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1. 发明专利

IL158491A 2-IMINOPYRROLIDINE DERIVATIVES 未知
公开(公告)号：IL158491A
公开(公告)日：2010-12-30
申请号：IL15849103
申请日：2003-10-19
申请人： 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 , EISAI R&D MAN CO LTD , 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.

2. 发明专利

CA2000985C 1,4-DIAZEPINE DERIVATIVE AND ITS PHARMACEUTICAL USE 未知
公开(公告)号：CA2000985C
公开(公告)日：2000-01-18
申请号：CA2000985
申请日：1989-10-18
申请人： OKANO KAZUO , MIYAZAWA SHUHEI , CLARK RICHARD STEPHEN JOHN , SHIMOMURA NAOYUKI , KATAYAMA SATOSHI , SAKUMA YOSHINORI , MURAMOTO KENZO , MIYAMOTO MITSUAKI , ASANO OSAMU , YOSHIMURA HIROYUKI , YAMADA KOUJI , SOUDA SHIGERU , MACHIDA YOSHIMASA , KATAYAMA KOUICHI , YAMATSU ISAO , ABE SHINYA , KAWAHARA TETSUYA , OBAISHI HIROSHI , HARADA KOUKICHI , TSUNODA HAJIME
发明人： OKANO KAZUO , MIYAZAWA SHUHEI , CLARK RICHARD STEPHEN JOHN , SHIMOMURA NAOYUKI , KATAYAMA SATOSHI , SAKUMA YOSHINORI , MURAMOTO KENZO , MIYAMOTO MITSUAKI , ASANO OSAMU , YOSHIMURA HIROYUKI , YAMADA KOUJI , SOUDA SHIGERU , MACHIDA YOSHIMASA , KATAYAMA KOUICHI , YAMATSU ISAO , ABE SHINYA , KAWAHARA TETSUYA , OBAISHI HIROSHI , HARADA KOUKICHI , TSUNODA HAJIME
IPC分类号： C07D495/04 , A61K31/55 , A61K31/675 , A61P11/00 , A61P11/08 , A61P37/08 , C07D495/14 , C07D495/22 , C07F9/6561
摘要： Triazolo-1,4-di-azepine compounds of the formula: (see formula I) and pharmacologically acceptable salts thereof, wherein R1 and R2 are hydrogen or alkyl, R3 is hydrogen or halogen, R4 is hydrogen or alkyl, X is -OCO-, -NHCO-, -CO- or others and Y is cycloalkyl, cycloalkylalkyl, alkynyl or others, are useful in the pharmaceutical field, especially pertaining to allergic diseases.

3. 发明专利

DE60231608D1 未知
公开(公告)号：DE60231608D1
公开(公告)日：2009-04-30
申请号：DE60231608
申请日：2002-04-19
申请人： EISAI R&D MAN 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 , KURAMOCHI HIROKO , CHIBA KEN-ICHI , KIMURA AKIFUMI , ONO NAOTO
IPC分类号： C07D207/273 , A61K20060101 , A61K31/40 , A61K31/4015 , A61K31/4025 , A61K31/403 , A61K31/4035 , A61K31/407 , 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.

4. 发明专利

AT425964T 未知
公开(公告)号：AT425964T
公开(公告)日：2009-04-15
申请号：AT02720534
申请日：2002-04-19
申请人： EISAI R&D MAN 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 , KURAMOCHI HIROKO , CHIBA KEN-ICHI , KIMURA AKIFUMI , ONO NAOTO
IPC分类号： C07D207/273 , A61K20060101 , A61K31/40 , A61K31/4015 , A61K31/4025 , A61K31/403 , A61K31/4035 , A61K31/407 , 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.

5. 发明专利

ES2310202T3 COMPUESTO CICLICO CONDENSADO QUE CONTIENE NITROGENO QUE TIENE UN GRUPO PIRAZOLILO COMO GRUPO SUSTITUYENTE Y COMPOSICION FARMACEUTICA DEL MISMO. 未知
公开(公告)号：ES2310202T3
公开(公告)日：2009-01-01
申请号：ES02722791
申请日：2002-04-25
申请人： EISAI R&D MAN CO LTD
发明人： YOSHIDA ICHIRO , YONEDA NAOKI , OHASHI YOSHIAKI , SUZUKI SHUICHI , MIYAMOTO MITSUAKI , MIYAZAKI FUTOSHI
IPC分类号： C07D401/04 , A61K31/4155 , A61K31/4184 , A61K31/423 , A61K31/437 , A61K31/4439 , A61K31/4725 , A61K31/496 , A61K31/517 , A61K31/5377 , A61K31/5415 , A61K31/551 , A61P1/04 , A61P3/04 , A61P11/00 , A61P17/00 , A61P29/00 , A61P31/04 , A61P31/12 , A61P31/18 , A61P33/00 , A61P35/00 , A61P35/02 , A61P37/02 , A61P37/08 , A61P43/00 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07D471/04 , C07D493/04 , C07F5/02
摘要： Un compuesto representado por la siguiente fórmula (I), o una sal del mismo o un hidrato del mismo: (Ver fórmula) en el que X es un grupo cíclico de imidazo[1,2-a]piridina y tiene (R 4 )n como grupos sustituyentes en los que n es 0, 1, 2 ó 3, y los grupos sustituyentes (R 4 )n representan independientemente un átomo de hidrógeno, átomo de halógeno, grupo ciano, grupo hidroxilo, grupo amino, grupo alquilo C1 - 6, grupo alquilo C1 - 6 halogenado, grupo alquenilo C2 - 6, grupo alquilsulfonilo C1 - 6, grupo alquilsulfonilamino C1 - 6, grupo alquilsulfinilo C1 - 6, grupo N-(alquil C1 - 6)amino, grupo N,N-di(alquil C1 - 6)amino, grupo alcoxilo C1 - 6, grupo alquilsulfanilo C1 - 6, grupo carbamoílo, grupo N-(alquil C1 - 6)carbamoílo, grupo N,N-di(alquil C1 - 6)carbamoílo, grupo sulfamoílo, grupo fenilo, grupo heteroarilo, grupo fenoxilo, grupo heteroariloxilo, grupo fenil-alquilamino C1 - 6 o grupo heteroaril-alquilamino C1 - 6, que está unido a un átomo que constituye X; Y es un grupo fenilo, grupo piridilo, grupo tienilo, grupo tiazolilo, grupo pirazolilo, grupo 1,2,4-tiadiazolilo, grupo 1,2,4-oxadiazolilo, grupo 1,3,4-tiadiazolilo, grupo 1,3,4-oxadiazolilo o grupo benzotiazolilo; (Z)n son n grupos (Z) unidos a Y, en los que n es 0, 1, 2 ó 3, los grupos Z están unidos a un átomo que constituye el grupo cíclico Y y representan independientemente un grupo seleccionado de (1) átomo de hidrógeno, (2) grupo amino, (3) átomo de halógeno, (4) grupo hidroxilo, (5) grupo nitro, (6) grupo ciano, (7) grupo azido, (8) grupo formilo, (9) grupo hidroxiamino, (10) grupo sulfamoílo, (11) grupo guanodino, (12) grupo oxo, (13) grupo alquenilo C2 - 6, (14) grupo alcoxilo C1 - 6, (15) grupo alquilhidroxiamino C1 - 6, (16) grupo alquilo C1 - 6 halogenado, (17) grupo alquenilo C2 - 6 halogenado, (18) fórmula -M 1 -M 2 -M 3 , en la que: M 1 y M 2 representan cada uno un enlace sencillo, -(CH2)m-, -CHR 5 CHR 6 -, -(CH2)m-CR 5 R 6 -(CH2)n-, -CR 5 =CR 6 -, -C C-, -CR 5 =CR 6 -CO-, -(CH2)m-O-(CH2)n-, -O-(CH2)n-CR 5 R 6 -, -(CH2)m-S-(CH2)n-, -SO(CH2)m-, -SO2(CH2)m-, -CO (CH2)m-, -COO-, -CONR 7 -, -CONR 7 CHR 8 -, -CONR 7 -CR 5 R 6 -, -CONR 7 -(CH2)m-, -NR 7 -, -NR 7 CO-CR 5 R 6 -, -NR 7 CO-CR 5 R 6 -CO-, -NR 7 CO-(CH2)m-, -NR 7 SO2(CH2)m-, -SO2NR 7 -(CH2)m-, -SO2NR 7 -CR 5 R 6 -, -NR 7 CONR 8 - o -NR 7 CSNR 8 -, donde n y m son independientemente 0, 1, 2 ó 3, o (19) un grupo seleccionado de (a) grupo cíclico hidrocarbonado aromático C6 - 14, (b) grupo cicloalquilo C3 - 14, (c) grupo cicloalquenilo C4 - 14, (d) grupo heterocíclico aromático de 5 a 14 miembros o (e) grupo heterocíclico no aromático de 4 a 14 miembros, cada uno de los cuales puede estar sustituido con 4 o menos grupos seleccionados del grupo sustituyente Q, M 3 representa (i) átomo de hidrógeno, (ii) grupo oxo, (iii) átomo de halógeno, (iv) grupo hidroxilo, (v) grupo amino, (vi) grupo ciano, (vii) grupo nitro, (viii) grupo azido, (viv) grupo ciano, (x) grupo carboxilo, (xi) grupo alquilo C1 - 6, (xii) grupo alquilo C1 - 6 halogenado, (xiii) grupo alquilo C1 - 6 sustituido con un grupo hidroxilo o ciano, (xiv) grupo alquenilo C2 - 6, (xv) grupo alquinilo C2 - 6, (xvi) grupo alquenilo C2 - 6 halogenado, (xvii) grupo alcoxilo C1 - 6 halogenado, (xviii) -OR 7 , (xviv) -NR 7 R 8 , (xx) -NR 7 COR 8 , (xxi) -COR 7 , (xxii) -CONR 7 R 8 , (xxiii) -SOR 7 , (xxiv) -SO2R 7 , (xxv) -NR 7 SO2R 8 , (xxvi) -SO2NR 7 R 8 , (xxvii) grupo metilendioxilo, (xxviii) grupo etilendioxilo o (xxviv) (a) grupo cicloalquilo C3 - 8, (b) grupo cicloalquenilo C4 - 8, (c) grupo heterocíclico no aromático de 5 a 14 miembros, (d) grupo cíclico hidrocarbonado aromático C6 - 14, (e) grupo heterocíclico aromático de 5 a 14 miembros, (f) grupo fenoxilo, (g) grupo heteroaliloxilo o (h) grupo cicloalquiloxilo C3 - 8, que pueden estar sustituidos con 4 o menos grupos seleccionados del grupo sustituyente Q; el grupo sustituyente Q representa un grupo oxo, átomo de halógeno, grupo hidroxilo, grupo amino, grupo ciano, grupo nitro, grupo azido, grupo ciano, grupo carboxilo, grupo alquilo C1 - 6, grupo alquilo C1 - 6 halogenado, grupo alquilo C1 - 6 sustituido con un grupo ciano o hidroxilo, grupo alquenilo C2 - 6, grupo alquinilo C2 - 6, grupo alquenilo C2 - 6 halogenado, grupo alcoxilo C1 - 6 halogenado, -OR 7 , -OCH2CONR 7 R 8 , -NR 7 R 8 , -NR 7 COR 8 , -COR 7 , -CONR 7 R 8 , -SOR 7 , -SO2R 7 , -NR 7 SO2R 8 , -SO2NR 7 R 8 , grupo metilendioxilo o grupo etilendioxilo; R 1 representa...

6. 发明专利

DE60227794D1 未知
公开(公告)号：DE60227794D1
公开(公告)日：2008-09-04
申请号：DE60227794
申请日：2002-04-25
申请人： EISAI R&D MAN CO LTD
发明人： YOSHIDA ICHIRO , YONEDA NAOKI , OHASHI YOSHIAKI , SUZUKI SHUICHI , MIYAMOTO MITSUAKI , MIYAZAKI FUTOSHI , SESHIMO HIDENORI , KAMATA JUNICHI , TAKASE YASUTAKA , SHIRATO MANABU , SHIMOKUBO DAIYA , SAKUMA YOSHINORI , YOKOHAMA HIROMITSU
IPC分类号： C07D401/04 , A61K31/4155 , A61K31/4184 , A61K31/423 , A61K31/437 , A61K31/4439 , A61K31/4725 , A61K31/496 , A61K31/517 , A61K31/5377 , A61K31/5415 , A61K31/551 , A61P1/04 , A61P3/04 , A61P11/00 , A61P17/00 , A61P29/00 , A61P31/04 , A61P31/12 , A61P31/18 , A61P33/00 , A61P35/00 , A61P35/02 , A61P37/02 , A61P37/08 , A61P43/00 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07D471/04 , C07D493/04 , C07F5/02
摘要： The present invention provides a compound having an excellent inhibitory action on activation of STAT6 and a pharmaceutical composition thereof. In particular, it provides a compound represented by the following formula (I), a salt thereof or a hydrate of them. In the formula, the groups X,Y,Z,R 1 -R 4 and n are defined as in claim 1.

7. 发明专利

DE60233043D1 未知
公开(公告)号：DE60233043D1
公开(公告)日：2009-09-03
申请号：DE60233043
申请日：2002-04-19
申请人： EISAI R&D MAN 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 TAKAHASHI , KOGUSHI MOTOJI , KAWATA TSUTOMU , MATSUOKA TOSHIYUKI , KOBAYASHI HIROKO , CHIBA , KIMURA AKIFUMI , ONO NAOTO
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
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.

8. 发明专利

AT402164T 未知
公开(公告)号：AT402164T
公开(公告)日：2008-08-15
申请号：AT02722791
申请日：2002-04-25
申请人： EISAI R&D MAN CO LTD
发明人： YOSHIDA ICHIRO , YONEDA NAOKI , OHASHI YOSHIAKI , SUZUKI SHUICHI , MIYAMOTO MITSUAKI , MIYAZAKI FUTOSHI , SESHIMO HIDENORI , KAMATA JUNICHI , TAKASE YASUTAKA , SHIRATO MANABU , SHIMOKUBO DAIYA , SAKUMA YOSHINORI , YOKOHAMA HIROMITSU
IPC分类号： C07D401/04 , A61K31/4155 , A61K31/4184 , A61K31/423 , A61K31/437 , A61K31/4439 , A61K31/4725 , A61K31/496 , A61K31/517 , A61K31/5377 , A61K31/5415 , A61K31/551 , A61P1/04 , A61P3/04 , A61P11/00 , A61P17/00 , A61P31/04 , A61P31/12 , A61P31/18 , A61P33/00 , A61P35/00 , A61P35/02 , A61P37/02 , A61P37/08 , A61P43/00 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07D471/04 , C07D493/04 , C07F5/02
摘要： The present invention provides a compound having an excellent inhibitory action on activation of STAT6 and a pharmaceutical composition thereof. In particular, it provides a compound represented by the following formula (I), a salt thereof or a hydrate of them. In the formula, the groups X,Y,Z,R 1 -R 4 and n are defined as in claim 1.

9. 发明专利

HK1086269A1 2-iminopyrrolidine derivatives 未知
公开(公告)号：HK1086269A1
公开(公告)日：2006-09-15
申请号：HK06106324
申请日：2006-06-01
申请人： EISAI R&D MAN CO LTD
发明人： SUZUKI SHUICHI , KOTAE 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 , MUSYA TAKASHI , KOGUSHI MOTOJI , KAWADA TSUTOMU , MATSUOKA TOSHIYUKI , KOBAYASHI HIROKO , CHIBA KEN-ICHI , KIMURA AKIFUMI , ONO NAOTO
IPC分类号： C07D20060101 , 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 , 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.

10. 发明专利

ES2462995T3 Derivados de 2-iminoisoindolinona como antagonistas del receptor de la trombina 未知
公开(公告)号：ES2462995T3
公开(公告)日：2014-05-27
申请号：ES11166172
申请日：2002-04-19
申请人： EISAI R&D MAN 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： 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
摘要： Un compuesto o una sal del mismo, en el que el compuesto se selecciona del grupo que consiste en 1- (3-terc-butil-4-metoxi-5-morfolino-fenil) -2- (5, 6-dietoxi-7-fluoro-1-imino-1, 3-dihidro-isoindol-2-il) -etanona, 1-{3-terc-butil-5-[4- (2-hidroxi-acetil) piperazin-1-il]-4-metoxi-fenil}-2- (5, 6-dietoxi-7-fluoro-1-imino-1, 3-dihidro-isoindol-2-il) -etanona, (4-{3-terc-butil-5-[2- (5, 6-dietoxi-7-fluoro-1-imino-1, 3-dihidro-isoindol-2-il) -acetil]-2-metoxi-fenil}piperazin-1-il) acetato de etilo, 1- (3-terc-butil-4-metoxi-5-piperazin-1-il-fenil) -2- (5, 6-dietoxi-7-fluoro-1-imino-1, 3-dihidroisoindol-2-il) -etanona, y ácido (4-{3-terc-butil-5-[2- (5, 6-dietoxi-7-fluoro-1-imino-1, 3-dihidro-isoindol-2-il) -acetil]-2-metoxifenil}-piperazin-1-il) -acético.

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