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1. 发明公开

EP1908755A1 THERAPEUTIC AGENT FOR RESTENOSIS 审中-公开
标题翻译：治疗MITTEL GEGEN RESTENOSE
公开(公告)号：EP1908755A1
公开(公告)日：2008-04-09
申请号：EP06767189.1
申请日：2006-06-22
申请人： KYOWA HAKKO KOGYO CO., LTD. , Fujifilm Corporation
发明人： NAKAI, Ryuichiro , SHIMOIKE, Emi , KUSAKA, Hideaki , MURAKATA, Chikara , YAMASHITA, Yoshinori
IPC分类号： C07D285/135 , A61K31/433 , A61P9/00 , C07D285/12
CPC分类号： A61K31/433 , C07D285/12 , C07D285/135 , C07D417/12 , C07D491/10
摘要： A therapeutic and/or prophylactic agent for restenosis, which comprises a thiadiazoline derivative represented by the general formula (0), or a pharmaceutically acceptable salt thereof:

[wherein, n represents an integer of 1 to 3, R 0 represents aryl, -NR 1 CONR 2 (wherein R 1 represents a hydrogen atom or the like, and R 2 represents lower alkyl or the like) or the like, R 3 represents lower alkyl, R 4 represents a hydrogen atom or the like, and R 5 represents aryl or the like].
摘要翻译：用于再狭窄的治疗和/或预防剂，其包含由通式（0）表示的噻二唑啉衍生物或其药学上可接受的盐：[其中，n表示1〜3的整数，R 0表示芳基，-NR 1 CONR 2（其中R 1表示氢原子等，R 2表示低级烷基等）等，R 3表示低级烷基，R 4表示氢原子等，R 5表示芳基等等]。

2. 发明授权

EP0657412B1 SAINTOPIN DERIVATIVE 失效
标题翻译： SAINTOPIN DERIVATE
公开(公告)号：EP0657412B1
公开(公告)日：1998-02-04
申请号：EP94900271.1
申请日：1993-11-17
申请人： Kyowa Hakko Kogyo Co., Ltd.
发明人： NAKANO, Hirofumi , FUJII, Noboru , YAMASHITA, Yoshinori , SAITOH, Yutaka , AGATSUMA, Tsutomu , ANDO, Katsuhiko , NISHIIE, Yasushi , KITA, Katsunori , MORISHIMA, Naoki , GOMI, Katsushige
IPC分类号： C07C50/36 , C12P29/00 , A61K31/65 , C12N1/14
CPC分类号： C07C305/26 , C07C50/38 , C07C305/22 , C12P29/00
摘要： A saintopin E derivative represented by general formula (I) and useful as an antibacterial and antitumor agent, wherein when R represents hydrogen, then R represents SO2OH (in the case of UCE1022), while when R represents acetyl, then R represents hydrogen (in the case of saintopin E).

3. 发明公开

EP0791581A1 COMPOUNDS UCH 15 失效
标题翻译：化合物UCH 15
公开(公告)号：EP0791581A1
公开(公告)日：1997-08-27
申请号：EP96930356.9
申请日：1996-09-11
申请人： KYOWA HAKKO KOGYO CO., LTD.
发明人： MIZUKAMI, Tamio , ASAI, Akira , YAMASHITA, Yoshinori , NAKANO, Hirofumi , KAKITA, Shingo , UOSAKI, Youichi , OCHIAI, Keiko , ASHIZAWA, Tadashi , MIHARA, Akira
IPC分类号： C07D207/34
CPC分类号： C07D207/34
摘要： This invention relates to UCH15 compounds of the formula (I):
wherein R 1 represents a hydrogen atom or a hydroxyl group.
摘要翻译：本发明涉及式（I）的UCH15化合物：其中R1代表氢原子或羟基。

4. 发明授权

EP0823429B1 RADICICOL DERIVATIVES 失效
标题翻译： RADICICOLS的衍生物
公开(公告)号：EP0823429B1
公开(公告)日：2000-07-12
申请号：EP96912263.9
申请日：1996-04-26
申请人： KYOWA HAKKO KOGYO CO., Ltd.
发明人： AGATSUMA, Tsutomu , SAITOH, Yutaka , YAMASHITA, Yoshinori , MIZUKAMI, Tamio , AKINAGA, Shiro , GOMI, Katsushige , AKASAKA, Kazuhito , TAKAHASHI, Isami
IPC分类号： C07D313/00 , C07D493/04 , A61K31/365
CPC分类号： C07D313/00
摘要： Radicicol derivatives represented by general formula (I) or pharmacologically acceptable salts thereof, wherein R?1 and R2¿ may be the same or different and each represents hydrogen, alkanoyl, alkenoyl or tert-butyldimethylsilyl; and (1) when X represents halogeno, then Y represents oxygen or R?4-O-N (R4¿ being hydrogen or (un)substituted lower alkyl) and R3 represents hydrogen, alkanoyl, alkenoyl, etc.; while (2) when X is combined with R3 to represent a single bond, Y represents R?4B-O-N (R4B¿ being the same as R4). The derivatives have a tyrosine kinase inhibitory activity and thus have various pharmacological activities such as antitumor, antibacterial and immunosuppressive effects.

5. 发明公开

EP0657412A1 SAINTOPIN DERIVATIVE 失效
标题翻译： SAINTOPIN DERIVATE。
公开(公告)号：EP0657412A1
公开(公告)日：1995-06-14
申请号：EP94900271.1
申请日：1993-11-17
申请人： KYOWA HAKKO KOGYO CO., LTD.
发明人： NAKANO, Hirofumi , FUJII, Noboru , YAMASHITA, Yoshinori , SAITOH, Yutaka , AGATSUMA, Tsutomu , ANDO, Katsuhiko , NISHIIE, Yasushi , KITA, Katsunori , MORISHIMA, Naoki , GOMI, Katsushige
IPC分类号： C07C50/36 , C12P29/00 , A61K31/65 , C12N1/14
CPC分类号： C07C305/26 , C07C50/38 , C07C305/22 , C12P29/00
摘要： A saintopin E derivative represented by general formula (I) and useful as an antibacterial and antitumor agent, wherein when R¹ represents hydrogen, then R² represents SO₂OH (in the case of UCE1022), while when R¹ represents acetyl, then R² represents hydrogen (in the case of saintopin E).
摘要翻译：由通式（I）表示的saintopin E衍生物，可用作抗菌和抗肿瘤剂，其中当R 1表示氢时，R 2表示SO 2 OH（在UCE1022的情况下），而当R 1表示氢时，表示乙酰基，则R 2表示氢（在saintopin E的情况下）。

6. 发明授权

EP0791581B1 UCH15 COMPOUNDS 失效
标题翻译： UCH-14连接
公开(公告)号：EP0791581B1
公开(公告)日：2001-10-10
申请号：EP96930356.9
申请日：1996-09-11
申请人： KYOWA HAKKO KOGYO CO., LTD.
发明人： MIZUKAMI, Tamio , ASAI, Akira , YAMASHITA, Yoshinori , NAKANO, Hirofumi , KAKITA, Shingo , UOSAKI, Youichi , OCHIAI, Keiko , ASHIZAWA, Tadashi , MIHARA, Akira
IPC分类号： C07D207/34 , A61K31/40
CPC分类号： C07D207/34
摘要： Compounds UCH 15 represented by general formula (I), wherein R1 represents hydrogen or hydroxy.

7. 发明公开

EP1109796A1 TELOMERASE INHIBITORS AND METHODS OF THEIR USE 审中-公开
标题翻译：端粒酶抑制剂和方法及其用途
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
申请人： Geron Corporation , KYOWA HAKKO KOGYO CO., LTD.
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.

8. 发明公开

EP0823429A1 RADICICOL DERIVATIVES 失效
标题翻译： DERIVATE DES RADICICOLS
公开(公告)号：EP0823429A1
公开(公告)日：1998-02-11
申请号：EP96912263.9
申请日：1996-04-26
申请人： Kyowa Hakko Kogyo Co., Ltd.
发明人： AGATSUMA, Tsutomu , SAITOH, Yutaka , YAMASHITA, Yoshinori , MIZUKAMI, Tamio , AKINAGA, Shiro , GOMI, Katsushige , AKASAKA, Kazuhito , TAKAHASHI, Isami
IPC分类号： C07D313/00 , C07D493/04 , A61K31/365
CPC分类号： C07D313/00
摘要： The present invention relates to radicicol derivatives represented by the following formula (I) or pharmacologically acceptable salts thereof:
wherein R 1 and R 2 are the same or different and each represents hydrogen, alkanoyl, alkenoyl or tert-butyldimethylsilyl; (1) when X represents halogen, Y represents an oxygen atom or R 4 -O-N (wherein R 4 represents hydrogen or substituted or unsubstituted lower alkyl); and R 3 represents hydrogen, alkanoyl, alkenoyl or the like; and (2) when X and R 3 are combined with each other to represent a single bond; Y represents R 4B -O-N (wherein R 4B has the same meaning as R 4 ). The radicicol derivatives of the present invention demonstrate tyrosine kinase inhibition activity and pharmacological activities such as antitumor, antimicrobial or immunosuppression effects.
摘要翻译：本发明涉及由下式（I）表示的根赤壳菌素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，各自代表氢，链烷酰基，烯酰基或叔 - 甲基硅烷基; （1）当X表示卤素时，Y表示氧原子或R 4 -O-N（其中R 4表示氢或取代或未取代的低级烷基）; 和R 3代表氢，烷酰基，烯酰基等; 和（2）当X和R 3彼此结合以表示单键时; Y表示R 4B-N-N（其中R 4具有与R 4相同的含义）。本发明的根皮霉素衍生物显示出酪氨酸激酶抑制活性和药理活性，如抗肿瘤，抗微生物或免疫抑制作用。

9. 发明授权

EP1616866B1 M-STAGE KINESIN INHIBITOR 有权
标题翻译： M-STAGE-驱动蛋白抑制剂
公开(公告)号：EP1616866B1
公开(公告)日：2011-12-14
申请号：EP04728012.8
申请日：2004-04-16
申请人： Kyowa Hakko Kirin Co., Ltd. , FUJIFILM Corporation
发明人： MURAKATA, Chikara , YAMASHITA, Yoshinori , NAKAI, Ryuichiro , AKASAKA, Kazuhito , INO, Yoji , KATO, Kazuhiko , KITAMURA, Yushi
IPC分类号： C07D285/12 , C07D417/04 , C07D417/12 , A61K31/433 , A61K31/4439 , A61K31/5377 , A61K31/506 , A61P9/04 , A61P9/10 , A61P19/02 , A61P37/02
CPC分类号： C07D285/13 , A61K31/433 , A61K31/4439 , A61K31/506 , A61K31/5377 , C07D285/135
摘要： An M-stage kinesin Eg5 inhibitor which contains as an active ingredient either a thiadiazoline derivative represented by the general formula (I): [wherein R1 represents hydrogen, etc.; R2 represents hydrogen, -C(=W)R6 (wherein W represents oxygen or sulfur and R6 represents (un)substituted lower alkyl, etc.), etc.; R3 represents -C(=Z)R19 (wherein Z represents oxygen or sulfur and R19 represents (un)substituted lower alkyl, etc.) etc.; R4 represents (un)substituted lower alkyl, etc.; and R5 represents (un)substituted aryl, etc.] or a pharmacologically acceptable salt of the derivative.

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