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21. 发明专利

AU2005202135A1 2-Iminopyrrolidine derivatives 未知
公开(公告)号：AU2005202135A1
公开(公告)日：2005-06-09
申请号：AU2005202135
申请日：2005-05-17
申请人： EISAI CO LTD
发明人： KOGUSHI MOTOJI , KOTAKE MAKOTO , MATSUOKA TOSHIYUKI , MATSUURA FUMIYOSHI , MIYAMOTO MITSUAKI , MIYAZAWA SYUHEI , NAOE YOSHIMITSU , OKANO KAZUO , ONO NAOTO , OOHASHI YOSHIAKI , OZAKI FUMIHIRO , SATO NOBUAKI , SHINODA MASANOBU , SUZUKI SHUICHI , TANAKA HIROSHI , TERAUCHI TARO , TSUKADA ITARU , MUSHA TAKASHI , CHIBA KEN-ICHI , CLARK RICHARD , HISHINUMA IEHARU , ITO OSAMU , KAJIWARA AKIHARU , KAMADA ATSUSHI , KAWATA TSUTOMU , KAWAHARA TETSUYA , KIMURA AKIFUMI , KOBAYASHI HIROKO
IPC分类号： A61K20060101 , A61K31/403 , A61K31/4035 , A61K31/4178 , A61K31/4184 , A61K31/422 , A61K31/437 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/538 , A61P20060101 , A61P7/02 , A61P9/00 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P13/12 , A61P19/10 , A61P25/00 , A61P29/00 , A61P35/00 , A61P43/00 , C07D20060101 , C07D207/22 , C07D207/24 , C07D207/26 , C07D207/263 , C07D207/267 , C07D207/34 , C07D209/44 , C07D209/52 , C07D209/54 , C07D209/62 , C07D209/96 , C07D213/73 , C07D213/74 , C07D233/46 , C07D233/66 , C07D233/88 , C07D233/90 , C07D235/30 , C07D249/14 , C07D261/14 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/10 , C07D403/12 , C07D405/06 , C07D409/04 , C07D409/06 , C07D409/10 , C07D413/06 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/10 , C07D471/04 , C07D487/04 , C07D491/10 , C07D498/04 , C07D521/00
摘要： The present invention relates to a 2-iminopyrrolidine derivative selected from the group consisting of 1-(3-tert-butyl-4-methoxy-5-morpholino-phenyl)-2-(5,6-diethoxy-7-fluoro-1-imino-1,3-dihydro-isoindol-2-yl)-ethanone; 1-{3-tert-butyl-5-[4-(2-hydroxy-acetyl)piperazin-1-yl]-4-methoxyphenyl}-2-(5,6-diethoxy-7-fluoro-1-imino-1,3-diyhdro-isoindol-2-yl)-ethanone; ethyl (4-{3-tert-butyl-5-[2-(5,6-diethoxy-7-fluoro-1-imino-1,3-dihydro-isoindol-2-yl)-acetyl]-2-methoxy-phenyl}piperazin-1-yl)-acetate; 1-(3-tert-butyl-4-methoxy-5-piperazin-1-yl-phenyl)-2-(5,6-diethoxy-7-fluoro-1-imino-1,3-dihydro-isoindol-2-yl)-ethanone, and (4-{3-tert-butyl-5-[2-(5,6-diethoxy-7-fluoro-1-imino-1,3-dihydro-isoindol-2-yl)-acetyl]-2-methoxy-phenyl}-piperazin-1-yl)-acetic acid; and salts thereof.

22. 发明专利

HU0400467A2 2-IMINOPYRROLIDINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND THEIR USE 未知
公开(公告)号：HU0400467A2
公开(公告)日：2005-02-28
申请号：HU0400467
申请日：2002-04-19
申请人： EISAI CO LTD
发明人： SUZUKI SHUICHI , KOTAKE MAKOTO , MIYAMOTO MITSUAKI , KAWAHARA TETSUYA , KAJIWARA AKIHARU , HISHINUMA IEHARU , OKANO KAZUO , MIYAZAWA SYUHEI , CLARK RICHARD , OZAKI FUMIHIRO , SATO NOBUAKI , SHINODA MASANOBU , KAMADA ATSUSHI , TSUKADA ITARU , MATSUURA FUMIYOSHI , NAOE YOSHIMITSU , TERAUCHI TARO , OOHASHI YOSHIAKI , ITO OSAMU , TANAKA HIROSHI , MUSHA TAKASHI , KOGUSHI MOTOJI , KAWATA TSUTOMU , MATSUOKA TOSHIYUKI , KOBAYASHI HIROKO , CHIBA KEN-ICHI , KIMURA AKIFUMI , ONO NAOTO
IPC分类号： A61K20060101 , A61K31/403 , A61K31/4035 , A61K31/4178 , A61K31/4184 , A61K31/422 , A61K31/437 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/538 , A61P20060101 , A61P7/02 , A61P9/00 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P13/12 , A61P19/10 , A61P25/00 , A61P29/00 , A61P35/00 , A61P43/00 , C07D20060101 , C07D207/22 , C07D207/24 , C07D207/26 , C07D207/263 , C07D207/267 , C07D207/34 , C07D209/44 , C07D209/52 , C07D209/54 , C07D209/62 , C07D209/96 , C07D213/73 , C07D213/74 , C07D233/46 , C07D233/66 , C07D233/88 , C07D233/90 , C07D235/30 , C07D249/14 , C07D261/14 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/10 , C07D403/12 , C07D405/06 , C07D409/04 , C07D409/06 , C07D409/10 , C07D413/06 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/10 , C07D471/04 , C07D487/04 , C07D491/10 , C07D498/04 , C07D521/00
摘要： The present invention relates to a 2-iminopyrrolidine derivative selected from the group consisting of 1-(3-tert-butyl-4-methoxy-5-morpholino-phenyl)-2-(5,6-diethoxy-7-fluoro-1-imino-1,3-dihydro-isoindol-2-yl)-ethanone; 1-{3-tert-butyl-5-[4-(2-hydroxy-acetyl)piperazin-1-yl]-4-methoxyphenyl}-2-(5,6-diethoxy-7-fluoro-1-imino-1,3-diyhdro-isoindol-2-yl)-ethanone; ethyl (4-{3-tert-butyl-5-[2-(5,6-diethoxy-7-fluoro-1-imino-1,3-dihydro-isoindol-2-yl)-acetyl]-2-methoxy-phenyl}piperazin-1-yl)-acetate; 1-(3-tert-butyl-4-methoxy-5-piperazin-1-yl-phenyl)-2-(5,6-diethoxy-7-fluoro-1-imino-1,3-dihydro-isoindol-2-yl)-ethanone, and (4-{3-tert-butyl-5-[2-(5,6-diethoxy-7-fluoro-1-imino-1,3-dihydro-isoindol-2-yl)-acetyl]-2-methoxy-phenyl}-piperazin-1-yl)-acetic acid; and salts thereof.

23. 发明专利

DE60014390D1 未知
公开(公告)号：DE60014390D1
公开(公告)日：2004-11-04
申请号：DE60014390
申请日：2000-07-27
申请人： EISAI CO LTD
发明人： KAYANO AKIO , CHIBA HIROYUKI , NAKAMURA TAIJU , SAKURAI SHIN , ISHIZUKA HIROYUKI , SAITO HIROYUKI , KOMATSU YUUKI , SASHO MANABU , SATO NOBUAKI , NEGI SHIGETO
IPC分类号： C07D477/02 , C07D477/08 , C07D477/20 , C07D499/68 , C07D501/22 , C07D501/36 , C07D501/46 , C07D463/00 , C07D499/00 , C07D501/00
摘要： The present invention provides: an industrially-excellent and novel process for producing a basic antibiotic.inorganic acid salt, for example, an excellent production process for producing a hydrochloride thereof industrially, that is, a production process which comprises subjecting a basic antibiotic.oxalate (II) to salt-exchange with an alkali earth metal salt (III) of an inorganic acid: (wherein the ring A means the basic antibiotic; R means a protected functional group used in organic synthesis; Ak-E means the alkali earth metal; and B means the inorganic acid, respectively); a novel oxalate useful as a production intermediate for producing an antibiotic.hydrochloride industrially, that is, an oxalate (II-I) of a carbapenem compound represented by the following formula: (wherein the ring A represents a 3- to 7-membered ring having at least one nitrogen atom, and the ring A may be substituted with other than R ; R represents hydrogen or methyl group; R and R are the same as or different form each other and each represents hydrogen or a hydroxyl-protecting group; R represents a carboxyl-protecting group; R represents hydrogen, a lower alkyl group or an amino-protecting group; R represents (1) hydrogen, (2) an optionally protected hydroxyl group, carbamoyl, formimidoyl, acetoimidoyl or a lower alkyl group which may be substituted with a substituent represented by the formula: (wherein R and R are the same as or different from each other and each represents hydrogen, a lower alkyl group or an amino-protecting group) or (3) an amino-protecting group or an imino-protecting group; and m is 0 or 1); and a process for producing its.

24. 发明专利

CZ20032824A3 未知
公开(公告)号：CZ20032824A3
公开(公告)日：2004-04-14
申请号：CZ20032824
申请日：2002-04-19
申请人： EISAI CO LTD
发明人： SUZUKI SHUICHI , KOTAKE MAKOTO , MIYAMOTO MITSUAKI , KAWAHARA TETSUYA , KAJIWARA AKIHARU , HISHINUMA IEHARU , OKANO KAZUO , MIYAZAWA SYUHEI , CLARK RICHARD , OZAKI FUMIHIRO , SATO NOBUAKI , SHINODA MASANOBU , KAMADA ATSUSHI , TSUKADA ITARU , MATSUURA FUMIYOSHI , NAOE YOSHIMITSU , TERAUCHI TARO , OOHASHI YOSHIAKI , ITO OSAMU , TANAKA HIROSHI , MUSHA TAKASHI , KOGUSHI MOTOJI , KAWATA TSUTOMU , MATSUOKA TOSHIYUKI , KOBAYASHI HIROKO , CHIBA KEN-ICHI , KIMURA AKIFUMI , ONO NAOTO
IPC分类号： A61K20060101 , A61K31/403 , A61K31/4035 , A61K31/4178 , A61K31/4184 , A61K31/422 , A61K31/437 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/538 , A61P20060101 , A61P7/02 , A61P9/00 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P13/12 , A61P19/10 , A61P25/00 , A61P29/00 , A61P35/00 , A61P43/00 , C07D20060101 , C07D207/22 , C07D207/24 , C07D207/26 , C07D207/263 , C07D207/267 , C07D207/34 , C07D209/44 , C07D209/52 , C07D209/54 , C07D209/62 , C07D209/96 , C07D213/73 , C07D213/74 , C07D233/46 , C07D233/66 , C07D233/88 , C07D233/90 , C07D235/30 , C07D249/14 , C07D261/14 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/10 , C07D403/12 , C07D405/06 , C07D409/04 , C07D409/06 , C07D409/10 , C07D413/06 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/10 , C07D471/04 , C07D487/04 , C07D491/10 , C07D498/04 , C07D521/00 , A61P7/00
摘要： The present invention relates to a 2-iminopyrrolidine derivative selected from the group consisting of 1-(3-tert-butyl-4-methoxy-5-morpholino-phenyl)-2-(5,6-diethoxy-7-fluoro-1-imino-1,3-dihydro-isoindol-2-yl)-ethanone; 1-{3-tert-butyl-5-[4-(2-hydroxy-acetyl)piperazin-1-yl]-4-methoxyphenyl}-2-(5,6-diethoxy-7-fluoro-1-imino-1,3-diyhdro-isoindol-2-yl)-ethanone; ethyl (4-{3-tert-butyl-5-[2-(5,6-diethoxy-7-fluoro-1-imino-1,3-dihydro-isoindol-2-yl)-acetyl]-2-methoxy-phenyl}piperazin-1-yl)-acetate; 1-(3-tert-butyl-4-methoxy-5-piperazin-1-yl-phenyl)-2-(5,6-diethoxy-7-fluoro-1-imino-1,3-dihydro-isoindol-2-yl)-ethanone, and (4-{3-tert-butyl-5-[2-(5,6-diethoxy-7-fluoro-1-imino-1,3-dihydro-isoindol-2-yl)-acetyl]-2-methoxy-phenyl}-piperazin-1-yl)-acetic acid; and salts thereof.

25. 发明专利

CA2440842A1 NOVEL 1H-INDAZOLE COMPOUNDS 未知
公开(公告)号：CA2440842A1
公开(公告)日：2002-10-24
申请号：CA2440842
申请日：2002-04-15
申请人： EISAI CO LTD
发明人： SOEJIMA MOTOHIRO , SATO NOBUAKI , TERAUCHI TARO , OHI NORIHITO , OINUMA HITOSHI , SESHIMO HIDENORI , DOKO TAKASHI , KOHMURA NAOHIRO
IPC分类号： A61P21/00 , A61P25/00 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/28 , A61P29/00 , A61P37/00 , A61P43/00 , C07D231/56 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D401/06 , C07D409/06 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D401/14 , C07D405/14 , C07D409/14 , A61K31/416 , A61K31/4178 , A61K31/427 , A61K31/428 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/496 , A61K31/50 , A61K31/517 , A61K31/5377 , A61K31/541
摘要： A novel 1H-indazole compound having excellent JNK inhibitory activity. It is a compound represented by the following general formula (I), a salt thereof, o r a hydrate of either: (I) wherein R1 means C6-14 aromatic cyclic hydrocarbon group; R2, R4, and R5 each independently means hydrogen, halogeno, cyano, etc.; L means a single bond, C1-6 alkylene, etc.; X means a single bond, a group represented by -CO-NH- or -NH-CO-, etc.; and Y means C3-8 cycloalkyl, a C6-14 aromatic cyclic hydrocarbon group, a 5- to 14-membered aromatic heterocyclic group, etc.

26. 发明专利

HK1013986A1 CARBAPENEM DERIVATIVE 未知
公开(公告)号：HK1013986A1
公开(公告)日：1999-09-17
申请号：HK98115149
申请日：1998-12-23
申请人： EISAI CO LTD
发明人： SATO NOBUAKI , SASHO MANABU , KAMATA ATSUSHI , SUZUKI TAKAAKI , SUGIYAMA ISAO , KATSU KANEMASA , SUZUKI TAKESHI
IPC分类号： C07D477/00 , A61K31/397 , A61K31/40 , A61K31/445 , A61P31/04 , C07D477/20 , C07D , A61K
摘要： Compounds having potent antimicrobial effects over Gram-positive bacteria and Gram-negative bacteria, high stability to beta -lactamases and DHP-I and high safety for the human body and a process for producing the same. Carbapenem compounds represented by the following general formula (I) or salts thereof: wherein the ring A represents a 3- to 7-membered ring containing at least one nitrogen atom and optionally having a substituent other than R ; R represents hydrogen or methyl; R and R are the same or different and each represents hydrogen or a protecting group of the hydroxyl group; R represents hydrogen or a protecting group of the carboxyl group; R represents hydrogen, lower alkyl or a protecting group of the amino group; R represents: (1) hydrogen, (2) lower alkyl optionally substituted by optionally protected hydroxy, carbamoyl, formimidoyl, acetimidoyl or wherein R and R are the same or different and each represents hydrogen, lower alkyl, or a protecting group of the amino group), or (3) a protecting group of the amino group or a protecting group of the imino group; and m is 0 or 1. These compounds have antimicrobial effects and are useful as a drug.

27. 发明专利

CA2379650C PROCESS FOR PRODUCING A BASIC ANTIBIOTIC INORGANIC ACID SALT, AND OXALATE INTERMEDIATE 未知
公开(公告)号：CA2379650C
公开(公告)日：2008-09-02
申请号：CA2379650
申请日：2000-07-27
申请人： EISAI CO LTD
发明人： SAKURAI SHIN , KOMATSU YUUKI , NEGI SHIGETO , ISHIZUKA HIROYUKI , SATO NOBUAKI , NAKAMURA TAIJU , KAYANO AKIO , SAITO HIROYUKI , CHIBA HIROYUKI , SASHO MANABU
IPC分类号： C07D477/20 , C07D463/02 , C07D463/22 , C07D477/02 , C07D477/08 , C07D499/04 , C07D499/21 , C07D499/68 , C07D501/02 , C07D501/22 , C07D501/34 , C07D501/36 , C07D501/38 , C07D501/46 , C07D519/06
摘要： The present invention provides: an industrially-excellent and novel process for producing a basic antibiotic inorganic acid salt, for example; an excellent production process for producing a hydrochloride thereof industrially, that is, a production process which comprises subjecting a basic antibiotic oxalate (II) to salt-exchange with an alkali earth metal salt (III) of an inorganic acid: (SEE ABOVE FORMULA) (wherein the ring A means the basic antibiotic; R10 means a protected functional group used in organic synthesis; Ak-E means the alkali earth metal; and B means the inorganic acid, respectively); a novel oxalate useful as a production intermediate for producing an antibiotic hydrochloride industrially, that is, an oxalate (II-I) of a carbapenem compound represented by the following formula: (SEE FORMULA II-I) (wherein the ring A represents a 3- to 7-membered ring having at least one nitrogen atom, and the ring A may be substituted with other than R6; R1 represents hydrogen or methyl group; R2 and R5 are the same as or different form each other and each represents hydrogen or a hydroxyl-protecting group; R3 representsacarboxyl -protecting group; R4 representshydrogen, a lower alkyl group or an amino-protecting group; R6 represents (1) hydrogen, (2) an optionally protected hydroxyl group, carbamoyl, formimidoyl, acetoimidoyl or a lower alkyl group which may be substituted with a substituent represented by the formula: (SEE ABOVE FORMULA) (wherein R7 and R8 are the same as or different from each other and each represents hydrogen, a lower alkyl group or an amino-protecting group) or (3) an amino-protecting group or an imino-protecting group; and m is 0 or 1); and a process for producing its. 39

28. 发明专利

CA2194399C NOVEL CARBAPENEM DERIVATIVE 未知
公开(公告)号：CA2194399C
公开(公告)日：2007-02-13
申请号：CA2194399
申请日：1995-06-29
申请人： EISAI CO LTD
发明人： SATO NOBUAKI , SASHO MANABU , KAMADA ATSUSHI , SUGIYAMA ISAO , SUZUKI TAKESHI , KATSU KANEMASA , SUZUKI TAKAAKI
IPC分类号： C07D477/00 , C07D477/20 , A61K31/395 , A61K31/397 , A61K31/40 , A61K31/43 , A61K31/445 , A61K31/695 , A61P31/04 , C07F7/10
摘要： Compounds having potent antimicrobial effects over Gram-positive bacteria and Gram-negative bacteria, high stability to .beta.-lactamases and DHP-I and high safety for the human body and a process for producing the same. Carbapenem compounds represented by the following general formula (I) or salts thereof: (see Formula I) wherein the ring A represents a 3- to 7-membered ring containing at least one nitrogen atom and optionally having a substituent other than R6; R1 represents hydrogen or methyl; R2 and R5 are the same or different and each represents hydrogen or a protecting group of the hydroxyl group; R3 represents hydrogen or a protecting group of the carboxyl group; R4 represents hydrogen, lower alkyl or a protecting group of the amino group; R6 represents: (1) hydrogen, (2) lower alkyl optionally substituted by optionally protected hydroxy, carbamoyl, formimidoyl, acetimidoyl or (see Formula II) wherein R7 and R8 are the same or different and each represents hydrogen, lower alkyl, or a protecting group of the amino group), or (3) a protecting group of the amino group or a protecting group of the imino group; and m is 0 or 1. These compounds have antimicrobial effects and are useful as a drug.

29. 发明专利

NO20020471L 未知
公开(公告)号：NO20020471L
公开(公告)日：2002-03-22
申请号：NO20020471
申请日：2002-01-29
申请人： EISAI CO LTD
发明人： KAYANO AKIO , CHIBA HIROYUKI , NAKAMURA TAIJU , SAKURAI SHIN , ISHIZUKA HIROYUKI , SAITO HIROYUKI , KOMATSU YUUKI , SASHO MANABU , SATO NOBUAKI , NEGI SHIGETO
IPC分类号： C07D477/02 , C07D477/08 , C07D477/20 , C07D499/68 , C07D501/22 , C07D501/36 , C07D501/46 , C07D
摘要： The present invention provides: an industrially-excellent and novel process for producing a basic antibiotic.inorganic acid salt, for example, an excellent production process for producing a hydrochloride thereof industrially, that is, a production process which comprises subjecting a basic antibiotic.oxalate (II) to salt-exchange with an alkali earth metal salt (III) of an inorganic acid: (wherein the ring A means the basic antibiotic; R means a protected functional group used in organic synthesis; Ak-E means the alkali earth metal; and B means the inorganic acid, respectively); a novel oxalate useful as a production intermediate for producing an antibiotic.hydrochloride industrially, that is, an oxalate (II-I) of a carbapenem compound represented by the following formula: (wherein the ring A represents a 3- to 7-membered ring having at least one nitrogen atom, and the ring A may be substituted with other than R ; R represents hydrogen or methyl group; R and R are the same as or different form each other and each represents hydrogen or a hydroxyl-protecting group; R represents a carboxyl-protecting group; R represents hydrogen, a lower alkyl group or an amino-protecting group; R represents (1) hydrogen, (2) an optionally protected hydroxyl group, carbamoyl, formimidoyl, acetoimidoyl or a lower alkyl group which may be substituted with a substituent represented by the formula: (wherein R and R are the same as or different from each other and each represents hydrogen, a lower alkyl group or an amino-protecting group) or (3) an amino-protecting group or an imino-protecting group; and m is 0 or 1); and a process for producing its.

30. 发明专利

NO20020471A 未知
公开(公告)号：NO20020471A
公开(公告)日：2002-03-22
申请号：NO20020471
申请日：2002-01-29
申请人： EISAI CO LTD
发明人： KAYANO AKIO , CHIBA HIROYUKI , NAKAMURA TAIJU , SAKURAI SHIN , ISHIZUKA HIROYUKI , SAITO HIROYUKI , KOMATSU YUUKI , SASHO MANABU , SATO NOBUAKI , NEGI SHIGETO
IPC分类号： C07D477/02 , C07D477/08 , C07D477/20 , C07D499/68 , C07D501/22 , C07D501/36 , C07D501/46 , C07D
CPC分类号： C07D477/20 , C07D477/02 , C07D477/08 , Y02P20/55

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