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1. 发明申请

WO2004082715A8 CONCOMITANT DRUG AS THERAPEUTIC AGENT FOR INFLAMMATORY BOWEL DISEASE 审中-公开
标题翻译：作为治疗诱发剂的治疗药物的可持续药物
公开(公告)号：WO2004082715A8
公开(公告)日：2005-05-12
申请号：PCT/JP2004003662
申请日：2004-03-18
申请人： EISAI CO LTD , HORIZOE TATSUO
发明人： HORIZOE TATSUO
IPC分类号： A61K31/00 , A61K38/13 , A61K45/06 , A61P1/04 , C07K16/24 , A61K45/00
CPC分类号： C07K16/241 , A61K31/00 , A61K38/13 , A61K45/06 , A61K2300/00
摘要： A drug having enhanced efficacy against inflammatory bowel diseases, such as ulcerative colitis and Crohn's disease. In particular, a therapeutic agent for inflammatory bowel diseases comprising active ingredient (a) consisting of at least one compound having inflammation inhibiting activity selected from the group consisting of an aminosalicylic acid derivative, an antiinflammatory glucocorticoid, an immunosuppressive compound, an anti-TNFalpha antibody, a neurohypophysial hormone and an antiinfective compound, combined with active ingredient (b) consisting of at least one compound having PPARgamma agonist activity. In the application of this therapeutic agent for inflammatory bowel diseases, compound (a) and compound (b) can be administered simultaneously, separately or with intervals.
摘要翻译：一种具有增强的抗炎症性肠病如溃疡性结肠炎和克罗恩病的功效的药物。特别地，涉及炎症性肠病的治疗剂，其含有由至少一种具有炎症抑制活性的化合物组成的活性成分（a），所述化合物具有选自氨基水杨酸衍生物，抗炎糖皮质激素，免疫抑制化合物，抗TNFα抗体，神经嗜睡激素和抗感染化合物，与由至少一种具有PPARγ激动剂活性的化合物组成的活性成分（b）组合。在该治疗剂用于炎性肠病的应用中，化合物（a）和化合物（b）可以同时，分开地或间隔地施用。

2. 发明申请

WO0102400A8 FUSED IMIDAZOLE COMPOUNDS AND REMEDIES FOR DIABETES MELLITUS 审中-公开
标题翻译：熔化的咪唑化合物和糖尿病患者的补救措施
公开(公告)号：WO0102400A8
公开(公告)日：2001-04-05
申请号：PCT/JP0004358
申请日：2000-06-30
申请人： EISAI CO LTD , ASANO OSAMU , HARADA HITOSHI , YOSHIKAWA SEIJI , WATANABE NOBUHISA , INOUE TAKASHI , HORIZOE TATSUO , YASUDA NOBUYUKI , OHASHI KAYA , MINAMI HIROE , NAGAOKA JUNSAKU , MURAKAMI MANABU , KOBAYASHI SEIICHI , TANAKA ISAO , KAWATA TSUTOMU , SHIMOMURA NAOYUKI , AKAMATSU HIROFUMI , OZEKI NAOKI , SHIMIZU TOSHIKAZU , HAYASHI KENJI , HAGA TOYOKAZU , NEGI SHIGETO , NAITO TOSHIHIKO
发明人： ASANO OSAMU , HARADA HITOSHI , YOSHIKAWA SEIJI , WATANABE NOBUHISA , INOUE TAKASHI , HORIZOE TATSUO , YASUDA NOBUYUKI , OOHASHI KAYA , MINAMI HIROE , NAGAOKA JUNSAKU , MURAKAMI MANABU , KOBAYASHI SEIICHI , TANAKA ISAO , KAWATA TSUTOMU , SHIMOMURA NAOYUKI , AKAMATSU HIROFUMI , OZEKI NAOKI , SHIMIZU TOSHIKAZU , HAYASHI KENJI , HAGA TOYOKAZU , NEGI SHIGETO , NAITO TOSHIHIKO
IPC分类号： A61P3/10 , A61P43/00 , C07D471/04 , C07D473/00 , C07D473/34 , C07D473/40 , A61K31/437 , A61K31/52 , A61K31/522 , C07D213/73 , C07D213/75 , C07D235/18 , C07D239/48 , C07D471/08 , C07D473/18 , C07D487/04
CPC分类号： C07D471/04 , C07D473/00 , C07D473/34 , C07D473/40
摘要： Novel fused imidazole compounds of general formula (I), pharmacologically acceptable salts thereof, or hydrates of both, exhibiting adenosine A2 receptor antagonism and being effective in the prevention and treatment of diabetes mellitus and complications of diabetes; wherein R is optionally alkylated amino or the like; R is hydrogen, alkyl, or the like; R is optionally substituted aryl, a pyridinone group, a pyrimidinone group, or the like; Ar is an optionally sybstituted aryl or heteroaryl group, or the like; and Q and W are each independently N or CH.
摘要翻译：通式（I）的新型稠合咪唑化合物，其药理学上可接受的盐或两者的水合物，显示出腺苷A2受体拮抗作用，并且有效预防和治疗糖尿病以及糖尿病并发症; 其中R 1任选地是烷基化的氨基等; R 2是氢，烷基等; R 3是任选取代的芳基，吡啶酮基，嘧啶酮基等; Ar是任选取代的芳基或杂芳基等; Q和W各自独立地为N或CH。

3. 发明公开

EP1221444A4 FUSED IMIDAZOLE COMPOUNDS AND REMEDIES FOR DIABETES MELLITUS 有权
标题翻译：恩智利帝国糖尿病
公开(公告)号：EP1221444A4
公开(公告)日：2003-05-07
申请号：EP00940909
申请日：2000-06-30
申请人： EISAI CO LTD
发明人： ASANO OSAMU , HARADA HITOSHI , YOSHIKAWA SEIJI , WATANABE NOBUHISA , INOUE TAKASHI , HORIZOE TATSUO , YASUDA NOBUYUKI , OHASHI KAYA , MINAMI HIROE , NAGAOKA JUNSAKU , MURAKAMI MANABU , KOBAYASHI SEIICHI , TANAKA ISAO , KAWATA TSUTOMU , SHIMOMURA NAOYUKI , AKAMATSU HIROSHI , OZEKI NAOKI , SHIMIZU TOSHIKAZU , HAYASHI KENJI , HAGA TOYOKAZU
IPC分类号： A61P3/10 , A61P43/00 , C07D471/04 , C07D473/00 , C07D473/34 , C07D473/40 , C07D213/73 , C07D213/75 , C07D235/18 , C07D239/48 , C07D401/12 , C07D471/08 , C07D473/18 , C07D487/04
CPC分类号： C07D471/04 , C07D473/00 , C07D473/34 , C07D473/40
摘要： Novel fused imidazole compounds of general formula (I), pharmacologically acceptable salts thereof, or hydrates of both, exhibiting adenosine A2 receptor antagonism and being effective in the prevention and treatment of diabetes mellitus and complications of diabetes; wherein R1 is optionally alkylated amino or the like; R2 is hydrogen, alkyl, or the like; R3 is optionally substituted aryl, a pyridinone group, a pyrimidinone group, or the like; Ar is an optionally sybstituted aryl or heteroaryl group, or the like; and Q and W are each independently N or CH.
摘要翻译：本发明提供了一种基于腺苷A2受体拮抗剂作用的新型糖尿病和糖尿病并发症的预防或治疗剂。也就是说，提供了具有腺苷A2受体拮抗剂作用的新颖的缩合咪唑化合物，对预防或治疗糖尿病和糖尿病并发症有效，并且由式（I）表示：其中R 1，例如可以被烷基取代的氨基; R 2表示例如可以被羟基取代的氢原子，烷基，环烷基或烷基，烯基或炔基等; R 3表示例如任选取代的烷基，烯基，炔基，芳基，杂芳基，吡啶酮基，嘧啶酮基或哌嗪酮基; Ar表示例如任选取代的芳基或杂芳基; Q和W相同彼此相同或不同，并且各自表示N或CH），其药理学上可接受的盐或其水合物。

4. 发明公开

EP1054012A4 PURINE DERIVATIVES AND ADENOSINE A2 RECEPTOR ANTAGONISTS SERVING AS PREVENTIVES/REMEDIES FOR DIABETES 有权
标题翻译：嘌呤衍生物和腺苷A2受体的拮抗剂，它们的提供或治愈糖尿病的
公开(公告)号：EP1054012A4
公开(公告)日：2001-12-12
申请号：EP98961528
申请日：1998-12-24
申请人： EISAI CO LTD
发明人： ASANO OSAMU , HARADA HITOSHI , HOSHINO YORIHISA , YOSHIKAWA SEIJI , INOUE TAKASHI , HORIZOE TATSUO , YASUDA NOBUYUKI , NAGATA KAYA , NAGAOKA JUNSAKU , MURAKAMI MANABU , KOBAYASHI SEIICHI
IPC分类号： A61K31/52 , A61P3/10 , C07D473/00 , C07D473/30 , C07D473/34 , A61K31/505 , A61K45/00 , C07D473/04 , C07D473/40 , C07D487/04 , C07D487/14 , A61K31/645
CPC分类号： C07D473/30 , A61K31/52 , C07D473/00 , C07D473/34
摘要： Preventives/remedies of a novel type for diabetes and complications thereof based on the adenosine A2 receptor antagonism. Purine derivatives represented by general formula (I), pharmacologically acceptable salts thereof or hydrates of the same have adenosine A2 receptor antagonism and are useful in preventing and treating diabetes and its complications. Moreover, adenosine A2 receptor antagonists being different from the above compounds in structure, for example KW6002 are also useful in preventing and treating diabetes and its complications. In formula (I), W represents -CH2CH2-, -CH=CH- or -C≡C-; and R1 represents KW6002.

5. 发明专利

ES2246867T3 COMPUESTOS DE IMIDAZOL CONDENSADOS Y MEDICAMENTOS CONTRA LA DIABETES MELLITUS. 未知
公开(公告)号：ES2246867T3
公开(公告)日：2006-03-01
申请号：ES00940909
申请日：2000-06-30
申请人： EISAI CO LTD
发明人： ASANO OSAMU , HARADA HITOSHI , YOSHIKAWA SEIJI , WATANABE NOBUHISA , INOUE TAKASHI , HORIZOE TATSUO
IPC分类号： A61P3/10 , A61P43/00 , C07D471/04 , C07D473/00 , C07D473/34 , C07D473/40 , C07D473/18 , C07D471/08 , C07D239/48 , C07D213/73 , C07D213/75 , C07D235/18 , C07D487/04 , C07D401/12
摘要： Un compuesto de imidazol condensado, una sal farmacológicamente aceptable del mismo o hidratos del mismo, que está representado por la fórmula (I), (en la que R1 representa hidrógeno o la fórmula -NR4R5 (en la que R4 y R5 son iguales o diferentes entre sí y cada uno de ellos representa hidrógeno, un grupo cicloalquilo C3-C8 o o un grupo alquilo CC1-C8); R2 representa 1) hidrógeno, 2) un átomo de halógeno, 3) un grupo alquinilo C2-C8 que puede estar sustituido con un grupo hidroxilo o cicloalquilo C3-C6, 4) un grupo alquilo C1-C8 o 5) un grupo alcoxi C1-C8; R3 representa un grupo 1, 2-dihidro-2-oxopiridilo que puede estar sustituido con a) un átomo de halógeno o un grupo alquilo C1-C6, y y cuyo átomo de nitrógeno puede estarsustituido adicionalmente con b-1) un grupo alquilo C1-C6 que puede estar sustituido con un átomo de halógeno, hidroxilo, fenilo, alquenilo C2-C8 o un grupo carboxilo opcionalmente protegido, b-2) un grupo cicloalquil C3-C6 alquilo C1-C4 opcionalmente sustituido o b-3) ungrupo cicloalquilo C3-C6 opcionalmente sustituido; Ar representa 1) un grupo fenilo opcionalmente sustituido, 2) un grupo piridilo opcionalmente sustituido, 3) un grupo furilo opcionalmente sustituido o 4) un grupo tienilo opcionalmente sustituido; y tanto Q como W son N o uno de Q y W es N y el otro es CH;

6. 发明专利

CA2376835A1 CONDENSED IMIDAZOLE COMPOUNDS AND A THERAPEUTIC AGENT FOR DIABETES MELLITUS 未知
公开(公告)号：CA2376835A1
公开(公告)日：2001-01-11
申请号：CA2376835
申请日：2000-06-30
申请人： EISAI CO LTD
发明人： YOSHIKAWA SEIJI , SHIMOMURA NAOYUKI , KAWATA TSUTOMU , TANAKA ISAO , KOBAYASHI SEIICHI , NAGAOKA JUNSAKU , SHIMIZU TOSHIKAZU , MURAKAMI MANABU , OZEKI NAOKI , HAYASHI KENJI , HORIZOE TATSUO , INOUE TAKASHI , HARADA HITOSHI , NAITO TOSHIHIKO , MINAMI HIROE , NEGI SHIGETO , YASUDA NOBUYUKI , HAGA TOYOKAZU , ASANO OSAMU , OHASHI KAYA , WATANABE NOBUHISA , AKAMATSU HIROSHI
IPC分类号： A61P3/10 , A61P43/00 , C07D471/04 , C07D473/00 , C07D473/34 , C07D473/40 , C07D487/04 , C07D471/08 , C07D235/18 , C07D473/18 , A61K31/437 , C07D239/48 , A61K31/52 , A61K31/522 , C07D213/73 , C07D213/75
摘要： Novel fused imidazole compounds of general formula (I), pharmacologically acceptable salts thereof, or hydrates of both, exhibiting adenosine A2 receptor antagonism and being effective in the prevention and treatment of diabetes mellitus and complications of diabetes; wherein R1 is optionally alkylated amino or the like; R2 is hydrogen, alkyl, or the like; R3 is optionally substituted aryl, a pyridinone group, a pyrimidinone group, or th e like; Ar is an optionally sybstituted aryl or heteroaryl group, or the like; and Q and W are each independently N or CH.

7. 发明专利

NZ516260A Fused imidazole compounds and remedies for diabetes mellitus 未知
公开(公告)号：NZ516260A
公开(公告)日：2004-08-27
申请号：NZ51626000
申请日：2000-06-30
申请人： EISAI CO LTD
发明人： ASANO OSAMU , HARADA HITOSHI , YOSHIKAWA SEIJI , WATANABE NOBUHISA , INOUE TAKASHI , HORIZOE TATSUO , YASUDA NOBUYUKI , OHASHI KAYA , MINAMI HIROE , NAGAOKA JUNSAKU , MURAKAMI MANABU , KOBAYASHI SEIICHI , TANAKA ISAO , SHIMOMURA NAOYUKI , AKAMATSU HIROSHI , OZEKI NAOKI , SHIMIZU TOSHIKAZU , HAYASHI KENJI , HAGA TOYOKAZU , NEGI SHIGETO , NAITO TOSHIHIKO , KAWATA TSUTOMU
IPC分类号： A61P3/10 , A61P43/00 , C07D471/04 , C07D473/00 , C07D473/34 , C07D473/40 , C07D473/18 , C07D471/08 , C07D239/48 , C07D213/73 , C07D213/75 , C07D235/18 , C07D487/04 , A61K31/437 , A61K31/52 , A61K31/522
摘要： Fused condensed imidazole compounds of formula (I) exhibiting adenosine A2 receptor antagonism and useful for preventing or treating diabetes mellitus, diabetic complications or diabetic retinopathy.

9. 发明专利

ZA9509475B Pyrazole derivatives 未知
公开(公告)号：ZA9509475B
公开(公告)日：1996-05-15
申请号：ZA9509475
申请日：1995-11-08
申请人： EISAI CO LTD
发明人： NUMATA HIROTOSHI , OKAMOTO YASUSHI , SHINODA MASANOBU , KOBAYASHI NAOKI , MIYAZAWA SHUHEI , KAWAHARA TETSUYA , SHIROTA HIROSHI , NAGAKURA NAOKI , HORIZOE TATSUO , ABE SHINYA , KOBAYASHI SEIICHI , YAMANAKA TAKASHI
IPC分类号： A61K20060101 , C07C20060101 , C07D20060101 , A61K , C07C , C07D

10. 发明专利

DE60022366D1 未知
公开(公告)号：DE60022366D1
公开(公告)日：2005-10-06
申请号：DE60022366
申请日：2000-06-30
申请人： EISAI CO LTD
发明人： ASANO OSAMU , HARADA HITOSHI , YOSHIKAWA SEIJI , WATANABE NOBUHISA , INOUE TAKASHI , HORIZOE TATSUO , YASUDA NOBUYUKI , OHASHI KAYA , MINAMI HIROE , NAGAOKA JUNSAKU , MURAKAMI MANABU , KOBAYASHI SEIICHI , TANAKA ISAO , KAWATA TSUTOMU , SHIMOMURA NAOYUKI , AKAMATSU HIROSHI , OZEKI NAOKI , SHIMIZU TOSHIKAZU , HAYASHI KENJI , HAGA TOYOKAZU , NEGI , NAITO
IPC分类号： A61P3/10 , A61P43/00 , C07D471/04 , C07D473/00 , C07D473/34 , C07D473/40 , C07D73/34 , C07D73/18 , C07D71/08 , C07D73/40 , C07D39/48 , C07D13/73 , C07D13/75 , C07D35/18 , C07D70/04 , C07D87/04 , C07D01/12
摘要： The present invention provides a preventive or therapeutic agent for diabetes mellitus and diabetic complications, which is a new type based on an adenosine A2 receptor antagonist action. That is, it provides a novel condensed imidazole compound which has an adenosine A2 receptor antagonist action, is effective for preventing or treating diabetes mellitus and diabetic complications, and is represented by the formula (I): (wherein R represents e.g. an amino group which may be substituted with an alkyl group; R represents e.g. hydrogen atom, an alkyl group, a cycloalkyl group or an alkyl group, alkenyl group or alkynyl group which may be substituted with hydrox etc.; R represents e.g. an optionally substituted alkyl group, alkenyl group, alkynyl group, aryl group, heteroaryl group, pyridinone group, pyrimidinone group or piperadinone group; Ar represents e.g. an optionally substituted aryl or heteroaryl group; and Q and W are the same as or different from each other and each represents N or CH), a pharmacologically acceptable salt or hydrates thereof.

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