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1. 发明申请

WO1995018104A1 NOVEL BENZAMIDE DERIVATIVE AND MEDICINAL COMPOSITION CONTAINING THE SAME 审中-公开
标题翻译：新颖的苯甲酸衍生物和含有它们的药物组合物
公开(公告)号：WO1995018104A1
公开(公告)日：1995-07-06
申请号：PCT/JP1994002261
申请日：1994-12-27
申请人： YAMANOUCHI PHARMACEUTICAL CO., LTD. , SUZUKI, Takeshi , IMANISHI, Naoki , ITAHANA, Hirotsune , KAMATO, Takeshi , MIYATA, Keiji , OHTA, Mitsuaki
发明人： YAMANOUCHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07D207/09
CPC分类号： C07D265/30 , C07D207/09 , C07D211/26 , C07D223/04 , C07D241/04 , C07D241/08 , C07D243/08 , C07D267/10 , C07D279/12 , C07D281/06 , C07D453/02 , C07D487/08
摘要： A novel benzamide derivative represented by general formula (I), or a salt, hydrate or solvate thereof. The compound is useful as a 5-HT4 receptor agonist for preventing and treating central nervous system diseases such as schizophrenia, digestive tract movement disorders such as nausea, vomiting, irritable bowel syndrome, gastric ulcer and duodenal ulcer, heart action disorders such as cardiac failure, and urologic diseases such as urinary obstruction. It is also useful as an antinociceptive agent.
摘要翻译：由通式（I）表示的新型苯甲酰胺衍生物或其盐，水合物或溶剂合物。该化合物可用作预防和治疗中枢神经系统疾病如精神分裂症，消化道运动障碍如恶心，呕吐，肠易激综合征，胃溃疡和十二指肠溃疡，心脏功能障碍如心力衰竭的5-HT4受体激动剂，泌尿系统疾病如尿路梗阻。它也可用作抗伤害感受剂。

2. 发明申请

WO1994022874A1 CEPHALOSPORIN DERIVATIVE 审中-公开
标题翻译： CEPHALOSPORIN衍生物
公开(公告)号：WO1994022874A1
公开(公告)日：1994-10-13
申请号：PCT/JP1994000472
申请日：1994-03-24
申请人： YAMANOUCHI PHARMACEUTICAL CO., LTD. , HARA, Ryuichiro , ITAHANA, Hirotsune , SAKAMOTO, Kenichiro , HISAMICHI, Hiroyuki , NAGANO, Noriaki
发明人： YAMANOUCHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07D501/20
CPC分类号： C07D501/00 , Y02P20/55
摘要： A cephalosporin derivative represented by general formula (I) or a salt thereof, wherein R represents hydrogen, lower alkenyl, lower alkynyl, cycloalkyl, hydroxyl-protecting group, or (un)substituted lower alkyl; R represents hydrogen, ester residue, or negative charge; R represents either (1) a group represented by general formula (a), wherein R and R represent each independently lower alkoxy or (un)substituted amino, or R and R may be combined together with the neighboring tetrahydropyridazine ring to form an (un)substituted fused 5- or 6-membered ring, or (2) a group represented by general formula (b) or (c), wherein R and R represent each independently hydrogen, halogen, amino, azido, carbamoyl, lower alkyl which may be substituted by amino, azido, carbamoyl or halogen, carbamoyl, or (un)substituted 5- or 6-membered heterocyclic group (provided the nitrogen atom of the heterocycle may be substituted to form a quaternary amine); X represents methine (-CH=) or nitrogen; and ring A represents a 4- to 5-membered nitrogenous heterocycle which may contain oxygen.
摘要翻译：由通式（I）表示的头孢菌素衍生物或其盐，其中R 1表示氢，低级烯基，低级炔基，环烷基，羟基保护基或（取代的）取代的低级烷基; R 2表示氢，酯残基或负电荷; R 3表示（1）由通式（a）表示的基团，其中R 4和R 5各自独立地代表低级烷氧基或（未）取代的氨基，或R 4和R 5 可以与相邻的四氢哒嗪环一起形成（未）取代的稠合的5元或6元环，或（2）由通式（b）或（c）表示的基团，其中R 6和 R 7各自独立地表示氢，卤素，氨基，叠氮基，氨基甲酰基，可以被氨基，叠氮基，氨基甲酰基或卤素取代的低级烷基，氨基甲酰基或（取代的）取代的5-或6-元杂环基团杂环的氮原子可以被取代以形成季胺）; X表示次甲基（-CH =）或氮; 环A表示可含有氧的4-至5-元含氮杂环。

3. 发明申请

WO1995024399A1 5-HT3 RECEPTOR AGONIST, NOVEL THIAZOLE DERIVATIVE, AND INTERMEDIATE THEREFOR 审中-公开
标题翻译： 5-HT3受体激动剂，新型噻唑衍生物及其中间体
公开(公告)号：WO1995024399A1
公开(公告)日：1995-09-14
申请号：PCT/JP1995000385
申请日：1995-03-09
申请人： YAMANOUCHI PHARMACEUTICAL CO., LTD. , IWAOKA, Kiyoshi , ANAN, Hideki , IMANISHI, Naoki , KAZUTA, Kenichi , KOSHIO, Hiroyuki , SUZUKI, Takeshi , ITAHANA, Hirotsune , ITO, Hiroyuki , MIYATA, Keiji , OHTA, Mitsuaki
发明人： YAMANOUCHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07D277/28
CPC分类号： C07D277/60 , C07D417/04 , C07D417/06 , C07D417/14 , C07D471/04 , C07D471/08 , C07D487/04 , C07D487/08 , C07D513/04 , Y02P20/55
摘要： A 5-HT3 receptor agonist containing a thiazole derivative represented by general formula (I) as the active ingredient, a specified compound useful as a 5-HT3 receptor agonist, and a specified thioamide derivative useful as an intermediate therefor, wherein ring A represents one of the following rings which may be substituted by at least one substituent selected from the group consisting of halogen, lower alkyl and lower alkoxy: (1) a benzene ring, and (2) a 5- or 6-membered unsaturated heterocycle having one or two heteroatoms selected from among nitrogen, oxygen and sulfur; one of L and L represents a single bond, and the other of them is absent, or represents C1-C4 alkylene or C2-C5 alkenylene; R represents a group represented by any of general formulae: (1), (2), (3) and (4); L represents lower alkylene; L represents a single bond or lower alkylene; R and R represent each independently hydrogen, lower alkyl or an amino-protecting group; R represents hydrogen, lower alkyl, oxo or optionally protected amino; R is absent, or represents hydrogen, lower alkyl, aralkyl or an amino-protecting group; ring B represents one of the following rings which are either monocyclic or bicyclic and may bear an oxygen atom(s): (1) a nitrogenous saturated heterocycle bearing four to sixteen ring atoms, and (2) a nitrogenous heterocycle having a double bond and bearing four to sixteen ring atoms: and ring D represents a saturated carbocycle bearing four to eight ring atoms; provided the nitrogen atom of R may form an unsubstituted quaternary ammonium salt.
摘要翻译：含有由通式（I）表示的噻唑衍生物作为活性成分的5-HT 3受体激动剂，可用作5-HT 3受体激动剂的特定化合物和用作其中间体的特定硫代酰胺衍生物，其中环A表示1 可以被选自卤素，低级烷基和低级烷氧基的至少一个取代基取代的以下环：（1）苯环，和（2）具有一个或多个的一个或多个的5-或6-元不饱和杂环，选自氮，氧和硫的两个杂原子; L 1和L 2之一表示单键，另一个不存在，或表示C1-C4亚烷基或C2-C5亚烯基; R表示由通式（1），（2），（3）和（4）中的任一个表示的基团。 L 3表示低级亚烷基; L 4代表单键或低级亚烷基; R 1和R 2各自独立地表示氢，低级烷基或氨基保护基; R 3表示氢，低级烷基，氧代或任选保护的氨基; R 4不存在，或表示氢，低级烷基，芳烷基或氨基保护基; 环B表示单环或双环的以下环之一，并且可以带有氧原子：（1）具有4至16个环原子的含氮饱和杂环，和（2）具有双键的含氮杂环和具有四至十六个环原子：环D表示带有四至八个环原子的饱和碳环; 条件是R的氮原子可以形成未取代的季铵盐。

4. 发明申请

WO1998006724A1 METABOTROPIC GLUTAMATE RECEPTOR AGONISTS 审中-公开
标题翻译：代谢谷氨酸受体激动剂
公开(公告)号：WO1998006724A1
公开(公告)日：1998-02-19
申请号：PCT/JP1997002748
申请日：1997-08-07
申请人： YAMANOUCHI PHARMACEUTICAL CO., LTD. , HAYASHIBE, Satoshi , ITAHANA, Hirotsune , YAHIRO, Kiyoshi , TSUKAMOTO, Shin-ichi , OKADA, Masamichi , YAMASHITA, Hiroshi
发明人： YAMANOUCHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07D513/04
CPC分类号： C07D513/04 , A61K31/00 , A61K31/429
摘要： Medicinal compositions containing compounds represented by general formula (I) or pharmaceutically acceptable salts thereof having metabotropic glutamate receptor agonism and thus being useful as remedies for various diseases which can be cured or relieved thereby, in particular, epilepsy, pain, Parkinson's syndrome, etc.; the use of these compounds for producing these compositions; methods for treating the above-mentioned diseases through the administration of these compounds in effective dosages; and novel imidazobenzothiazole derivatives (II and III) or pharmaceutically acceptable salts thereof which are useful as remedies for the above-mentioned diseases, wherein the ring A represents an optionally substituted aryl, monocyclic heterocycle or dicyclic heterocycle group; R represents H, halogeno, lower alkyl, hydroxy(lower alkyl), lower alkoxy(lower alkyl) or lower alkoxy; R to R represent each a substituent selected from among various ones such as H, halogeno, lower alkyl, CN, NO2, alkoxy, thiol, carboxylate, sulfonate, carbamoyl, amine, substituted alkyl and heterocycles; R to R represent the same substituents as those of R to R excluding specific substituents and combinations thereof; and R represents hydroxymethyl, etc.
摘要翻译：含有由通式（I）表示的化合物或其药学上可接受的盐的代谢型谷氨酸受体激动剂的药用组合物，因此可用作可由其治愈或缓解的各种疾病，特别是癫痫，疼痛，帕金森综合症等的补救措施。 ; 这些化合物用于制备这些组合物的用途; 通过以有效剂量施用这些化合物来治疗上述疾病的方法; 和其可用作上述疾病的补救剂的新型咪唑并噻唑衍生物（II和III）或其药学上可接受的盐，其中环A表示任选取代的芳基，单环杂环或二环杂环基; R 1表示H，卤代，低级烷基，羟基（低级烷基），低级烷氧基（低级烷基）或低级烷氧基; R 2至R 5各自表示选自各种如H，卤代，低级烷基，CN，NO 2，烷氧基，硫醇，羧酸酯，磺酸酯，氨基甲酰基，胺，取代的烷基和杂环的取代基。 R 11至R 14代表与R 2至R 5相同的取代基，不包括特定取代基及其组合; R 13表示羟甲基等。

5. 发明申请

WO1996005166A1 SUBSTITUTED AMINE DERIVATIVE AND MEDICINAL COMPOSITION CONTAINING THE SAME 审中-公开
标题翻译：取代的胺衍生物和含有其的药物组合物
公开(公告)号：WO1996005166A1
公开(公告)日：1996-02-22
申请号：PCT/JP1995001587
申请日：1995-08-09
申请人： YAMANOUCHI PHARMACEUTICAL CO., LTD. , SUZUKI, Takeshi , IMANISHI, Naoki , ITAHANA, Hirotsune , WATANUKI, Susumu , KAMATO, Takeshi , MIYATA, Keiji , OHTA, Mitsuaki
发明人： YAMANOUCHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07C211/35
CPC分类号： C07D213/82 , C07C237/44 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07D209/42 , C07D211/58 , C07D215/54 , C07D235/06 , C07D235/26 , C07D235/30 , C07D265/36 , C07D307/79 , C07D309/14 , C07D311/74 , C07D319/18 , C07D333/34 , C07D333/38 , C07D335/02 , C07D471/04
摘要： A substituted amine derivative represented by general formula (I), having an agonistic activity on 5-HT4 receptors, and useful as a 5-HT4 receptor agonist for preventing and/or treating diseases accompanied with the insufficiency of such an agonistic activity, such as central nervous system disorder or digestive tract movement disorder, a pharmaceutically acceptable salt thereof, a medicinal composition containing the same, and an intermediate represented by general formula (IIIa) wherein ring A represents a benzene ring, a heterocycle containing N, S or O, etc.; X represents -CONR5-, etc.; R and R represent each hydrogen or lower alkyl; ring B represents a cycloalkane ring or a heterocycle containing N, S or O; and R and R represent each hydrogen or lower alkyl, or R , R and the adjacent nitrogen atom are combined together to represent a heterocycle.
摘要翻译：由通式（I）表示的取代胺衍生物，其具有对5-HT 4受体的激动作用，可用作5-HT 4受体激动剂，用于预防和/或治疗伴随这种激动活性不足的疾病，例如中枢神经系统疾病或消化道运动障碍，其药学上可接受的盐，含有它们的药物组合物和由通式（IIIa）表示的中间体，其中环A表示苯环，含有N，S或O的杂环，等等。; X代表-CONR5-等; R 1和R 2各自代表氢或低级烷基; 环B表示环烷烃环或含有N，S或O的杂环; R 3和R 4分别代表氢或低级烷基，或R 3，R 4和相邻的氮原子结合在一起代表杂环。

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