公开(公告)号：EP1622624A1

公开(公告)日：2006-02-08

申请号：EP04730660.0

申请日：2004-04-30

申请人： Eisai Co., Ltd.

发明人： OZAWA, Yoichi

IPC分类号： A61K31/635 ,  A61K31/555 ,  A61K31/505 ,  A61K31/7072 ,  A61P35/00

CPC分类号： A61K45/06

摘要： The present invention provides a medicinal composition having an excellent antitumor activity. That is, it provides a medicinal composition comprising N-(3-chloro-1H-indol-7-yl)-4-sulfamoylbenzenesulfonamide or a salt thereof, combined with at least one substance selected from (1) carboplatin; (2) oxaliplatin; (3) capecitabine; and (4) a salt of the above-mentioned (1) to (3).

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，它提供了一种药物组合物，它含有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）卡铂， （2）奥沙利铂; （3）卡培他滨; 和（4）上述（1）至（3）的盐。

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。

公开(公告)号：EP1243583A1

公开(公告)日：2002-09-25

申请号：EP00985953.9

申请日：2000-12-27

申请人： Eisai Co., Ltd.

发明人： HANEDA, Toru ,  TSURUOKA, Akihiko ,  KAMATA, Junichi ,  OKABE, Tadashi ,  TAKAHASHI, Keiko ,  NARA, Kazumasa ,  HAMAOKA, Shinichi ,  UEDA, Norihiro ,  WAKABAYASHI, Toshiaki ,  FUNAHASHI, Yasuhiro ,  SEMBA, Taro ,  HATA, Naoko ,  YAMAMOTO, Yuji ,  OZAWA, Yoichi ,  TSUKAHARA, Naoko ,  OWA, Takashi

IPC分类号： C07D215/38

CPC分类号： C07D215/38 ,  C07D215/48 ,  C07D217/02 ,  C07D217/22 ,  C07D217/24 ,  C07D217/26 ,  C07D311/16 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D411/12 ,  C07D417/12 ,  C07D471/04

摘要： The present invention provides a sulfonamide- or sulfonylurea-containing heterocyclic compounds. Specifically, it provides a heterocyclic compound represented by the formula (I), a pharmacologically acceptable salt thereof or a hydrate of them.
In the formula, A is hydrogen atom, a halogen atom, a C1-C4 alkyl or alkoxy group which may be substituted with a halogen atom, or cyano group; B is an optionally substituted aryl group or monocyclic heteroaryl group, or:
(wherein, the ring Q is an aromatic ring which may have nitrogen atom; and the ring M is a ring sharing a double bond with the ring Q, which ring may have a heteroatom; and the rings Q and M may share nitrogen atom); K is a single bond; T, W, X and Y are the same as or different from each other and each is =C(D)- (wherein, D is hydrogen or a halogen atom) or nitrogen atom; U and V are the same as or different from each other and each is =C(D)-, nitrogen atom, -CH 2 -, oxygen atom or -CO-; Z is a single bond or -CO-NH-; and R 1 is hydrogen atom, etc.

公开(公告)号：EP1243583B1

公开(公告)日：2005-09-28

申请号：EP00985953.9

申请日：2000-12-27

申请人： Eisai Co., Ltd.

发明人： HANEDA, Toru ,  TSURUOKA, Akihiko ,  KAMATA, Junichi ,  OKABE, Tadashi ,  TAKAHASHI, Keiko ,  NARA, Kazumasa ,  HAMAOKA, Shinichi ,  UEDA, Norihiro ,  WAKABAYASHI, Toshiaki ,  FUNAHASHI, Yasuhiro ,  SEMBA, Taro ,  HATA, Naoko ,  YAMAMOTO, Yuji ,  OZAWA, Yoichi ,  TSUKAHARA, Naoko ,  OWA, Takashi

IPC分类号： A61K31/47 ,  A61K31/4709 ,  A61K31/472 ,  A61K31/4725 ,  C07D215/38 ,  C07D215/48 ,  C07D217/22 ,  C07D217/24 ,  C07D217/26 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D411/12 ,  C07D417/12 ,  A61P19/02 ,  A61P29/00 ,  A61P35/00 ,  A61P35/04

CPC分类号： C07D215/38 ,  C07D215/48 ,  C07D217/02 ,  C07D217/22 ,  C07D217/24 ,  C07D217/26 ,  C07D311/16 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D411/12 ,  C07D417/12 ,  C07D471/04

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

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。

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.

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。