D277/34 , C07D277/36 , C07D417/06 , C07D417/10 , C07D513/04 , A61K31/425 , A61K31/44
CPC分类号： C07D417/06 , A61K31/426 , A61K31/4439 , A61K31/506 , C07D277/34 , C07D277/36 , C07D417/10 , C07D513/04
摘要： Thiazolidinedione compounds, compositions, and methods of inhibiting telomerase activity in vitro and treatmnet of telomerase mediated conditions or diseases ex vivo and in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of conditions or diseases mediated by telomerase activity, such as in the treatment of cancer. Also disclosed are novel methods for assaying or screening for inhibitors of telomerase activity.
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公开(公告)号：EP1373243B1
公开(公告)日：2005-06-22
申请号：EP01923228.9
申请日：2001-04-06
申请人： THE GOVERNMENT OF THE UNITED STATES OF AMERICA, as represented by THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES , KYOWA HAKKO KOGYO CO., LTD.
IPC分类号： C07D311/30 , A61K31/35 , A61P35/00
CPC分类号： C07D311/30
摘要： The invention provides an aminoflavone having formula (I), wherein each of R?1 and R2¿ is H, COCH¿2-R?7, wherein R7 is amino, alkylamino, dialkylamino, or alkyl- or dialkylaminoalkyl, or an α-amino acid residue, provided that at least one of R1 or R2 is other than H, and R3 is H, branched or straight-chain alkyl, hydroxyalkyl, alkanoyloxyalkyl, alkanoyloxy, alkoxy, or alkoxyalkyl, or pharmaceutically acceptable salts thereof. The present invention also provides a pharmaceutical composition comprising an aminoflavone as described above, and a method of inhibiting the growth of a tumor in a host by administering a tumor growth-inhibiting amount of an aminoflavone compound having the formula as described above.
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公开(公告)号：EP1227097A1
公开(公告)日：2002-07-31
申请号：EP00969907.5
申请日：2000-10-19
发明人： AKAMA, Tsutomu , ASAI, Akira Pharm. Res. Kyowa Hakko Kogyo Co. Ltd , AGATSUMA, Tsutomu Tokyo Res. Kyowa Hakko Kogyo Ltd , NARA, Shinji Pharm. Res. Kyowa Hakko Kogyo Co.Ltd , YAMASHITA, Yoshinori Kyowa Hakko Kogyo Co. Ltd , MIZUKAMI, Tamio Kyowa Hakko Kogyo Co.Ltd , IKEDA, Shun-ichi Sakai KyowaHakko Kogyo Co. Ltd , SAITOH, Yutaka Fuji Kyowa Hakko Kogyo Co., Ltd , KANDA, Yutaka Pharm. R. Kyowa Hakko Kogyo Co. Ltd
IPC分类号： C07D487/04 , C07D487/14 , C07D487/16 , C07D491/147 , C07D491/16 , A61K31/407 , A61K31/4162 , A61K31/4439 , A61P31/04 , A61P35/00
CPC分类号： C07D487/04 , C07D487/14 , C07D491/14
摘要： UCS 1025 derivatives having antitumor activity or antibacterial activity which are represented by formula (I):
wherein R 1 represents hydrogen, lower alkyl, etc.; R 2 represents hydrogen, or is combined with R 3 to represent a bond, etc., or is combined with R 4 to represent -O(C=O)-, etc.; R 3 represents hydrogen, etc., or is combined with R 2 to represent a bond, etc.; R 4 represents hydrogen, etc., or is combined with R 2 to represent -(C=O)O-, etc.; R 5 represents hydrogen or is combined with R 6 to represent a bond; R 6 represents hydrogen, etc., or is combined with R 5 to represent a bond; R 7 represents hydrogen or is combined with R 8 to represent =O; R 8 represents hydroxy or is combined with R 7 to represent =O; ---- represents a single bond or a double bond, and a represents a single bond (two carbon atoms to which a is bound are combined to form a single bond) or an oxygen atom, or pharmaceutically acceptable salts thereof.摘要翻译： 由式（I）表示的具有抗肿瘤活性或抗菌活性的UCS 1025衍生物：其中R 1表示氢，低级烷基等; R 2表示氢，或与R 3结合以表示键等，或与R 4结合以表示-O（C = O） - 等; R 3表示氢等，或与R 2结合以代表键等; R 4表示氢等，或与R 2结合代表 - （C = O）O-等; R 5表示氢或与R 6结合以表示键; R 6表示氢等，或与R 5结合以表示键; R 7代表氢或与R 8结合代表= O; R 8表示羟基或与R 7结合代表= O; ----表示单键或双键，a表示单键（键合有两个碳原子结合形成单键）或氧原子，或其药学上可接受的盐。
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公开(公告)号：EP1097934A1
公开(公告)日：2001-05-09
申请号：EP99929753.4
申请日：1999-07-08
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： 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 R 1 is a lower alkanoyl or acryloyl group which may be substituted with, e.g., lower alkoxy, or the like; R 2 is hydrogen, halogeno or the like; R 2' is hydrogen, or R 2' together with R 3 forms a bond; R 3 is optionally substituted lower alkanoyl, or R 3 together with R 2' forms a bond; R 4 and R 5 are each hydrogen, optionally substituted lower alkanoyl or the like; R 6 is hydrogen or the like; and R 7 and R 8 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 R 1 is (E)-methoxyacryloyl; R 2 , R 4 , R 5 , R 6 and R 7 are each hydrogen; R 8 is acetyl; and R 2' and R 3 together form a bond is excepted.
摘要翻译： 具有通式（I）表示的LK6-A衍生物及其药理学上可接受的盐，其具有免疫抑制，细胞抑制和抗肿瘤作用等，其中R 1为低级烷酰基或丙烯酰基，其可被例如较低级 烷氧基等; R 2是氢，卤素等; R 2是氢，或R 2与R 3一起形成键; R 3是任选取代的低级烷酰基，或R 3与R 2'一起形成键; R 4和R 5各自为氢，任选取代的低级烷酰基等; R 6是氢等; R 7和R 8各自为氢，任选取代的低级烷酰基等，条件是对应于通式（I）的化合物的LK6-A，其中R 1为（E） - 甲氧基丙烯酰基 ; R 2，R 4，R 5，R 6和R 7各自为氢; R 8是乙酰基; 和R 2'和R 3一起形成键。
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