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1. 发明授权

EP0673937B1 BICYCLIC HETEROCYCLIC SULFONAMIDE AND SULFONIC ESTER DERIVATIVES 失效
标题翻译：二环杂环磺酰胺和磺酸
公开(公告)号：EP0673937B1
公开(公告)日：2003-11-26
申请号：EP94926372.7
申请日：1994-09-08
申请人： Eisai Co., Ltd.
发明人： YOSHINO, Hiroshi , OWA, Takashi , OKAUCHI, Tatsuo , YOSHIMATSU, Kentaro , SUGI, Naoko , NAGASU, Takeshi , OZAWA, Yoichi , KOYANAGI, Nozomu , KITO, Kyosuke
IPC分类号： C07D409/12 , C07D471/04 , A61K31/40 , A61K31/415 , A61K31/435 , A61K31/635 , C07D209/08 , C07D209/30 , C07D209/34 , C07D231/56 , C07D209/12 , C07D209/42 , C07D401/12 , C07D405/12 , C07D403/12
CPC分类号： C07D401/12 , C07D209/08 , C07D209/12 , C07D209/30 , C07D209/34 , C07D209/42 , C07D231/56 , C07D403/12 , C07D405/12 , C07D409/12 , C07D471/04 , C07D487/04

2. 发明公开

EP1433479A1 APPETITE-STIMULATING AGENTS AND REMEDIES FOR ANOREXIA 有权
标题翻译： MITTEL ZUR ANREGUNG DES APPETITS UND MITTEL ZUR BEHANDLUNG VON ANOREXIE
公开(公告)号：EP1433479A1
公开(公告)日：2004-06-30
申请号：EP02767898.6
申请日：2002-09-05
申请人： Eisai Co., Ltd
发明人： OWA, Takashi , OZAWA, Yoichi , HIDA, Takayuki , MIYAMOTO, Norimasa , NAGASU, Takeshi , OKAUCHI, Tatsuo , YOSHINO, Hiroshi , HATA, Naoko , YOSHIMATSU, Kentaro , KOYANAGI, Nozomu , KITO, Kyosuke
IPC分类号： A61K31/404 , A61K31/4178 , A61K31/427 , A61K31/4439 , A61K45/00 , A61P1/14 , A61P35/00 , A61P43/00 , C07D209/08 , C07D209/30 , C07D209/34 , C07D209/42 , C07D231/56 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D417/12 , C07D471/04
CPC分类号： C07D401/12 , A23L33/10 , A61K31/4035 , C07D209/08 , C07D209/12 , C07D209/30 , C07D209/34 , C07D209/42 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D417/12 , C07D471/04
摘要： An appetite-stimulating agent and a therapeutic agent for anorexia, each comprising, as an active ingredient, a sulfonamide derivative or sulfonic acid ester derivative represented by the following general formula (I):
wherein the ring A represents a monocyclic or bicyclic aromatic ring which may be substituted,
the ring B represents a 6-membered unsaturated hydrocarbon ring or a 6-membered unsaturated heterocyclic ring containing one nitrogen atom as a heteroatom, each of which may be substituted,
the ring C represents a 5-membered heterocyclic ring containing one or two nitrogen atoms, which may be substituted,
W represents a single bond or -CH=CH-,
X represents -N(R 1 )- or an oxygen atom,
Y represents a carbon atom or a nitrogen atom,
Z represents -N(R 2 )- or a nitrogen atom, and
R 1 and R 2 may be identical or different and each represents a hydrogen atom or a lower alkyl group, or a
pharmacologically acceptable salt thereof, or a hydrate thereof.
摘要翻译：作为厌食症的食欲刺激剂和治疗剂，其各自含有作为活性成分的由以下通式（I）表示的磺酰胺衍生物或磺酸酯衍生物：其中环A表示单环或双环可以被取代的芳环，环B表示含有一个氮原子作为杂原子的6元不饱和烃环或6元不饱和杂环，其各自可以被取代，环C表示5元杂环可以被取代的一个或两个氮原子的环表示单键或-CH = CH-，X表示-N（R 1） - 或氧原子，Y表示碳原子或氮原子，Z表示-N（R 2） - 或氮原子，R 1和R 2可以相同或不同，各自表示氢原子或低级烷基，或其药理学上可接受的盐，或其水合物。

3. 发明公开

EP0750609A1 ISOPRENYL TRANSFERASE INHIBITORS 失效
标题翻译：异戊烯基转移酶抑制剂
公开(公告)号：EP0750609A1
公开(公告)日：1997-01-02
申请号：EP95914096.0
申请日：1995-03-15
申请人： Eisai Co., Ltd.
发明人： LEWIS, Michael, D. , KOWALCZYK, James, J. , CHRISTUK, Amy, E. , FAN, Rulin , HARRINGTON, Edmund, M. , SHENG, Xiaoning, C. , YANG, Hu , GARCIA, Ana, Maria , HISHINUMA, Ieharu , NAGASU, Takeshi , YOSHIMATSU, Kentaro
IPC分类号： C07D295 , A61K31 , A61P35 , C07C323 , C07D213 , C07D277 , C07D307 , C07D333 , C07D417 , C07K5 , A61K38
CPC分类号： C07D417/10 , A61K38/00 , C07C323/27 , C07C323/59 , C07C323/60 , C07D277/04 , C07D307/54 , C07D333/24 , C07K5/06034 , C07K5/06043 , C07K5/06078 , C07K5/06139
摘要： Peptidomimetic compounds useful in the treatment of Ras-associated human cancers, and other conditions mediated by farnesylated or geranylgeranylated proteins; and synthetic intermediates thereof.

4. 发明公开

EP0673937A1 BICYCLIC HETEROCYCLIC SULFONAMIDE AND SULFONIC ESTER DERIVATIVES 失效
标题翻译： BICYCLISCHE，SUTERFYCLISCHE SULFONAMIDE UNDSULFONSÄUREESTER。
公开(公告)号：EP0673937A1
公开(公告)日：1995-09-27
申请号：EP94926372.7
申请日：1994-09-08
申请人： Eisai Co., Ltd.
发明人： YOSHINO, Hiroshi , OWA, Takashi , OKAUCHI, Tatsuo , YOSHIMATSU, Kentaro , SUGI, Naoko , NAGASU, Takeshi , OZAWA, Yoichi , KOYANAGI, Nozomu , KITO, Kyosuke
IPC分类号： C07D409/12 , C07D471/04 , A61K31/40 , A61K31/415 , A61K31/435 , A61K31/635 , C07D209/08 , C07D209/30 , C07D209/34 , C07D231/56 , C07D209/12 , C07D209/42 , C07D401/12 , C07D405/12 , C07D403/12
CPC分类号： C07D401/12 , C07D209/08 , C07D209/12 , C07D209/30 , C07D209/34 , C07D209/42 , C07D231/56 , C07D403/12 , C07D405/12 , C07D409/12 , C07D471/04 , C07D487/04
摘要： Novel bicyclic heterocyclic sulfonamide and sulfonic ester derivatives represented by general formula (I) having an antitumor activity and a reduced toxicity, pharmacologically acceptable salts thereof, and a process for producing the same; wherein ring A represents an optionally substituted mono- or bicyclic aromatic group; ring B represents an optionally substituted 6-membered unsaturated hydrocarbon ring or 6-membered unsaturated heterocyclic group containing one nitrogen atom; ring C represents an optionally substituted 5-membered heterocyclic group containing one or two nitrogen atoms; W represents a single bond or -CH=CH-; X represents -NR¹- or oxygen; Y represents carbon or nitrogen; Z represents -NR²- or nitrogen; and R¹ and R² represent each independently hydrogen or lower alkyl.
摘要翻译：由具有抗肿瘤活性和降低毒性的通式（I）表示的新型双环杂环磺酰胺和磺酸酯衍生物及其药理学上可接受的盐及其制备方法; 其中环A表示任选取代的单环或双环芳基; 环B表示含有一个氮原子的任选取代的6元不饱和烃环或6元不饱和杂环基; 环C表示含有一个或两个氮原子的任选取代的5元杂环基; W表示单键或-CH = CH-; X表示-NR 1 - 或氧; Y表示碳或氮; Z表示-NR 2 - 或氮; R 1和R 2各自独立地表示氢或低级烷基。

5. 发明授权

EP0831094B1 FUSED POLYCYCLIC HETEROCYCLE DERIVATIVES 失效
标题翻译：相关环的杂环化合物
公开(公告)号：EP0831094B1
公开(公告)日：2004-12-08
申请号：EP96920027.8
申请日：1996-05-31
申请人： Eisai Co., Ltd.
发明人： SUGUMI, Hiroyuki , NIIJIMA, Jun , KOTAKE, Yoshihiko , OKADA, Toshimi , KAMATA, Jun-ichi , YOSHIMATSU, Kentaro , NAGASU, Takeshi , NAKAMURA, Katsuji , UENAKA, Toshimitsu , YAMAGUCHI, Atsumi , YOSHINO, Hiroshi , KOYANAGI, Nozomu , KITO, Kyosuke
IPC分类号： C07D471/06 , C07D471/16 , C07D487/06 , C07D491/16 , C07D495/16 , C07D498/06 , C07D513/06 , A61K31/495 , A61K31/535 , A61K31/54 , C07D487/16
CPC分类号： C07D471/06 , C07D487/06 , C07D513/06

7. 发明公开

EP0679641A1 SULFONAMIDE AND SULFONIC ESTER DERIVATIVES EACH HAVING TRICYCLIC HETERO RING 失效
标题翻译： SULFONAMIDE UNDSULFONSÄURE-ESTER MIT JE EINEM TRIZYCLISCHEN HETERORING。
公开(公告)号：EP0679641A1
公开(公告)日：1995-11-02
申请号：EP94921819.2
申请日：1994-07-26
申请人： Eisai Co., Ltd.
发明人： YOSHINO, Hiroshi , UEDA, Norihiro 1077-140, Yatabe , NIIJIMA, Jun 14-10-B-202, Matsuhiro 1-chome , HANEDA, Toru 9-24-1003, Chuo 2-chome , KOTAKE, Yoshihiko , YOSHIMATSU, Kentaro , WATANABE, Tatsuo , NAGASU, Takeshi 852-13, Nagakuni , TSUKAHARA, Naoko 796-2-101, Shibazaki , KOYANAGI, Nozomu 10-15, Toukoudai 1-chome , KITOH, Kyosuke 10-8, Toukoudai 1-chome
IPC分类号： C07D209/88 , C07D219/08 , C07D223/22 , C07D241/46 , C07D243/38 , C07D253/06 , C07D265/38 , C07D267/18 , C07D267/20 , C07D279/14 , C07D279/20 , C07D221/12 , C07D281/14 , C07D498/04 , C07D513/04
CPC分类号： C07D219/04 , C07C211/55 , C07C229/58 , C07C311/29 , C07D209/88 , C07D219/06 , C07D219/08 , C07D221/12 , C07D223/22 , C07D243/38 , C07D265/38 , C07D267/18 , C07D267/20 , C07D279/20 , C07D281/14 , C07D413/12 , C07D513/04 , C07F7/1856
摘要： Novel antitumor sulfonamide and sulfonic ester derivatives each having a tricyclic hetero ring, represented by general formula (I), and a process for producing the same, wherein G represents a 5- or 6-membered aromatic ring; L represents O or NR¹, wherein R¹ represents hydrogen or lower alkyl; and M represents a tricyclic structure selected from the members (a), (b), (c), (d), (e), (f), wherein rings A and B represent each a 5- or 6-membered unsaturated ring; X represents NR² (wherein R² represents hydrogen or lower alkyl) or NHCO; Y represents O, S(O) n , CR³R⁴, CO, NR⁵, CHR⁶CHR⁷, CR⁸=CR⁹, NR¹⁰CO, N=CR¹¹, OCHR¹², S(O) n CHR¹³ or NR¹⁴CHR¹⁵; and Z represents N or CR¹⁶, wherein n represents 0, 1 or 2; R³-R¹³, R¹⁵ and R¹⁶ represent each hydrogen or lower alkyl; and R¹⁴ represents hydrogen, lower alkyl or lower acyl.
摘要翻译：具有由通式（I）表示的三环杂环的新型抗肿瘤磺酰胺和磺酸酯衍生物及其制备方法，其中G表示5-或6-元芳香环; L表示O或NR 1，其中R 1表示氢或低级烷基; 并且M表示选自成员（a），（b），（c），（d），（e），（f））的三环结构，其中环A和B各自表示5-或6-元不饱和环 ; X表示NR 2（其中R 2表示氢或低级烷基）或NHCO; Y表示O，S（O）n，CR 3 R 4，CO，NR 5，CHR 6 CHR 7，CR 8 = CR 9，NR 1， CO，N = CR 1，OCHR 1，S（O）n CHR 1或NR 1 CHR 1 5。 Z表示N或CR 1，其中n表示0,1或2; R 3 -R 1，R 5和R 6代表每个氢或低级烷基; R 1表示氢，低级烷基或低级酰基。

8. 发明授权

EP1331005B1 MEDICINAL COMPOSITIONS FOR CONCOMINANT USE AS ANTICANCER ATENT 有权
标题翻译：医药组合物与其他疗法对癌症
公开(公告)号：EP1331005B1
公开(公告)日：2006-04-05
申请号：EP01978983.3
申请日：2001-10-31
申请人： Eisai Co., Ltd.
发明人： OZAWA, Yoichi , YOSHIMATSU, Kentaro , KAI, Junko
IPC分类号： A61K31/404 , A61K31/4745 , A61K31/407 , A61K31/513 , A61K31/24 , A61K31/7068 , A61K31/704 , A61K31/337 , C07D209/08 , C07D235/06 , C07D231/56 , C07D471/04 , A61P35/00
CPC分类号： C07D209/30
摘要： Medicinal compositions having an excellent antitumor effect. Namely, medicinal compositions characterized in that sulfonamide derivatives or sulfonic acid ester derivatives represented by the following general formula (I) or salts thereof, in particular, N-(3-chloro-1H-indol-7-yl)-4-sulfamoylbenzenesulfonamide or its salt are combined with at least one member selected from among (1) irinotecan hydrochloride trihydrate, (2) mitomycin C, (3) 5-fluorouracil, (4) cisplatin, (5) gemcitabine hydrochloride, (6) doxorubicin, (7) Taxol and (8) salts of the compounds (1) to (7) as cited above: (I) wherein the ring A represents an optionally substituted aromatic ring; the ring B represents an optionally substituted 6-membered unsaturated hydrocarbyl ring, etc.; the ring C represents a 5-membered heterocycle having 1 or 2 nitrogen atoms which may be substituted; W represents a single bond or CH=CH-; X represents NH-, etc.; Y represents a carbon atom or a nitrogen atom; and Z represents NH-, etc.

9. 发明公开

EP1331005A1 MEDICINAL COMPOSITIONS FOR CONCOMINANT USE AS ANTICANCER ATENT 有权
标题翻译：医药化妆品
公开(公告)号：EP1331005A1
公开(公告)日：2003-07-30
申请号：EP01978983.3
申请日：2001-10-31
申请人： Eisai Co., Ltd.
发明人： OZAWA, Yoichi , YOSHIMATSU, Kentaro , KAI, Junko
IPC分类号： A61K31/404 , A61K31/4745 , A61K31/407 , A61K31/513 , A61K31/24 , A61K31/7068 , A61K31/704 , A61K31/337 , C07D209/08 , C07D235/06 , C07D231/56 , C07D471/04 , A61P35/00
CPC分类号： C07D209/30
摘要： The present invention provides a medicinal composition having an excellent antitumor activity. That is, it provides a medicinal composition comprising a sulfonamide compound, a sulfonate compound or a salt of them, which is represented by the following formula:
(wherein ring A represents an aromatic ring which may have a substituent group; ring B represents a 6-membered unsaturated hydrocarbon ring which may have a substituent group etc.; ring C represents a 5-membered hetero-ring containing one or two nitrogen atoms, and the ring C may have a substituent group; W represents a single bond or -CH=CH-; X represents -NH- etc.; and Y represents a carbon atom or a nitrogen atom; and Z represents -NH- etc.), particularly N-(3-chloro-1H-indol-7-yl)-4-sulfamoylbenzenesulfonamide or a salt thereof, combined with at least one substance selected from (1) irinotecan hydrochloride trihydrate; (2) mitomycin C; (3) 5-fluorouracil; (4) cisplatin; (5) gemcitabinehydrochloride; (6) doxorubicin; (7) taxol; and (8) a salt of the above-mentioned (1) to (7).
摘要翻译：本发明提供具有优异的抗肿瘤活性的药物组合物。也就是说，提供由下式表示的磺酰胺化合物，磺酸酯化合物或它们的盐的药物组合物：（其中环A表示可具有取代基的芳香环;环B 表示可以具有取代基的6元不饱和烃环等;环C表示含有一个或两个氮原子的5元杂环，环C可以具有取代基; W表示单键或 -CH = CH-; X表示-NH-等; Y表示碳原子或氮原子; Z表示-NH-等），特别是N-（3-氯-1H-吲哚-7-基））-4-氨磺酰基苯磺酰胺或其盐与至少一种选自（1）盐酸伊立替康三水合物的物质组合; （2）丝裂霉素C; （3）5-氟尿嘧啶; （4）顺铂; （5）吉西他滨盐酸盐; （6）多柔比星; （7）紫杉醇; 和（8）上述（1）至（7）的盐。

10. 发明公开

EP0831094A1 FUSED POLYCYCLIC HETEROCYCLE DERIVATIVES 失效
标题翻译： VERKNÜPFTE聚合物杂环化合物VERBINDUNGEN
公开(公告)号：EP0831094A1
公开(公告)日：1998-03-25
申请号：EP96920027.8
申请日：1996-05-31
申请人： Eisai Co., Ltd.
发明人： SUGUMI, Hiroyuki , NIIJIMA, Jun , KOTAKE, Yoshihiko , OKADA, Toshimi , KAMATA, Jun-ichi , YOSHIMATSU, Kentaro , NAGASU, Takeshi , NAKAMURA, Katsuji , UENAKA, Toshimitsu , YAMAGUCHI, Atsumi , YOSHINO, Hiroshi , KOYANAGI, Nozomu , KITO, Kyosuke
IPC分类号： C07D471/06 , C07D471/16 , C07D487/06 , C07D491/16 , C07D495/16 , C07D498/06 , C07D513/06 , A61K31/495 , A61K31/535 , A61K31/54
CPC分类号： C07D471/06 , C07D487/06 , C07D513/06
摘要： Novel fused polycyclic heterocycle derivatives having excellent antitumor effects and a process for producing the same.
A compound represented by the following general formula (I) or pharmacologically acceptable salts thereof:
wherein the ring A represents an optionally substituted monocyclic aromatic ring or a dicyclic fused ring in which at least one of the rings is an aromatic ring; the ring B represents pyrrole, 4H-1,4-oxazine, 4H-1,4-thiazine or 4(1H)-pyridone; the ring C represents an optionally substituted, monocyclic or dicyclic fused aromatic ring; and Y represents a group represented by the formula -e-f (wherein e represents a lower alkylene; and f represents amidino, guanidino or amino optionally substituted by optionally hydroxylated or optionally lower-alkylaminated lower alkyl;
provided that the cases where the rings A and B are both optionally substituted monocyclic aromatic rings are excluded.
Which has an excellent antitumor activity.
摘要翻译：具有优异抗肿瘤效果的新型稠合多环杂环衍生物及其制备方法。由以下通式（I）表示的化合物或其药理学上可接受的盐：其中环A表示任选取代的单环芳环或二环稠合环，其中至少一个环为芳环; 环B表示吡咯，4H-1,4-恶嗪，4H-1,4-噻嗪或4（1H） - 吡啶酮; 环C表示任选取代的单环或二环稠合芳环; Y表示由式-ef表示的基团（其中e表示低级亚烷基; f表示任选被羟基化或任选低级烷基化的低级烷基取代的脒基，胍基或氨基）;条件是环A和B 均为任选取代的单环芳环，其具有优异的抗肿瘤活性。

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