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公开(公告)号：EP1391456A4
公开(公告)日：2006-02-01
申请号：EP02718622
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
IPC分类号： C07D233/88 , A61K20060101 , A61K31/403 , A61K31/4035 , A61K31/4168 , A61K31/4178 , A61K31/4184 , A61K31/4196 , A61K31/422 , A61K31/437 , A61K31/4439 , 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 , C07D233/90 , 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
CPC分类号： C07D209/44
摘要： A 2-iminoimidazole derivative represented by the formula (I) or a salt thereof: (I) wherein R1, R2, and R3 each represents hydrogen, optionally substituted C1-6 alkyl, etc.; R6 represents hydrogen, C1-6 alkyl, C1-6 alkyloxycarbonyl, etc.; Y1 represents a single bond, -CH2-, etc.; Y2 represents a single bond, -CO-, etc.; and Ar represents hydrogen, a group represented by the formula (II): (II) (wherein R10 to R14 each represents hydrogen, C1-6 alkyl, hydroxy, C1-6 alkoxy, etc., provided that R12 may be bonded to R11 or R13 to form a 5- to 8-membered heterocycle), etc.
摘要翻译： 由式（I）表示的2-亚氨基咪唑衍生物或其盐：（I）其中R1，R2和R3各自代表氢，任选取代的C1-6烷基等; R6代表氢，C1-6烷基，C1-6烷氧基羰基等; Y1表示单键，-CH2-等; Y2表示单键，-CO-等; （II）表示的基团：其中R 10至R 14各自表示氢，C 1-6烷基，羟基，C 1-6烷氧基等，条件是R 12可以与R 11键合 或R13形成5至8元杂环）等。
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公开(公告)号：EP1386912A4
公开(公告)日：2006-02-01
申请号：EP02720534
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
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 , C07D207/273 , A61K31/40 , A61K31/4015 , A61K31/4025 , A61K31/407
CPC分类号： C07D209/44
摘要： A cyclic amidine derivative represented by the formula (I) or a salt thereof: (I) wherein R?1, R2, and R3¿ each represents hydrogen, C¿1-6? alkyl, C1-6 alkyl substituted by aryl, etc.; R?4, R5, and R7¿ each represents hydrogen, C¿1-6? alkyl, etc.; z is 0 or 1; R?6¿ represents hydrogen, C¿1-6? alkyl, (C1-6 alkyl)oxycarbonyl, etc.; n is 1 or 2; Y?1¿ represents a single bond, -CH¿2?-, etc.; Y?2¿ represents a single bond, -CO-, etc.; and Ar represents hydrogen, a group represented by the formula (II): (II) (wherein R?10 to R14¿ each represents hydrogen, C¿1-6? alkyl, hydroxy, C1-6 alkoxy, etc., provided that R?12¿ may be bonded to R?11 or R13¿ to form a 5- to 8-membered heterocycle), etc.
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公开(公告)号：EP1300464A4
公开(公告)日：2006-02-01
申请号：EP01947898
申请日：2001-07-06
申请人： EISAI CO LTD
发明人： TSUKAHARA KAPPEI , HATA KATSURA , SAGANE KOJI , NAKAMOTO KAZUTAKA , TSUCHIYA MAMIKO , WATANABE NAOAKI , OBA FUMINORI , TSUKADA ITARU , UEDA NORIHIRO , TANAKA KEIGO , KAI JUNKO
IPC分类号： A61K31/00 , A61K31/4355 , A61K31/4365 , A61K31/437 , A61K31/44 , A61K31/472 , A61K31/4725 , A61K31/5377 , A61K38/00 , A61P31/10 , C07D213/68 , C07D217/18 , C07D217/20 , C07D491/048 , C07D491/056 , C07K14/37 , C07K14/38 , C07K14/39 , C07K14/395 , C07K14/40 , C12N15/09 , A61K39/395 , A61K45/00 , C07K16/14 , C12N15/31 , G01N33/15 , G01N33/50
CPC分类号： C07K14/40 , A61K31/00 , A61K31/4355 , A61K31/4365 , A61K31/437 , A61K31/44 , A61K31/472 , A61K31/4725 , A61K31/5377 , A61K38/00 , C07D213/68 , C07D217/18 , C07D217/20 , C07K14/37 , C07K14/38 , C07K14/39 , C07K14/395 , C07K2319/02 , G01N2500/00 , Y10S435/911
摘要： A reporter system reflecting the transport process of GPI anchor protein to cell wall is constructed and a compound inhibiting this process is found out. Further, a gene imparting tolerance to the above compound is identified and a method of screening a compound inhibiting the activity of the protein encoded by this gene is developed. Thus, it is clarified by the novel compound that antifungal agents depending on a novel mechanism, wherein the transport process of GPI anchor protein to cell wall is inhibited, are available.
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公开(公告)号：EP1391451A4
公开(公告)日：2006-02-01
申请号：EP02724628
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
IPC分类号： C07D209/44 , 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 , C07D209/52 , 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
CPC分类号： C07D209/44
摘要： 2-Iminopyrrolidine derivatives represented by the general formula (I) or salts thereof: (I) wherein B is a benzene or pyridine ring, or the like; R101 to R103 are each hydrogen, halogeno, C1-6 alkyl, or the like; R5 is hydrogen, C1-6 alkyl, C1-6 alkoxy C1-6 alkyl, or the like; R6 is hydrogen, C1-6 alkyl, C1-6 alkyloxycarbonyl, or the like; Y1 is a single bond, -CH2-, or the like; Y2 is a single bond, -CO-, or the like; and Ar is hydrogen, a group represented by the general formula (II): (II) (wherein R10 to R14 are each hydrogen, C1-6 alkyl, hydroxyl, C1-6 alkoxy, or the like, or R11 and R12 or R12 and R13 may be united to form a 5- to 8-membered heterocycle), or the like.
摘要翻译： 由下式表示的2-亚氨基咪唑衍生物：其中R 1，R 2和R 3代表氢，任选取代的C 1-6烷基等; R 6表示氢，C 1-6烷基，C 1-6烷氧基羰基等; Y 1表示单键，-CH 2 - 等; Y 2表示单键，-CO-等; 和Ar表示氢，由下式表示的基团：其中R 10 -R 14表示氢，C 1-6烷基，羟基，C 1-6烷氧基等，R 11和R 11 R 12或R 12和R 13可以键合在一起形成5-至8-元杂环或其盐。
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公开(公告)号：EP1394152A4
公开(公告)日：2005-02-02
申请号：EP02720536
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
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
CPC分类号： C07D209/44
摘要： 2-Iminoimidazole derivatives represented by the general formula (I) or salts thereof: (I) wherein C is a benzene ring, a pyridine ring, or the like; R1 is optionally substituted C1-6 alkyl or the like; R201 is hydrogen, halogeno, acyl, or the like; R6 is hydrogen, C1-6 alkyl, C1-6 alkyloxycarbonyl, or the like; Y1 is a single bond, -CH2-, or the like; Y2 is a single bond, -CO-, or the like; and Ar is hydrogen, a group represented by the general formula (II): (II) (wherein R10 to R14 are each hydrogen, C1-6 alkyl, hydroxyl, C1-6 alkoxy, or the like, or R11 and R12 or R12 and R13 may be united to form a 5- to 8-membered heterocycle), or the like.
摘要翻译： （I）表示的2-氨基咪唑衍生物或其盐：（I）其中C是苯环，吡啶环等; R1是任选取代的C1-6烷基等; R201是氢，卤代，酰基等; R6是氢，C1-6烷基，C1-6烷氧基羰基等; Y1是单键，-CH2-等; Y2是单键，-CO-等; （II）:(式中，R 10〜R 14分别为氢，C 1-6烷基，羟基，C 1-6烷氧基等，或R 11和R 12或R 12表示的基团， 和R13可以结合形成5至8元杂环）等。
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公开(公告)号：EP1057819A4
公开(公告)日：2003-02-05
申请号：EP99905213
申请日：1999-02-17
申请人： EISAI CO LTD
发明人： WATANABE NOBUHISA , KARIBE NORIO , MIYAZAKI KAZUKI , OZAKI FUMIHIRO , KAMADA ATSUSHI , MIYAZAWA SHUHEI , NAOE YOSHIMITSU , KANEKO TOSHIHIKO , TSUKADA ITARU , NAGAKURA TADASHI , ISHIHARA HIROKI , KODAMA KOHTAROU , ADACHI HIDEYUKI
IPC分类号： A61K31/50 , A61K31/501 , A61P15/00 , A61P15/10 , C07D237/28 , C07D237/34 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D409/14 , C07D411/14 , C07D417/04 , C07D417/14 , C07D451/06 , C07D471/08 , C07D491/04 , C07D491/08 , C07D491/10 , C07D491/107 , C07D491/113 , C07D498/08 , C07D521/00 , C07D451/02
CPC分类号： C07D231/12 , C07D233/56 , C07D237/28 , C07D237/34 , C07D249/08 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D409/14 , C07D411/14 , C07D417/04 , C07D417/14 , C07D451/06 , C07D471/08 , C07D491/04 , C07D491/08 , C07D491/10
摘要： Phthalazine derivatives represented by general formula (I) or pharmacologically acceptable salts thereof or hydrates of the same usable as remedies for erectile dysfunction, wherein R1 and R2 are the same or different and each represents halogeno, optionally halogenated alkyl or alkoxy, or cyano; X represents cyano, nitro, halogeno, optionally substituted hydroxyimino or optionally substituted heteroaryl; and Y represents heteroaryl, aryl, alkynyl, alkenyl, alkyl or cyclic amine.
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