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1. 发明公开

EP0889037A1 NITROGENOUS TRICYCLIC COMPOUNDS AND DRUGS COMPRISING THE SAME 失效
标题翻译：医疗器械制造商维吾尔自行车
公开(公告)号：EP0889037A1
公开(公告)日：1999-01-07
申请号：EP97907297.2
申请日：1997-03-13
申请人： Eisai Co., Ltd.
发明人： MIYAMOTO, Mitsuaki , YOSHIUCHI, Tatsuya , SATO, Keizo , KAINO, Makoto , TANAKA, Masayuki , SOEJIMA, Motoharu , MORIYA, Katsuhiro , SAKUMA, Yoshinori , YAMADA, Koji , HARADA, Kokichi , NISHIZAWA, Yukio , KOBAYASHI, Seiichi , OKITA, Makoto , KATAYAMA, Koichi
IPC分类号： C07D219/14 , C07D243/38 , C07D279/24 , C07D279/34 , C07D417/06 , C07D417/12 , C07D417/14 , A61K31/54 , A61K31/645
CPC分类号： C07D417/06 , C07D279/22 , C07D279/24 , C07D417/12 , C09B21/00 , C09B57/08
摘要： To provide a novel phenothiazine, acridan, acridone oxime, acridone hydrazone and dibenzodiazepine derivative efficacious against diseases in which histamine, leukotrienes, etc. participate.
A phenothiazine, acridan, acridone oxime, acridone hydrazone and dibenzodiazepine derivative represented by the following formula are efficacious in preventing or treating diseases in which chemical mediators such as histamine and leukotrienes participate, for example, asthma, allergic rhinitis, atopic dermatitis, urticaria, hay fever, gastrointestinal allergy and food allergy.
A nitrogen-containing tricyclic compound represented by the following formula (I), a hydrate thereof or a pharmacologically acceptable salt thereof:
(wherein D represents alkylene, etc.)
wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and R 8 are the same or different from each other and each represents hydrogen, hydroxy, cyano, nitro, optionally substituted carbamoyl, halogeno, optionally halogenated lower alkyl, etc.; Z represents -S-, -SO-, -SO 2 -, =NO-substituent, -NC(O)- or =NN-substituent; and Q represents, for example, -NR 20 R 21 (wherein R 20 and R 21 are the same or different from each other and each represents hydrogen, optionally halogenated lower alkyl, optionally substituted aryl, optionally substituted arylalkyl, optionally substituted heteroaryl or optionally substituted heteroarylalkyl, or R 20 and R 21 may form together with the nitrogen atom to which they are bonded a 3- to 8-membered ring).
摘要翻译：提供对组胺，白三烯等参与的疾病有效的新型吩噻嗪，吖啶酮，吖啶酮肟，吖啶酮腙和二苯并二氮杂衍生物。由下式表示的吩噻嗪，吖啶酮，吖啶酮肟，吖啶酮腙和二苯并二氮杂衍生物可有效预防或治疗化学介质如组胺和白三烯参与的疾病，例如哮喘，过敏性鼻炎，特应性皮炎，荨麻疹，干草发烧，胃肠道过敏和食物过敏。由下式（I）表示的含氮三环化合物，其水合物或其药理学上可接受的盐：（其中D表示亚烷基等，其中R 1，R 2， R 3，R 4，R 5，R 6，R 7和R 8彼此相同或不同，各自表示氢，羟基，氰基，硝基，任选取代的氨基甲酰基，卤代，任选卤代的低级烷基等; Z表示-S-，-SO-，-SO 2 - ，= NO-取代基，-NC（O） - 或= N - 取代基; Q表示例如-NR R 20和R 21彼此相同或不同，各自表示氢，任选卤代的低级烷基，任选取代的芳基，任选取代的芳烷基，任选取代的杂芳基或任选取代的杂芳基烷基或R 20和R 21可以与它们所键合的氮原子一起形成3-至8-元环）。

2. 发明公开

EP1364952A1 BICYCLIC NITROGENOUS FUSED-RING COMPOUND 审中-公开
标题翻译： BICYCLISCHE，STICKSTOFFHALTIGE VERBINDUNGEN MIT KONDENSIERTEM RING
公开(公告)号：EP1364952A1
公开(公告)日：2003-11-26
申请号：EP02711424.8
申请日：2002-02-08
申请人： Eisai Co., Ltd.
发明人： HIBI, Shigeki , TAKAHASHI, Yoshinori , HOSHINO, Yorihisa , KIKUCHI, Koichi , SOEJIMA, Motohiro , YOSHIUCHI, Tatsuya , SHIN, Kogyoku , ONO, Mutsuko , SHIBATA, Hisashi , INO, Mitsuhiro , HIRAKAWA, Tetsuya
IPC分类号： C07D487/04 , C07D471/04 , A61K31/4985 , A61K31/5025 , A61K31/5377 , A61K31/437 , A61K31/519 , A61P43/00 , A61P25/28 , A61P1/14 , A61P3/04 , A61P3/10 , A61P25/32 , A61P25/30 , A61P25/20
CPC分类号： C07D471/04 , C07D487/04
摘要： The present invention provides a novel compound having an excellent corticotrophin-releasing-factor receptor antagonistic activity. That is, it provides a compound represented by the following formula or a salt thereof.
Wherein R 1 denotes a hydrogen atom, a C 1-6 alkyl group, a C 1-6 alkoxy group and the like; R 2 denotes a halogen atom, a cyano group, a nitro group, a C 1-10 alkyl group, a C 2-10 alkenyl group, C 2-10 alkynyl group and the like; R 3 denotes a C 6-14 aromatic hydrocarbon cyclic group or a 5- to 14-membered aromatic heterocyclic group, each of which may have a substituent; and X, Y and X are independent of each other and each denotes N or CR 4 (wherein R 4 denotes a hydrogen atom, a halogen atom, a cyano group, a nitro group, an optionally halogenated C 1-6 alkyl group and the like) and, in this case, at least two of X, Y and Z denote CR 4 .
摘要翻译：本发明提供具有优异的促肾上腺皮质激素释放因子受体拮抗作用的新化合物。也就是说，它提供由下式表示的化合物或其盐。其中R 1表示氢原子，C 1-6烷基，C 1-6烷氧基等; R 2表示卤素原子，氰基，硝基，C 1-10烷基，C 2-10烯基，C 2-10炔基等; R 3表示可以具有取代基的C 6〜14芳香族烃环基或5〜14元芳香族杂环基。并且X，Y和X彼此独立，并且各自表示N或CR 4（其中R 4表示氢原子，卤素原子，氰基，硝基，任选卤代的C 1-6烷基组等），在这种情况下，X，Y和Z中的至少两个表示CR 4。

3. 发明公开

EP1389618A1 PYRAZOLO 1,5-A]PYRIDINES AND MEDICINES CONTAINING THE SAME 有权
标题翻译：吡咯唑酮1,5-A PYRIDINE IN DIESE ENTHALTENDE ARZNEIMITTEL
公开(公告)号：EP1389618A1
公开(公告)日：2004-02-18
申请号：EP02720608.5
申请日：2002-04-25
申请人： Eisai Co., Ltd.
发明人： HIBI, Shigeki , KIKUCHI, Koichi , HOSHINO, Yorihisa , SOEJIMA, Motohiro , YOSHIUCHI, Tatsuya , SHIN, Kogyoku , ONO, Mutsuko , TAKAHASHI, Yoshinori , SHIBATA, Hisashi , INO, Mitsuhiro , HIRAKAWA, Tetsuya
IPC分类号： C07D471/04 , A61K31/437 , A61K31/444 , A61P3/04 , A61P3/10 , A61P9/00 , A61P9/10 , A61P15/00 , A61P19/00 , A61P25/08 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P37/08 , A61P11/00 , A61P43/00
CPC分类号： C07D471/04 , A61K31/437 , C07F5/025 , C07F7/2212
摘要： Compounds represented by the general formula:
[wherein R 1 represents methoxy, ethyl, methylthio, etc., R 2 , R 3 and R 4 each represent hydrogen, a halogen, etc., R 5 and R 6 each represent -X 5 -X 6 -X 7 (wherein X 5 represents a single bond or -CO-, X 6 represents a single bond, -NR 3a , etc. and X 7 and R 3a each represent hydrogen, C 1-10 alkyl, etc.), and Ar represents phenyl, pyridyl, etc.], salts thereof and hydrates of the foregoing.
摘要翻译：由通式表示的化合物：其中R 1代表甲氧基，乙基，甲硫基等，R 2，R 3和R 4各自表示氢，卤素等，R <5>和R 6各自表示-X 5 -X 6 -X 7（其中X 5表示单键或-CO-，X 6表示单键， - NR 3a等，X 7和R 3a各自代表氢，C 1-10烷基等），Ar代表苯基，吡啶基等，其盐和上述的水合物。

4. 发明公开

EP1057830A1 HETEROCYCLE-FUSED BENZOTHIAZINE DERIVATIVES 审中-公开
标题翻译：异丁基苯乙烯 - 苯乙烯苯并三唑衍生物
公开(公告)号：EP1057830A1
公开(公告)日：2000-12-06
申请号：EP99906524.6
申请日：1999-02-26
申请人： Eisai Co., Ltd. , Yamada, Sumiyo , Yamada, Ryoko
发明人： YAMADA, Koji , MIYAMOTO, Mitsuaki , YOSHIUCHI, Tatsuya , SATO, Keizo , SOEJIMA, Motohiro , SATO, Takashi , KIKUCHI, Koichi, Gardenhills Hisamatsu 302 , YOSHIMURA, Hiroyuki , MORIYA, Katsuhiro , SAKUMA, Yoshinori , AKASOFU, Shigeru
IPC分类号： C07D513/04 , A61K31/54 , A61K31/645
CPC分类号： C07D513/04
摘要： The invention provides a novel heterocyclic ring condensed benzothiazine compound which is effective for prevention or remedy of disease, in which histamine, leukotriene and the like participate. The heterocyclic ring condensed benzothiazine compound of the present invention or a pharmacologically acceptable salt thereof is effective for prevention or remedy of disease, in which a chemical mediator, such as histamine, leukotriene and the like, participate, for example, asthma, allergic coryza, atopic dermatitis, hives, hay fever, gastrointestinal allergy, food allergy and the like. Further, the heterocyclic ring condensed benzothiazine compound of the present invention, its pharmacologically acceptable salt or hydrates thereof is represented by the following formula:
In the formula, the ring Het represents an unsaturated heterocyclic ring; R 1 and R 2 are the same as or different from each other, and each represents halogen atom, a lower alkyl group that may be substituted with a halogen atom, a lower alkoxy group that may be substituted with a halogen atom, a lower alkyl lower alkoxy group, cyano group; D represents a lower alkylene group and the like that may have a substituent; Q represents, for example, the formula -NR 20 R 21 (in the formula, R 20 and R 21 are the same as or different from each other, and each represents hydrogen atom, a lower alkyl group that may be substituted with a halogen atom, an aryl group that may have a substituent, an arylalkyl group that may have a substituent, a heteroaryl group that may have a substituent or a heteroarylalkyl group that may have a substituent, or R 20 and R 21 may form a 3- to 8-membered ring along with the nitrogen atom to which they are bound); and x represents an integer of from 1 to 2.
摘要翻译：本发明提供一种新颖的杂环稠合苯并噻嗪化合物，其对组胺，白细胞三烯等参与的疾病的预防或治疗有效。本发明的杂环稠合苯并噻嗪化合物或其药理学上可接受的盐对于预防或治疗其中化学介质如组胺，白三烯等参与的疾病是有效的，例如哮喘，过敏性鼻炎，特应性皮炎，荨麻疹，花粉症，胃肠过敏，食物过敏等。此外，本发明的杂环稠合苯并噻嗪化合物，其药理学上可接受的盐或其水合物由下式表示：式中，环Het表示不饱和杂环; R 1和R 2彼此相同或不同，各自表示卤素原子，可被卤素原子取代的低级烷基，可被卤素原子取代的低级烷氧基，低级烷基低级烷氧基，氰基; D表示可以具有取代基的低级亚烷基等; Q表示例如式-NR 20 R 21（式中，R 20和R 21彼此相同或不同，各自表示氢原子，低级烷基可以被卤素原子取代的基团，可以具有取代基的芳基，可以具有取代基的芳烷基，可以具有取代基的杂芳基或可以具有取代基的杂芳基烷基，或者R 20 并且R 21可以与它们所结合的氮原子一起形成3至8元环; x表示1〜2的整数。

5. 发明授权

EP1238979B1 FUSED HETEROTRICYCLIC COMPOUNDS, PROCESS FOR PREPARING THE COMPOUNDS AND DRUGS CONTAINING THE SAME 有权
标题翻译： ANNE内衬杂环，法制造化合物和药物含
公开(公告)号：EP1238979B1
公开(公告)日：2005-03-02
申请号：EP00983479.7
申请日：2000-12-13
申请人： Eisai Co., Ltd.
发明人： HIBI, Shigeki , HOSHINO, Yorihisa , YOSHIUCHI, Tatsuya , SHIN, Kogyoku , KIKUCHI, Kouichi , SOEJIMA, Motohiro , TABATA, Mutsuko , TAKAHASHI, Yoshinori , SHIBATA, Hisashi , HIDA, Takayuki , HIRAKAWA, Tetsuya , INO, Mitsuhiro
IPC分类号： C07D487/14 , C07D471/14 , C07D473/02 , C07D495/14 , A61K31/437 , A61K31/519 , A61P1/04 , A61P1/08 , A61P1/10 , A61P1/12 , A61P1/14 , A61P9/04 , A61P9/10 , A61P9/12 , A61P11/00
CPC分类号： C07D471/14 , C07D487/14 , C07D491/14
摘要： Compounds represented by general formula (I) are provided, which exhibit antagonism against corticotropin-releasing factor receptor, wherein A, B and C are each independently -(CR1R2)m- (wherein R?1 and R2¿ are each C¿1-6? alkyl or the like, and m is an integer of 1 to 4), -NR?3¿- (wherein R3 is hydrogen or the like), or the like; E and G are each independently a heteroatom such as nitrogen, -(CR6R7)p- (wherein R?6 and R7¿ are each hydrogen or the like, and p is an integer of 0 to 2), or the like; J is a carbon atom substituted with aryl or the like, or a nitrogen atom; K and L are each independently carbon or nitrogen; M is hydrogen, optionally substituted alkyl, or the like; and the partial structures ----- are each a single or double bond.

6. 发明公开

EP1238979A1 FUSED HETEROTRICYCLIC COMPOUNDS, PROCESS FOR PREPARING THE COMPOUNDS AND DRUGS CONTAINING THE SAME 有权
标题翻译： ANNE内衬杂环，法制造化合物和药物含
公开(公告)号：EP1238979A1
公开(公告)日：2002-09-11
申请号：EP00983479.7
申请日：2000-12-13
申请人： Eisai Co., Ltd.
发明人： HIBI, Shigeki , HOSHINO, Yorihisa , YOSHIUCHI, Tatsuya , SHIN, Kogyoku , KIKUCHI, Kouichi , SOEJIMA, Motohiro , TABATA, Mutsuko , TAKAHASHI, Yoshinori , SHIBATA, Hisashi , HIDA, Takayuki , HIRAKAWA, Tetsuya , INO, Mitsuhiro
IPC分类号： C07D487/14 , C07D471/14 , C07D473/02 , C07D495/14 , A61K31/437 , A61K31/519 , A61P1/04 , A61P1/08 , A61P1/10 , A61P1/12 , A61P1/14 , A61P9/04 , A61P9/10 , A61P9/12 , A61P11/00
CPC分类号： C07D471/14 , C07D487/14 , C07D491/14
摘要： The present invention provides a novel compound having an excellent corticotrophin-releasing-factor receptor antagonistic activity. That is, it provides a compound represented by the following formula, a pharmacologically acceptable salt thereof or hydrates thereof.
Wherein A, B and D are the same as or different from each other and each represents a group represented by the formula - (CR 1 R 2 ) m - (wherein R 1 and R 2 are the same as or different from each other and each represents a C 1-6 alkyl group etc.), -NR 3 - (wherein R 3 represetns hydrogen etc.) etc.; E and G are the same as or different from each other and each represents a group represented by the formula - (CR 6 R 7 ) p - (wherein R 6 and R 7 are the same as or different from each other and each represents hydrogen etc.; and p represents an integer of 0, 1 or 2); J represents a carbon atom or nitrogen atom, each substituted with C 1-6 alkyl group optionally substituted with a halogen atom, etc.; K and L are the same as or different from each other and each represents carbon atom or nitrogen atom; M means hydrogen, a halogen atom, an optionally substituted C 1-6 alkyl group etc.; and the partial structure ----- means a single or double bond.
摘要翻译：本发明提供具有优异的促肾上腺皮质激素释放因子受体拮抗作用的新型化合物。即，它提供了由下式表示的化合物，其药理学上可接受的盐或其水合物。其中A，B和D是相同或不同的海誓山盟并且每个darstellt由下式表示的基团 - （CR <1> [R <2>）米（worin - [R <1>和R <2 >是相同的或从海誓山盟不同，并且各自darstellt C 1-6烷基等），-NR <3> - （worin - [R <3> represetns氢等），等; E和G是相同的或从海誓山盟不同，并且各自darstellt由下式表示的基团 - （CR <6> - [R <7>）对 - （worin - [R <6>和R <7>是相同的或从彼此，并且每个darstellt氢等不同;并且p darstellt为0的整数，1或2）; Ĵdarstellt一个碳原子或氮原子，各自具有substituiertem C1-6烷基被卤原子等OPTIONALLY substituiertem。 K和L是相同的或从海誓山盟不同，并且各自darstellt碳原子或氮原子; M表示氢，卤原子，以任选substituiertem C 1-6烷基等; 与该部分结构-----表示单键或双键。

7. 发明公开

EP0877020A1 ACRIDONE DERIVATIVE 失效
标题翻译：吖啶酮衍生物
公开(公告)号：EP0877020A1
公开(公告)日：1998-11-11
申请号：EP95932954.1
申请日：1995-10-02
申请人： Eisai Co., Ltd.
发明人： MIYAMOTO, Mitsuaki , YOSHIUCHI, Tatsuya , ABE, Shinya , TANAKA, Masayuki , MORIYA, Katsuhiro , KATAYAMA, Satoshi , YAMANAKA, Takashi , YAMADA, Koji
IPC分类号： C07D219/06 , C07D401/06 , C07D405/06 , C07D409/06 , A61K31/435 , A61K31/495 , A61K31/535 , A61K31/445 , A61K31/44
CPC分类号： C07D219/14
摘要： An acridone derivative represented by the following formula (I) and a pharmacologically acceptable salt thereof are effective in preventing and curing diseases which are associable with histamine, leucotriene, etc. and in preventing and curing allergic diseases such as asthma, allergic rhinitis, atopic dermatitis, urticaria, valerian fever, digestive tract allergy, or food allergy.
wherein R 1 - R 8 severally represent a hydrogen atom, a lower alkyl group, etc. and n represents an integer of 1 - 6.

8. 发明公开

EP0857721A1 ACRIDONE COMPOUNDS 失效
标题翻译： ACRIDONE化合物
公开(公告)号：EP0857721A1
公开(公告)日：1998-08-12
申请号：EP96932811.1
申请日：1996-10-03
申请人： Eisai Co., Ltd.
发明人： MIYAMOTO, Mitsuaki , YOSHIUCHI, Tatsuya , SATO, Keizo , KAINO, Makoto , TAKASHIMA, Yoshihiro , MORIYA, Katsuhiro , SAKUMA, Yoshinori , YAMADA, Koji , HARADA, kOkichi , NISHIZAWA, Yukio , KOBAYASHI, Seiichi , OKITA, Makoto , KATAYAMA, Koichi
IPC分类号： C07D219/14 , C07D219/06 , C07D401/12 , C07D405/06 , C07D405/12 , A61K31/645 , A61K31/44 , A61K31/47
CPC分类号： C07D219/14
摘要： Novel acridone compounds represented by the general formula (I) or pharmaceutically acceptable salts thereof efficacious in the prevention and treatment of diseases in which chemical transmitters such as histamine and leukotriene participate, typified by asthma, allergic rhinitis, atopic dermatitis, urticaria, hay fever, digestive tract allergy and food allergy:
wherein R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are the same or different and each represents hydrogen, hydroxy, halogeno, lower alkyl, cycloalkyl, lower alkoxy, etc.; Y represents -(CH 2 ) t -(B) m -(CH 2 ) n -Z {wherein m is 0 or 1; t and n represent each an integer of 0 to 6; B represents lower alkylene, optionally substituted arylene, etc.; and Z represents cyano, optionally protected carboxy, acyl, -NR 7 R 8 [wherein R 7 and R 8 are the same or different and each represents hydrogen, lower alkyl, lower alkoxy, hydroxyalkyl, etc.]}; and D represents oxygen or sulfur.
摘要翻译：由通式（I）表示的新型吖啶酮化合物或其药学上可接受的盐在预防和治疗其中化学传递物质例如组胺和白三烯参与的疾病中有效，所述疾病以哮喘，变应性鼻炎，特应性皮炎，荨麻疹，花粉热，消化道过敏和食物过敏：其中R1，R2，R3，R4，R5和R6相同或不同，并且各自代表氢，羟基，卤代，低级烷基，环烷基，低级烷氧基等; Y表示 - （CH 2）t - （B）m - （CH 2）n -Z {其中m是0或1; t和n分别表示0〜6的整数。 B代表低级亚烷基，任选取代的亚芳基等; 和Z代表氰基，任选保护的羧基，酰基，-NR7R8 [其中R7和R8相同或不同并且各自代表氢，低级烷基，低级烷氧基，羟基烷基等]}; D代表氧或硫。

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