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21. 发明专利

JPS63115859A ANTI-INFLAMMATORY AGENT CONTAINING 2-PYRROLIDONE DERIVATIVE 失效
公开(公告)号：JPS63115859A
公开(公告)日：1988-05-20
申请号：JP25853686
申请日：1986-10-31
申请人： EISAI CO LTD
发明人： IKUTA HIRONORI , YAMAGISHI YOJI , AKASAKA KOZO , YAMATSU ISAO , KOBAYASHI SEIICHI , SHIROTA HIROSHI , KATAYAMA KOICHI
IPC分类号： A61K31/40 , A61K31/4015 , A61P25/04 , A61P29/00 , C07D207/38 , C07D207/46
摘要： PURPOSE:To provide the titled agent containing a 2-pyrrolidone derivative as an active component, having high safety, exhibiting lipoxygenase-inhibiting action and antioxidation action, free from side effect of gastric disorder and effective to arthritis, rheumatism, neuritis, cold syndrome, etc. CONSTITUTION:The objective agent contains a 2-pyrrolidone derivative of formula I [R is H, lower alkyl, lower alkoxy, lower alkynyl or group of formula -(CH2)n-X (X is phenyl, hydroxyl or NR R ; R and R are same or different H or lower alkyl; n is 1 or 2)] or its pharmacologically permissible salt as an active component. It is administered orally in the form of powder, capsule, etc., or parenterally as suppository, injection, etc. The active component compound of formula I can be produced by reacting 3,5-di-tert-butyl-4- hydroxybenzaldehyde of formula II with a Wittig reagent of formula III.

22. 发明专利

JPS6310743A SUBSTITUTED DIPHENYLETHYLENE DERIVATIVE 失效
公开(公告)号：JPS6310743A
公开(公告)日：1988-01-18
申请号：JP6002287
申请日：1987-03-17
申请人： EISAI CO LTD
发明人： YAMAGISHI YOJI , AKASAKA KOZO , SUZUKI TAKESHI , MIYAMOTO MITSUAKI , NAKAMOTO KOJI , OKANO KAZUO , ABE SHINYA , IKUTA HIRONORI , HAYASHI KENJI , YOSHIMURA HIROYUKI , FUJIMORI TORU , HARADA KOKICHI , YAMATSU ISAO
IPC分类号： C07C57/42 , A61K31/165 , A61K31/18 , A61K31/19 , A61K31/215 , A61K31/22 , A61K31/275 , A61K31/277 , A61K31/33 , A61P7/02 , A61P9/08 , A61P9/10 , C07C51/00 , C07C59/64 , C07C67/00 , C07C69/618 , C07C231/00 , C07C231/02 , C07C233/11 , C07C235/34 , C07C237/20 , C07C239/00 , C07C241/00 , C07C253/00 , C07C253/30 , C07C255/34 , C07C255/37 , C07C255/41 , C07C255/61 , C07C257/04 , C07C257/10 , C07C301/00 , C07C303/38 , C07C311/00 , C07C325/00 , C07C327/58 , C07D213/40 , C07D213/72 , C07D213/75
摘要： NEW MATERIAL:A compound expressed by formula I [R and R are H, OH or lower alkoxy; X is H, CN or the formula -COR (R is OH or NH2); Y is Alk-COOR (Al is 1-3C alkylene; R is H or lower alkyl); formula II (R and R are H, lower alkyl, arylalkyl, etc.), etc.] and pharmacologically acceptable salt thereof. EXAMPLE:N-Benzyl-3,3-bis-(4-methoxyphenyl)acrylamide. USE:An antiblood platelet and antithrombotic agent. PREPARATION:A carboxylic acid expressed by formula III or a reactive derivative thereof is reacted with an amine expressed by formula IV in a solvent, e.g. THF, etc., at -50-+200 deg.C to afford the aimed compound expressed by formula I, etc.

23. 发明专利

JPS61257967A 2-PYRROLIDONE DERIVATIVE 失效
公开(公告)号：JPS61257967A
公开(公告)日：1986-11-15
申请号：JP9679985
申请日：1985-05-09
申请人： EISAI CO LTD
发明人： IKUTA HIRONORI , YAMAGISHI YOJI , AKASAKA KOZO , YAMATSU ISAO , KOBAYASHI SEIICHI , SHIROTA HIROSHI , KATAYAMA KOICHI
IPC分类号： A61K31/40 , A61K31/4015 , A61P25/04 , A61P29/00 , C07D207/36 , C07D207/38 , C07D207/46 , C07D207/50 , C07F9/572
摘要： NEW MATERIAL:A compound expressed by formula I {R is H, alkyl, alkoxy, alkynyl or -(CH2)n-X [X is phenyl, OH or -NR R (R and R are H or alkyl); n is 1 or 2]} and a salt thereof. EXAMPLE:N-Methyl-3-(3,5-di-tert-butyl-4-hydroxybenzylidene)-2-pyrrolid one. USE:An anti-inflammatory, analgesic and antipyretic agent. PREPARATION:3,5-Di-tert-butyl-4-hydroxybenzaldehyde and a compound expressed by formula II are subjected to the Witting reaction in a solvent, e.g. DMF or benzene, at 30-100 deg.C to afford the aimed compound expressed by formula I, etc.

24. 发明专利

JPS61257959A SUBSTITUTED BENZOPHENONE-OXIME ETHER DERIVATIVE 失效
公开(公告)号：JPS61257959A
公开(公告)日：1986-11-15
申请号：JP9679885
申请日：1985-05-09
申请人： EISAI CO LTD
发明人： AKASAKA KOZO , YAMAGISHI YOJI , IKUTA HIRONORI , YAMATSU ISAO , FUJIMORI TORU , HARADA KOKICHI , SHIOJIRI HIROYUKI
IPC分类号： C07D295/08 , A61K31/15 , A61K31/275 , A61K31/445 , A61K31/535 , A61K31/5375 , A61P7/02 , C07C67/00 , C07C239/00 , C07C251/50 , C07C251/58
摘要： NEW MATERIAL:A compound expressed by formula I [R and R are H, lower alkoxy or halogen; X is formula II (R and R are H or lower alkyl), formula III (the ring A may contain N or O) or cyano; n is an integer 1-3, except when both R and R are H and n is 2]. EXAMPLE:4, 4'-Dimethoxybenzophenone-oxime dimethylaminoethyl ether hydro chloride. USE:An antiblood platelet and antithrombotic agent having improved inhibitory action on blood platelet agglutination. PREPARATION:A benzophenone compound expressed by formula IV is reacted with hydroxylamine to give a benzophenone-oxime expressed by formula V, which is then reacted with a halide expressed by the formula Hal-(CH2)n-X (Hal is halogen) in a solvent, e.g. dimethylformamide, preferably in the presence of a base, e.g. NaH, at 0-100 deg.C to afford the aimed compound expressed by formula I.

25. 发明专利

JPS5993084A 3-UNSUBSTITUTED-3-CEPHEM DERIVATIVE, ITS PREPARATION AND ANTIBACTERIAL AGENT COMPOSED THEREOF 失效
公开(公告)号：JPS5993084A
公开(公告)日：1984-05-29
申请号：JP20186882
申请日：1982-11-19
申请人： EISAI CO LTD
发明人： IKUTA HIRONORI , YAMAUCHI HIROSHI , MACHIDA YOSHIMASA , NOMOTO SEIICHIROU , NEGI SHIGETO , SUGIYAMA ISAO , SAITOU ISAO
IPC分类号： C07D501/20 , A61K31/545 , A61K31/546 , A61P31/04 , C07D501/22 , C07D501/57
摘要： NEW MATERIAL:The compound of formula I (R1 is H or methoxy; R2 is H or OH) and its non-toxic salt. EXAMPLE:7beta-[ D-2-( 6,7-Dihydroxychromone-3-carboxamido )-2-( 4-hydroxyphenyl)- acetamido]-3-cephem-4-carboxylic acid. USE:An antibacterial agent effective to Gram-negative bacteria such as Pseudomonas aeruginosa. Some of the compound of formula I are low-toxic. PROCESS:The compound of formula I can be prepared by reacting the compound of formula II or its salt with the compound of formula III or its reactive derivative in a solvent such as acetone in the presence of a silylation agent. The reaction is carried out by the conventional method of amidation reaction, e.g. in the presence of a condensation agent such as N,N'-dicyclohexylcarbodiimide.

26. 发明专利

JPS5867698A 3-(2-BENZIMIDAZOLYL)THIOMETHYL-3-CEPHEM DERIVATIVE AND ITS PREPARATION 失效
公开(公告)号：JPS5867698A
公开(公告)日：1983-04-22
申请号：JP16567181
申请日：1981-10-19
申请人： EISAI CO LTD
发明人： IKUTA HIRONORI , NOMOTO SEIICHIROU , TAKAYANAGI KEIZOU , MACHIDA YOSHIMASA , YAMAUCHI HIROSHI , KANAI TAKEO , SAITOU ISAO
IPC分类号： C07D501/36
摘要： NEW MATERIAL:The 3-(2-benzimidazolyl)thiomethyl-3-cephem derivative of formulaIor its salt. EXAMPLE:7beta-[D-2-(6,7-dihydroxychromone-3-carboxamido)-2-(4-hydroxy- phenyl) acetamido]-3-(2-benzimidazolyl)thiomethyl-3-cephem-4-carboxylic acid. USE:Antibacterial agent. PROCESS:The objective compound is prepared by reacting the compound of formula II with the compound of formula III in a solvent preferably such as water, a buffer solution, etc. in the presence of a base such as sodium hydroxide, at 50-80 deg.C.

27. 发明专利

JPS5791990A 7ALPHA-METHOXYCEPHEM DERIVATIVE, ITS PREPARATION AND ANTIMICROBIAL AGENT CONSISTING OF THE SAME 失效
公开(公告)号：JPS5791990A
公开(公告)日：1982-06-08
申请号：JP16737180
申请日：1980-11-29
申请人： EISAI CO LTD
发明人： MACHIDA YOSHIMASA , SAITOU ISAO , NOMOTO SEIICHIROU , NEGI SHIGETO , IKUTA HIRONORI , KITOU KIYOUSUKE
IPC分类号： C07D501/57 , A61K31/545 , A61K31/546 , A61P31/04
摘要： NEW MATERIAL:A compound of formulaI(R1 is H or hydroxyl group; R2 is lower alkyl or chlorine-substituted lower alkyl; R3 is acyloxy or heterocyclic thio group containing nitrogen) and a nontoxic salt thereof. EXAMPLE:7beta-[D-2-[6,7-Bis(ethoxycarbonyloxy)chromone-3-carboxamido]2 -(4- hydroxyphenyl)acetamido]-7alpha-methoxy-3-(1-methoxycarbonylmethyl-5-t etrazolyl) thiomethyl-3-cephem-4-carboxylic acid. USE:An antimicrobial agent effective against Gram-positive and Gram-negative bacteria, particularly clinically intractable bacteria, e.g. Proteus morganii, and germs capable of producing beta-lactamase. PROCESS:A compound of formula II or a salt thereof is reacted with a compound of formula III or a reactive derivative thereof, e.g. an acid chloride, in an inert solvent, in the presence or absence of a basic reagent or silylating agent to give the compound of formulaI.

28. 发明专利

JPS5759883A Production of chromone-3-carboxylic acid 失效
标题翻译：生产氯仿-3-羧酸
公开(公告)号：JPS5759883A
公开(公告)日：1982-04-10
申请号：JP13530180
申请日：1980-09-30
申请人： Eisai Co Ltd
发明人： MACHIDA YOSHIMASA , NOMOTO SEIICHIROU , NEGI SHIGETO , IKUTA HIRONORI , SAITOU ISAO
IPC分类号： C07D311/22
摘要： PURPOSE: The reaction between a chromone-3-carboxyldehyde and an N-halogenosuccinimide is followed by the hydrolysis of the product to produce the titled compound used as an antiallergic without difficulty in waste water disposition.
CONSTITUTION: The reaction between a compound of formulaI(R is H, monovalent substituent; n is 1, 2) and an N-halogenosuccinimide is effected in a solvent such as dichloromethane under irradiation with light at 40W100°C. Then, the product is hydrolyzed with water to give chromone-3-carboxylic acid of formula II. The compound of formula II also is used as a synthetic intermediate of an antibiotic. The waste water from the process can be satisfactorily disposed by a usual method such as the activated sludge process.
COPYRIGHT: (C)1982,JPO&Japio
摘要翻译：目的：色酮-3-羧甲醛与N-卤代琥珀酰亚胺反应后，产物水解，产生用作抗过敏剂的标题化合物，难以在废水中处理。构成：式Ⅰ化合物（R为H，一价取代基; n为1,2）与N-卤代琥珀酰亚胺之间的反应在溶剂如二氯甲烷中，在40-100℃的光照射下进行。然后，将产物用水水解，得到式II的色酮-3-羧酸。式II的化合物也可用作抗生素的合成中间体。来自该方法的废水可以通过常规方法如活性污泥法令人满意地处理。

29. 发明专利

JP2004043429A New xanthine derivative and dppiv inhibitor 审中-公开
标题翻译：新西兰衍生物和DPPIV抑制剂
公开(公告)号：JP2004043429A
公开(公告)日：2004-02-12
申请号：JP2003044771
申请日：2003-02-21
申请人： Eisai Co Ltd , エーザイ株式会社
发明人： YOSHIKAWA SEIJI , EMORI EITA , MATSUURA FUMIYOSHI , CLARK RICHARD , IKUTA HIRONORI , YASUDA NOBUYUKI , NAGAKURA TEI , YAMAZAKI KAZUTO , AOKI MIKA
IPC分类号： C07D473/04 , A61K31/522 , A61K31/551 , A61P1/04 , A61P3/04 , A61P3/06 , A61P3/10 , A61P5/00 , A61P9/00 , A61P15/08 , A61P19/10 , A61P29/00 , A61P31/18 , A61P35/00 , A61P37/02 , A61P37/08 , A61P43/00 , C07D473/06 , C07D473/08 , C07D487/22 , C07D519/00
摘要： PROBLEM TO BE SOLVED: To provide a new compound exhibiting excellent DPPIV (dipeptidyl peptidase IV) inhibiting action. SOLUTION: The new compound exhibiting excellent DPPIV inhibiting action is represented by general formula (1) (wherein m is 0 or 1; n is 0; R 31 , R 32 , R 33 , R 34 , R 35 , R 36 , R 37 , R 38 , R 39 , R 40 , R 41 and R 42 are each a hydrogen atom; X is an alkynyl group, an aryl group or the like which may be substituted; R 1 and R 2 are each independently a hydrogen atom, an alkyl group, an alkoxy group or the like), its salt or a hydrate thereof. COPYRIGHT: (C)2004,JPO
摘要翻译：要解决的问题：提供显示优异的DPPIV（二肽基肽酶IV）抑制作用的新化合物。解决方案：通过通式（1）（其中m是0或1; n是0; SP>，R 33 ，R 34 ，R 35 ，R SP SP 36， SP>，R 38 ，R 39 ，R 40 ，R SP SP 41， SP>各自为氢原子; X为可被取代的炔基，芳基等; R SP 1和R SP 2各自独立地为氢原子，烷基，烷氧基等），其盐或其水合物。版权所有（C）2004，JPO

30. 发明专利

JPH072726A SUBSTITUTED DIPHENYLETHYLENE DERIVATIVE 失效
公开(公告)号：JPH072726A
公开(公告)日：1995-01-06
申请号：JP2113894
申请日：1994-02-18
申请人： EISAI CO LTD
发明人： YAMAGISHI YOJI , AKASAKA KOZO , SUZUKI TAKESHI , MIYAMOTO MITSUAKI , NAKAMOTO KOJI , OKANO KAZUO , ABE SHINYA , IKUTA HIRONORI , HAYASHI KENJI , YOSHIMURA HIROYUKI , FUJIMORI TORU , HARADA KOKICHI , YAMATSU ISAO
IPC分类号： A61K31/135 , A61K31/165 , A61K31/18 , A61K31/19 , A61K31/215 , A61P7/02 , A61P9/00 , A61P9/08 , A61P9/10 , C07C57/48 , C07C59/48 , C07C59/68 , C07C233/11 , C07C235/34 , C07C255/41 , C07C255/42 , C07C255/61 , C07C311/02 , C07C311/16
摘要： PURPOSE:To provide a new substituted diphenylethylene derivative having an excellent platelet aggregation-inhibiting action and useful as an antiplatelet agent or an antithrombogenic agent. CONSTITUTION:A compound of formula I {R , R are H, OH, lower alkoxy; X is H, CN, C(=O)R (R is OH, NH2); Y is -Alk-COOR (Alk is 1-3C alkylene which may be branched; R is H, lower alkyl), group of formula II (R , R are H, lower alkyl, arylalkyl, heteroarylalkyl), CH2-NH-SO2R (R is lower alkyl, aryl), group of formula III; R is lower alkyl, aryl; R is Z-R [Z is O, S, NR (R is H, lower alkyl); R is lower alkyl, lower alkenyl, aryl], group of formula IV (R is H, lower alkyl)}, e.g. N[3,3-bis(4-methoxyphenyl)allyl]- benzenesulfonamide. The compound of formula I in which Y is the group of formula II is obtained by reacting a caboxylic acid compound of formula V with an amine of formula VI.

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