专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明公开

EP1614680A3 Process for preparing 2-iminopyrrolidine derivatives 有权
标题翻译：一种用于2-亚氨基吡咯衍生物的制备过程
公开(公告)号：EP1614680A3
公开(公告)日：2006-02-01
申请号：EP05022069.8
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： C07D209/44
CPC分类号： C07D209/44
摘要： The present invention relates to a process for preparing a compound of the formula

which comprises reacting a compound represented by the formula:

with a compound represented by the formula:

wherein X 1 represents nitrogen or CR 1 , X 2 represents nitrogen or CR 2 , X 3 represents nitrogen or CR 3 , X 4 represents nitrogen or CR 4 ; R 1 and R 4 are the same or different and each represents hydrogen, halogeno, optionally substituted alkyl or optionally substituted alkoxy, R 2 and R 3 are the same or different and each represents hydrogen, halogeno, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkoxy, optionally substituted amino, optionally substituted carboxyl, optionally substituted aminocarbonyl, optionally substituted aminosulfonyl, optionally substituted sulfonylamino or optionally substituted alkanoylamino; R 5 represents hydrogen or optionally substituted alkyl; X represents chlorine or bromine; Ar represents (1) hydrogen, (2) a group represented by the formula:

wherein the meaning of R 10 , R 11 , R 12 , R 13 and R 14 is as defined in the specification. Moreover, the invention pertains to a process for preparing a compound of formula

which comprises reacting a compound of the formula

with a compound

wherein the substituent meanings are as defined above.

2. 发明公开

EP0381235A2 Pyrrolidine compound and pharmaceutical use 失效
标题翻译：吡咯烷 - 衍生物和药物Verwendung。
公开(公告)号：EP0381235A2
公开(公告)日：1990-08-08
申请号：EP90102102.2
申请日：1990-02-02
申请人： Eisai Co., Ltd.
发明人： Yamanaka, Motosuke , Hoshiko, Tomonori , Suda, Shinji , Yoneda, Naoki , Mori, Nobuyuki , Shino, Mitsumasa , Ishihara, Hiroki , Saito, Mamoru , Matsuoka, Toshiyuki
IPC分类号： C07D207/08 , C07D207/10 , C07D409/04 , C07D403/04 , C07D401/04 , C07D409/06 , A61K31/40
CPC分类号： C07D207/08 , C07D207/12 , C07D207/14 , C07D401/04 , C07D403/04 , C07D409/04 , C07D409/06
摘要： A pyrrolidine compound having the formula and a pharmacologically acceptable salt thereof is disclosed. It is useful in the pharmaceutical field.
in which X is hydrogen, a halogen, or a lower alkyl, Y is -(CH2)n-, n being zero, 1 or 2, -S(O)p-, p being zero, 1 or 2, -O-, or -NH- and R is phenyl, a substituent-having phenyl, naphtyl, a substituent-having naphthyl, a heteroaryl or a substituent-having heteroaryl.
摘要翻译：公开了具有下式的吡咯烷化合物及其药理学上可接受的盐。它在制药领域很有用。其中X为氢，卤素或低级烷基，Y为 - （CH 2）n - ，n为0,1或2，-S（O）p - ，p为0,1或2， -O-或-NH-，R是苯基，具有取代基的苯基，萘基，具有取代基的萘基，杂芳基或具有取代基的杂芳基。

3. 发明公开

EP1614680A2 Process for preparing 2-iminopyrrolidine derivatives 有权
标题翻译： Verfahren zur Herstellung von 2-Iminopyrrolidin-Derivaten
公开(公告)号：EP1614680A2
公开(公告)日：2006-01-11
申请号：EP05022069.8
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： C07D209/44
CPC分类号： C07D209/44
摘要： The present invention relates to a process for preparing a compound of the formula

which comprises reacting a compound represented by the formula:

with a compound represented by the formula:

wherein X 1 represents nitrogen or CR 1 , X 2 represents nitrogen or CR 2 , X 3 represents nitrogen or CR 3 , X 4 represents nitrogen or CR 4 ; R 1 and R 4 are the same or different and each represents hydrogen, halogeno, optionally substituted alkyl or optionally substituted alkoxy, R 2 and R 3 are the same or different and each represents hydrogen, halogeno, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkoxy, optionally substituted amino, optionally substituted carboxyl, optionally substituted aminocarbonyl, optionally substituted aminosulfonyl, optionally substituted sulfonylamino or optionally substituted alkanoylamino; R 5 represents hydrogen or optionally substituted alkyl; X represents chlorine or bromine; Ar represents (1) hydrogen, (2) a group represented by the formula:

wherein the meaning of R 10 , R 11 , R 12 , R 13 and R 14 is as defined in the specification. Moreover, the invention pertains to a process for preparing a compound of formula

which comprises reacting a compound of the formula

with a compound

wherein the substituent meanings are as defined above.
摘要翻译：本发明涉及一种制备下式化合物的方法，其包括使下式表示的化合物与下式表示的化合物反应：其中X 1表示硝基，X 2表示氮或 CR 2，X 3表示氮或CR 3，X 4表示氮或CR 4; R 1和R 4相同或不同，各自表示氢，卤代，任选取代的烷基或任选取代的烷氧基，R 2和R 3相同或不同，各自表示氢，卤代，任选取代的烷基，任选取代的烯基，任选取代的烷氧基，任选取代的氨基，任选取代的羧基，任选取代的氨基羰基，任选取代的氨基磺酰基，任选取代的磺酰基氨基或任选取代的烷酰基氨基; R 5表示氢或任选取代的烷基; X表示氯或溴; Ar表示（1）氢，（2）由下式表示的基团：其中R 10，R 11，R 12，R 13和R 14的含义如说明书中所定义。此外，本发明涉及制备式的化合物的方法，其包括使式的化合物与化合物的反应，其中取代基的定义如上所定义。

4. 发明授权

EP0598702B1 Biphenylmethane derivative, the use of it and pharmacological compositions containing same 失效
标题翻译：二苯甲烷衍生物，它们的制备方法和含有它们的药物组合物
公开(公告)号：EP0598702B1
公开(公告)日：1998-06-10
申请号：EP94101415.1
申请日：1990-09-27
申请人： Eisai Co., Ltd.
发明人： Miyake, Kazutoshi , Matsukura, Masayuki , Yoneda, Naoki , Hiroshima, Osamu , Mori, Nobuyuki , Ishihara, Hiroki , Musha, Takashi , Matsuoka, Toshiyuki , Hamano, Sachiyuki , Minami, Norio
IPC分类号： C07D403/10 , C07D235/08 , C07D235/28 , C07D235/26 , C07D471/04 , C07D487/04 , A61K31/415
CPC分类号： C07D403/10 , C07D235/08 , C07D235/26 , C07D235/28 , C07D471/04 , C07D487/04

5. 发明授权

EP0628557B1 Biphenylmethane derivatives, the use of them and pharmacological compositions containing same 失效
标题翻译： Biphenylmethanderivate，它们的用途和成分含有这些成分pharmacologische
公开(公告)号：EP0628557B1
公开(公告)日：1997-05-02
申请号：EP94109556.4
申请日：1990-09-27
申请人： Eisai Co., Ltd.
发明人： Miyake, Kazutoshi , Matsukura, Masayuki , Yoneda, Naoki , Hiroshima, Osamu , Mori, Nobuyuki , Ishihara, Hiroki , Musha, Takashi , Matsuoka, Toshiyuki , Hamano, Sachiyuki , Minami, Norio
IPC分类号： C07D471/04 , A61K31/44
CPC分类号： C07D403/10 , C07D235/08 , C07D235/26 , C07D235/28 , C07D471/04 , C07D487/04

6. 发明授权

EP0420237B1 Biphenylmethane derivative, the use of it and pharmacological compositions containing same 失效
标题翻译：二苯甲烷衍生物，它们的制备方法和含有它们的药物组合物
公开(公告)号：EP0420237B1
公开(公告)日：1996-03-06
申请号：EP90118565.2
申请日：1990-09-27
申请人： Eisai Co., Ltd.
发明人： Miyake, Kazutoshi , Matsukura, Masayuki , Yoneda, Naoki , Hiroshima, Osamu , Mori, Nobuyuki , Ishihara, Hiroki , Musha, Takashi , Matsuoka, Toshiyuki , Hamano, Sachiyuki , Minami, Norio
IPC分类号： C07D235/08 , A61K31/415 , C07D235/28 , C07D235/26 , C07D403/10 , C07D471/04 , C07D487/04
CPC分类号： C07D403/10 , C07D235/08 , C07D235/26 , C07D235/28 , C07D471/04 , C07D487/04

7. 发明公开

EP0628557A1 Biphenylmethane derivatives, the use of them and pharmacological compositions containing same 失效
标题翻译： Biphenylmethanderivate，ihre Anwendung und sie enthaltende pharmacologische Zusammensetzungen。
公开(公告)号：EP0628557A1
公开(公告)日：1994-12-14
申请号：EP94109556.4
申请日：1990-09-27
申请人： Eisai Co., Ltd.
发明人： Miyake, Kazutoshi , Matsukura, Masayuki , Yoneda, Naoki , Hiroshima, Osamu , Mori, Nobuyuki , Ishihara, Hiroki , Musha, Takashi , Matsuoka, Toshiyuki , Hamano, Sachiyuki , Minami, Norio
IPC分类号： C07D471/04 , A61K31/44
CPC分类号： C07D403/10 , C07D235/08 , C07D235/26 , C07D235/28 , C07D471/04 , C07D487/04
摘要： Disclosed are biphenylmethane derivatives having the formula:

wherein
R² and R³, which may be the same or different, are each a hydrogen atom, a halogen atom, a lower C₁₋₆ alkyl group a lower C₁₋₆ alkoxy group, a carbamoyl group or a cyano group;
R⁴ stands for hydrogen or a lower C₁₋₆ alkyl group;
R⁵ is 1H-tetrazol-5-yl, a carboxyl (-COOH) group or a carboxylic ester thereof;
R⁶ stands for hydrogen, a halogen atom, a hydroxy group or a lower C₁₋₆ alkoxy group, or a pharmacologically acceptable salt thereof,
wherein
compounds having the following formula and their pharmacologically acceptable salts are excluded:

wherein R⁵ is 1H-tetrazol-5-yl, a carboxyl (-COOH) group or a carboxylic ester thereof and n is an integer of 1 to 2;
or a pharmacologically acceptable salt thereof.
Further, a process for their preparation, pharmaceutical compositions containing same and their use for the preparation of such compositions for preventing and treating hypertension and/or cardiac failure are disclosed.
摘要翻译：公开了具有下式的联苯甲烷衍生物：其中R 2和R 3可以相同或不同，各自为氢原子，卤素原子，低级C 1-6烷基，低级C1 -6烷氧基，氨基甲酰基或氰基; R 4代表氢或低级C 1-6烷基; R 5是1H-四唑-5-基，羧基（-COOH）基或其羧酸酯; R 6代表氢，卤素原子，羟基或低级C 1-6烷氧基，或其药理学上可接受的盐，其中排除具有下式的化合物及其药理学上可接受的盐：其中R 5是1H-四唑-5-基，羧基（-COOH）基或其羧酸酯，n是1〜2的整数。或其药理学上可接受的盐。此外，公开了其制备方法，含有该组合物的药物组合物及其制备用于预防和治疗高血压和/或心力衰竭的组合物的用途。

8. 发明公开

EP0598702A1 Biphenylmethane derivative, the use of it and pharmacological compositions containing same 失效
标题翻译：二苯甲烷衍生物，它们的制备方法和含有药物组合物。
公开(公告)号：EP0598702A1
公开(公告)日：1994-05-25
申请号：EP94101415.1
申请日：1990-09-27
申请人： Eisai Co., Ltd.
发明人： Miyake, Kazutoshi , Matsukura, Masayuki , Yoneda, Naoki , Hiroshima, Osamu , Mori, Nobuyuki , Ishihara, Hiroki , Musha, Takashi , Matsuoka, Toshiyuki , Hamano, Sachiyuki , Minami, Norio
IPC分类号： C07D403/10 , C07D235/08 , C07D235/28 , C07D235/26 , C07D471/04 , C07D487/04 , A61K31/415
CPC分类号： C07D403/10 , C07D235/08 , C07D235/26 , C07D235/28 , C07D471/04 , C07D487/04
摘要： Disclosed are biphenylmethane derivatives having the formula (I):

wherein R 1 is hydrogen, alkyl, cycloalkyl, halogenated alkyl, -S-R7, -S0 2 -R7, -C=C-R 7 or -(CH 2 )p-OR7, R7 being hydrogen, alkyl, cycloalkyl or halogenated alkyl, p being zero or 1, -A1 =A2-A3 = A4- is -CH = CH-CH = CH- , -N = CH-CH = CH-, -CH = N-CH = CH-, -CH = C H - N = CH-, -CH = C H -C H = N- or -CH = N -C H = N-, R 2 and R 3 are each hydrogen, halogen, lower alkyl, lower alkoxy, carbamoyl or cyano, R 4 is hydrogen or lower alkyl, R 5 is 1 H-tetrazol-5-yl, carboxyl (-COOH) or a carboxylic ester group and R 6 is hydrogen, halogen, hydroxyl or lower alkoxy, or a pharmacologically acceptable salt thereof,
whereby compounds having the following formula and their pharmacologically acceptable salts are excluded:

wherein R 2 through R 6 are essentially as defined above. Further, a process for their preparation, pharmaceutical compositions containing same and their use for the preparation of such compositions for preventing and treating hypertension and/or cardiac failure are disclosed.
摘要翻译：本发明公开了具有式（I）联苯甲烷衍生物： worin - [R <1>是氢，烷基，环烷基，卤代烷基，-S-R 7 -SO 2 R 7，-C IDENTICAL C-R7或 - （CH 2） p-OR 7，R 7是氢，烷基，环烷基或卤代烷基，p是0或1，-A1 = A2-A3 = A4-是-CH = CH-CH = CH-，-N = CH-CH = CH- ，-CH = N-CH = CH-，-CH = CH-N = CH-，-CH = CH-CH = N-或-CH = N-CH = N-，R <2>和R <3> 各自为氢，卤素，低级烷基，低级烷氧基，氨基甲酰基或氰基，R <4>是氢或低级烷基，R <5>是1H-四唑-5-基，羧基（-COOH）或羧酸酯基和 [R <6>是氢，卤素，羟基或低级烷氧基，或其药理学上可接受的盐，从而被排除具有下式及其药理学上可接受的盐的化合物： worinř<2>至R <6>基本上如上所定义。此外，其制备方法，药物组合物含有相同，他们为寻求预防和治疗高血压和/或心脏衰竭的组合物的制备中的游离缺失盘。

9. 发明授权

EP0381235B1 Pyrrolidine compound and pharmaceutical use 失效
标题翻译：吡咯啉化合物和药物使用
公开(公告)号：EP0381235B1
公开(公告)日：1993-07-28
申请号：EP90102102.2
申请日：1990-02-02
申请人： Eisai Co., Ltd.
发明人： Yamanaka, Motosuke , Hoshiko, Tomonori , Suda, Shinji , Yoneda, Naoki , Mori, Nobuyuki , Shino, Mitsumasa , Ishihara, Hiroki , Saito, Mamoru , Matsuoka, Toshiyuki
IPC分类号： C07D207/08 , C07D207/10 , C07D409/04 , C07D403/04 , C07D401/04 , C07D409/06 , A61K31/40
CPC分类号： C07D207/08 , C07D207/12 , C07D207/14 , C07D401/04 , C07D403/04 , C07D409/04 , C07D409/06

10. 发明公开

EP0420237A1 Biphenylmethane derivative, the use of it and pharmacological compositions containing same 失效
标题翻译：二苯甲烷衍生物，它们的制备方法和含有药物组合物。
公开(公告)号：EP0420237A1
公开(公告)日：1991-04-03
申请号：EP90118565.2
申请日：1990-09-27
申请人： Eisai Co., Ltd.
发明人： Miyake, Kazutoshi , Matsukura, Masayuki , Yoneda, Naoki , Hiroshima, Osamu , Mori, Nobuyuki , Ishihara, Hiroki , Musha, Takashi , Matsuoka, Toshiyuki , Hamano, Sachiyuki , Minami, Norio
IPC分类号： C07D235/08 , A61K31/415 , C07D235/28 , C07D235/26 , C07D403/10 , C07D471/04 , C07D487/04
CPC分类号： C07D403/10 , C07D235/08 , C07D235/26 , C07D235/28 , C07D471/04 , C07D487/04
摘要： The biphenylmethane derivative having the formula (I) is disclosed
摘要翻译：具有式（I）的联苯甲烷衍生物游离缺失盘其中R 1是氢，烷基，环烷基，卤代烷基，-S-R 7，-SO 2 R 7，-C IDENTICAL C-R7或 - （CH 2 ）对 - OR 7，R 7是氢，烷基，环烷基或卤代烷基，p是0或1，-A1 = A2-A3 = A4-是-CH = CH-CH = CH-，-N = CH- CH = CH-，-CH = N-CH = CH-，-CH = CH-N = CH-，-CH = CH-CH = N-或-CH = N-CH = N-，R 2和R 3各自是氢，卤素，低级烷基，低级烷氧基，氨基甲酰基或氰基，R 4是氢或低级烷基，R 5是1H-四唑-5-基，羧基（-COOH）或羧酸酯和R6是氢，卤素，羟基或低级烷氧基，或其药理学上可接受的盐。此外，含有相同的，并且寻求用于预防和治疗高血压和/或心脏衰竭的组合物的制备中的用途的联苯甲烷衍生物的药物组合物是游离缺失光盘。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式