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1. 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。

2. 发明申请

WO1995009167A1 INDOLINE DERIVATIVE AND 5-HT3 RECEPTOR ANTAGONIST CONTAINING THE SAME AS ACTIVE INGREDIENT 审中-公开
标题翻译：含有它们的吲哚衍生物和5-HT3受体拮抗剂作为活性成分
公开(公告)号：WO1995009167A1
公开(公告)日：1995-04-06
申请号：PCT/JP1994001622
申请日：1994-09-29
申请人： TOKYO TANABE COMPANY LIMITED , TSUCHIYA, Shinji , YASUDA, Nobuyuki , FUKUZAKI, Atsushi , KAZAMA, Koichi
发明人： TOKYO TANABE COMPANY LIMITED
IPC分类号： C07D403/06
CPC分类号： C07D403/06
摘要： An indoline derivative represented by general formula (I); a physiologically acceptable salt thereof; solvates of these compounds; and a 5-HT3 receptor antagonist containing the same as the active ingredient. In said formula, R represents the group (a) ou (b); R represents optionally substituted phenyl or heteroaryl; and R represents hydrogen, halogen, lower alkyl, hydroxy, lower alkoxy, carbamoyl or lower alkoxycarbonyl. The derivative has a potent antagonism against 5-HT3 receptors in the intestinal tract as compared with the known 5-HT3 receptor antagonists and is excellent in the persistence of the activity. Hence it is useful for preventing or treating vomiting or nausea induced by chemotherapy or radiation, irritable bowel syndrom and diarrhea.
摘要翻译：由通式（I）表示的二氢吲哚衍生物; 其生理上可接受的盐; 这些化合物的溶剂合物; 和含有与活性成分相同的5-HT 3受体拮抗剂。在所述式中，R 1表示（a）ou（b）; R 2表示任选取代的苯基或杂芳基; R 3表示氢，卤素，低级烷基，羟基，低级烷氧基，氨基甲酰基或低级烷氧基羰基。与已知的5-HT 3受体拮抗剂相比，该衍生物对肠道中的5-HT 3受体具有强烈的拮抗作用，并且活性持久性优异。因此，可用于预防或治疗由化学疗法或放射线引起的呕吐或恶心，肠易激综合征和腹泻。

3. 发明申请

WO1997015549A1 PHENYLETHANOLAMINE COMPOUNDS USEFUL AS 'beta'3 AGONIST, PROCESS FOR PRODUCING THE SAME, AND INTERMEDIATES IN THE PRODUCTION OF THE SAME 审中-公开
标题翻译：苯乙醇胺化合物作为β3激动剂有用，其生产方法及其生产中的中间体
公开(公告)号：WO1997015549A1
公开(公告)日：1997-05-01
申请号：PCT/JP1996003097
申请日：1996-10-24
申请人： TOKYO TANABE COMPANY LIMITED , TSUCHIYA, Susumu , YASUDA, Nobuyuki , MATSUMOTO, Toshifumi , HIRATSUKA, Kozo , IIZUKA, Hiroyuki , HUKUZAKI, Atsusi , MATSUNAGA, Kouichi
发明人： TOKYO TANABE COMPANY LIMITED
IPC分类号： C07C217/74
CPC分类号： C07D295/185 , C07C215/42 , C07C217/74 , C07C219/24 , C07C235/36 , C07C2601/08 , C07C2601/14 , C07D235/08 , C07D317/46 , Y10S514/866 , Y10S514/909
摘要： Phenylethanolamine compounds represented by general formula (I) and pharmacologically acceptable salts thereof which have a potent effect of stimulating beta 3 adrenaline receptors and a high selectivity for beta 3 adrenaline receptors, wherein R1 represents hydrogen or halogeno; R2 represents hydrogen, hydroxy, lower alkoxy, lower alkoxy substituted by one or two lower alkoxycarbonyl or carboxy groups, lower alkoxy substituted by lower alkylaminocarbonyl optionally substituted by lower alkoxy, lower alkoxy substituted by cyclic C4-6 aminocarbonyl, lower alkoxycarbonyl, or carboxy; R3 represents hydrogen, hydroxy, lower alkoxy, or lower alkoxy substituted by one or two lower alkoxycarbonyl or carboxy groups, or R2 and R3 may be bonded to each other to thereby form methylenedioxy substituted by carboxy or lower alkoxycarbonyl; and m and n are each 0 or 1.
摘要翻译：由通式（I）表示的苯乙醇胺化合物及其药理学上可接受的盐具有刺激β3肾上腺素受体的强效果，对β3肾上腺素受体具有高选择性，其中R1表示氢或卤素; R 2表示氢，羟基，低级烷氧基，被一个或两个低级烷氧基羰基或羧基取代的低级烷氧基，被低级烷氧基取代的低级烷氧基取代的低级烷氧基，被环C 4-6氨基羰基取代的低级烷氧基，低级烷氧基羰基或羧基; R3表示氢，羟基，低级烷氧基或被一个或两个低级烷氧基羰基或羧基取代的低级烷氧基，或者R 2和R 3可以彼此键合，从而形成被羧基或低级烷氧基羰基取代的亚甲二氧基; m和n分别为0或1。

4. 发明申请

WO1996025396A1 PROCESS FOR PRODUCING INDOLINE COMPOUNDS AND INTERMEDIATES FOR THE PRODUCTION OF THE SAME 审中-公开
标题翻译：生产吲哚化合物的方法和用于生产吲哚化合物的中间体
公开(公告)号：WO1996025396A1
公开(公告)日：1996-08-22
申请号：PCT/JP1996000344
申请日：1996-02-16
申请人： TOKYO TANABE COMPANY LIMITED , YASUDA, Nobuyuki , KUNII, Shin-ichi , KAZAMA, Kouichi
发明人： TOKYO TANABE COMPANY LIMITED
IPC分类号： C07D209/08
CPC分类号： C07D209/08
摘要： A process for producing a 3-arylindoline compound represented by general formula (2), (wherein R represents optionally substituted phenyl or an aromatic heterocycle; and R represents hydrogen, halogeno, lower alkyl, hydroxy, lower alkoxy, carbamoyl or lower alkoxycarbamoyl) which is usable in the production of a 5-HT3 receptor antagonist 1-acyl-3-arylindoline compound represented by general formula (1), wherein R and R are as defined above; and R represents (a) or (b) on the basis of the facts that a 1-acyl-3-arylindole compound, obtained by binding an eliminable electron attractive group to the 1-position of a 3-arylindole compound by acylating the compound with an organic acid such as a carboxylic acid, sulfonic acid, etc., easily undergoes catalytic reduction under neutral or weakly acidic conditions to thereby give a 1-acyl-3-arylindoline compound; and that an optically active 1-acyl-3-arylindole compound, obtained by acylating a 3-arylindole compound with an organic acid such as an optically active carboxylic acid, sulfonic acid, etc., can give an optically active 1-acyl-3-arylindoline compound at a high selectivity by catalytic reduction.
摘要翻译：一种制备由通式（2）表示的3-芳基二氢吲哚化合物的方法，其中R 1表示任选取代的苯基或芳族杂环; R 2表示氢，卤代，低级烷基，羟基，低级烷氧基，氨基甲酰基或低级烷氧基氨基甲酰基），其可用于制备由通式（1）表示的5-HT 3受体拮抗剂1-酰基-3-芳基二氢化茚化合物，其中R 1和R 2如上所定义; 和R 3代表（a）或（b），基于以下事实：通过将3-可取代的吸电子基团与3-芳基吲哚化合物的1-位结合而获得的1-酰基-3-芳基吲哚化合物用有机酸如羧酸，磺酸等酰化化合物容易在中性或弱酸性条件下进行催化还原，从而得到1-酰基-3-芳基二氢吲哚化合物; 并且通过用有机酸如光学活性羧酸，磺酸等酰化3-芳基吲哚化合物获得的光学活性1-酰基-3-芳基吲哚化合物可以得到光学活性的1-酰基-3 - 二氢吲哚化合物通过催化还原以高选择性。

5. 发明申请

WO1995009168A1 INDOLINE COMPOUND AND 5-HT3 RECEPTOR ANTAGONIST CONTAINING THE SAME AS ACTIVE INGREDIENT 审中-公开
标题翻译：含有它们的吲哚化合物和5-HT3受体拮抗剂作为活性成分
公开(公告)号：WO1995009168A1
公开(公告)日：1995-04-06
申请号：PCT/JP1994001641
申请日：1994-09-30
申请人： TOKYO TANABE COMPANY LIMITED , TSUCHIYA, Shinji , YASUDA, Nobuyuki , FUKUZAKI, Atsushi , KAZAMA, Koichi
发明人： TOKYO TANABE COMPANY LIMITED
IPC分类号： C07D403/06
CPC分类号： C07D403/06
摘要： An indoline compound represented by general formula (I); a physiologically acceptable salt thereof; solvates of theses compounds; and a 5-HT3 receptor antagonist containing the same as the active ingredient. In formula (I) R represents the group (a) or (b), R represents optionally substituted phenyl or heteroaryl; and R represents hydrogen, halogen, lower alkyl, hydroxy, lower alkoxy, carbamoyl or lower alkoxycarbonyl. The compound has a potent antagonism against 5-HT3 receptors in the intestinal tract as compared with the known 5-HT3 receptor antagonists and is excellent in the persistence of the activity. Hence it is useful for preventing or treating vomiting or nausea induced by chemotherapy or radiation, irritable bowel syndrome and diarrhea.
摘要翻译：由通式（I）表示的二氢吲哚化合物; 其生理上可接受的盐; 这些化合物的溶剂合物; 和含有与活性成分相同的5-HT 3受体拮抗剂。在式（I）中，R 1表示（a）或（b）基团，R 2表示任选取代的苯基或杂芳基; R 3表示氢，卤素，低级烷基，羟基，低级烷氧基，氨基甲酰基或低级烷氧基羰基。与已知的5-HT 3受体拮抗剂相比，该化合物对肠道中的5-HT 3受体具有强烈的拮抗作用，并且活性持久性优异。因此，可用于预防或治疗由化疗或放射，肠易激综合征和腹泻引起的呕吐或恶心。

6. 发明申请

WO1992021658A1 QUINOLINE DERIVATIVE AND PRODUCTION THEREOF 审中-公开
标题翻译：喹啉衍生物及其生产
公开(公告)号：WO1992021658A1
公开(公告)日：1992-12-10
申请号：PCT/JP1992000693
申请日：1992-05-28
申请人： TOKYO TANABE COMPANY LIMITED , TSUCHIYA, Shinji , HIRATSUKA, Kouzou , YASUDA, Nobuyuki , FUKUZAKI, Atsushi , MATSUYAMA, Naoyuki
发明人： TOKYO TANABE COMPANY LIMITED
IPC分类号： C07D215/22
CPC分类号： C07D215/233 , C07D215/38 , C07D215/56 , C07D401/06 , C07D401/14 , C07D405/06 , C07D405/14
摘要： A 4-oxo-1,4-dihydroquinoline compound having a potent and selective 5-HT3 receptor antagonism, represented by general formula (I), an intermediate therefor, and a process for producing the same, wherein R represents optionally substituted phenyl or aromatic heterocyclic group; R represents hydrogen or methyl; R represents 5-(R )-1H-imidazol-4-yl or 4-(R )-1H-imidazol-5-yl; R represents hydrogen, amino or methylamino; and R represents methyl or ethyl.
摘要翻译：具有由通式（I）表示的有效和选择性的5-HT 3受体拮抗作用的4-氧代-1,4-二氢喹啉化合物及其制备方法，其中R 1表示任选取代的苯基或芳族杂环基; R 2表示氢或甲基; R 3表示5-（R 5）-1H-咪唑-4-基或4-（R 5）-1H-咪唑-5-基; R 4表示氢，氨基或甲基氨基; R 5表示甲基或乙基。

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