公开(公告)号：EP0235752B1

公开(公告)日：1993-11-18

申请号：EP87102743.9

申请日：1987-02-26

申请人： Eisai Co., Ltd.

发明人： Oinuma, Hitoshi ,  Yamanaka, Motosuke ,  Miyake, Kazutoshi ,  Hoshiko, Tomonori ,  Minami, Norio ,  Shoji, Tadao ,  Daiku, Yoshiharu ,  Sawada, Kohei ,  Nomoto, Kenichi

IPC分类号： C07D211/28 ,  C07D207/09 ,  C07D401/06 ,  C07D401/12 ,  C07D409/06 ,  C07D409/12 ,  C07D405/06 ,  C07D405/12 ,  C07D417/06 ,  C07D417/12 ,  C07D471/04

CPC分类号： C07D401/04 ,  C07D211/28 ,  C07D401/06 ,  C07D401/14 ,  C07D405/04 ,  C07D409/04 ,  C07D417/04 ,  C07D471/04 ,  C07D473/10

公开(公告)号：EP0304888B1

公开(公告)日：1992-11-11

申请号：EP88113786.3

申请日：1988-08-24

申请人： Eisai Co., Ltd.

发明人： Oinuma, Hitoshi ,  Yamanaka, Motosuke ,  Miyake, Kazutoshi ,  Hoshiko, Tomonori ,  Minami, Norio ,  Shoji, Tadao ,  Daiku, Yoshiharu ,  Sawada, Kohei ,  Nomoto, Kenichi

IPC分类号： C07D211/54 ,  C07D401/06 ,  C07D213/38 ,  C07D211/32 ,  C07D211/14 ,  C07C311/08 ,  A61K31/44 ,  A61K31/445 ,  A61K31/18

CPC分类号： C07D401/06 ,  C07D211/14 ,  C07D211/32 ,  C07D211/54 ,  C07D213/38 ,  Y10S514/821

公开(公告)号：EP0235752A3

公开(公告)日：1990-07-25

申请号：EP87102743.9

申请日：1987-02-26

申请人： Eisai Co., Ltd.

发明人： Oinuma, Hitoshi ,  Yamanaka, Motosuke ,  Miyake, Kazutoshi ,  Hoshiko, Tomonori ,  Minami, Norio ,  Shoji, Tadao ,  Daiku, Yoshiharu ,  Sawada, Kohei ,  Nomoto, Kenichi

IPC分类号： C07D211/28 ,  C07D207/09 ,  C07D401/06 ,  C07D401/12 ,  C07D409/06 ,  C07D409/12 ,  C07D405/06 ,  C07D405/12 ,  C07D417/06 ,  C07D417/12 ,  C07D471/04

CPC分类号： C07D401/04 ,  C07D211/28 ,  C07D401/06 ,  C07D401/14 ,  C07D405/04 ,  C07D409/04 ,  C07D417/04 ,  C07D471/04 ,  C07D473/10

摘要： A new piperidine compound is pharmacologically effective for treatment of the arrythmia and is defined by the formula:
in which R 1 is a lower alkyl or a tolyl, R 2 is hydrogen, hydroxyl, a lower alkoxy or a lower alkyl, R 3 is hydrogen, a lower alkyl, a lower alkenyl, a cycloalkyl or a cycloalkylalkyl, X is -CO-, -CH 2 - or -CHOH-, g is an integer of 1 to 3, h is an integer of 1 to 3, Y is hydrogen, a lower alkyl, a lower alkenyl, cyano, -CH 2 COOR, R being hydrogen or a lower alkyl, a cycloalkyl, a cycloalkylalkyl,
1 being 1 or 2, -A-B, A being -(CH 2 )n-, n being an integer of 1 to 5,
a straight-chain alkylene group having 1 to 5 carbon atoms which is a divalent group derived from a straight-chain alkane having lower alkyl, phenyl or hydroxyl. group(s) bonded directly to one or more carbon atoms constituting said alkane by removing a hydrogen atom bonded to each of the carbon atoms placed at both ends thereof, a straight-chain alkylene group having 1 to 5 carbon atoms which is a divalent group derived from a straight-chain alkene having a double bond formed between carbon atoms adjacent to each other by removing a hydrogen atom bonded to each of the carbon atoms placed at both ends thereof,
k being an integer of 2 to 5, - (CH 2 )p-CO-, p being an integer of 1 to 4, B being cyano, - NR 4 R 5 , a heterocyclic ring or a condensed aromatic ring. A pharmaceutical composition containing said compounds as active ingredient, and the use of said compound in the preparation of a medicament for the treatment of arrhythmia are also disclosed.

公开(公告)号：EP0630894A1

公开(公告)日：1994-12-28

申请号：EP94109221.5

申请日：1994-06-15

申请人： Eisai Co., Ltd.

发明人： Daiku, Yoshiharu ,  Kishi, Naoya ,  Yoshida, Fusayo ,  Nomoto, Kenichi ,  Ogawa, Toshiaki ,  Takamura, Tadanobu ,  Nose, Koichi ,  Tomimatsu, Mikio ,  Mizuno, Masanori ,  Matsukura, Masayuki ,  Sato, Keizo ,  Yoneda, Naoki ,  Kaino, Makoto ,  Miyake, Kazutoshi ,  Negi, Shigeto ,  Souda, Shigeru

IPC分类号： C07D401/12 ,  A61K31/415 ,  A61K31/44 ,  C07D231/12 ,  C07D233/54 ,  C07D405/14 ,  C07D409/14 ,  C07D409/04 ,  C07D405/04 ,  C07D213/61 ,  C07D213/38

CPC分类号： C07D231/12 ,  C07D213/38 ,  C07D213/61 ,  C07D233/64 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/04 ,  C07D409/14

摘要： A novel propenoic acid derivative which exhibits adenosine A1 antagonism is defined by the general formula (I):

(wherein A represents an aromatic ring; R¹ represents aryl or the like; R², R³ and R⁴ each represent hydrogen, lower alkyl or the like; and R⁷ and R⁸ each represent lower alkyl or the like)
or a pharmacologically acceptable salt thereof.

摘要翻译： 表现出腺苷A1拮抗作用的新型丙烯酸衍生物由通式（I）定义：（其中A表示芳环; R 1表示芳基等; R 2，R 3， 和R 4各自表示氢，低级烷基等; R 7和R 8各自表示低级烷基等，或其药理学上可接受的盐。

公开(公告)号：EP0235752A2

公开(公告)日：1987-09-09

申请号：EP87102743.9

申请日：1987-02-26

申请人： Eisai Co., Ltd.

发明人： Oinuma, Hitoshi ,  Yamanaka, Motosuke ,  Miyake, Kazutoshi ,  Hoshiko, Tomonori ,  Minami, Norio ,  Shoji, Tadao ,  Daiku, Yoshiharu ,  Sawada, Kohei ,  Nomoto, Kenichi

IPC分类号： C07D211/28 ,  C07D207/09 ,  C07D401/06 ,  C07D401/12 ,  C07D409/06 ,  C07D409/12 ,  C07D405/06 ,  C07D405/12 ,  C07D417/06 ,  C07D417/12 ,  C07D471/04

CPC分类号： C07D401/04 ,  C07D211/28 ,  C07D401/06 ,  C07D401/14 ,  C07D405/04 ,  C07D409/04 ,  C07D417/04 ,  C07D471/04 ,  C07D473/10

摘要： A new piperidine compound is pharmacologically effective for treatment of the arrythmia and is defined by the formula:
in which R 1 is a lower alkyl or a tolyl, R 2 is hydrogen, hydroxyl, a lower alkoxy or a lower alkyl, R 3 is hydrogen, a lower alkyl, a lower alkenyl, a cycloalkyl or a cycloalkylalkyl, X is -CO-, -CH 2 - or -CHOH-, g is an integer of 1 to 3, h is an integer of 1 to 3, Y is hydrogen, a lower alkyl, a lower alkenyl, cyano, -CH 2 COOR, R being hydrogen or a lower alkyl, a cycloalkyl, a cycloalkylalkyl,
1 being 1 or 2, -A-B, A being -(CH 2 )n-, n being an integer of 1 to 5,

a straight-chain alkylene group having 1 to 5 carbon atoms which is a divalent group derived from a straight-chain alkane having lower alkyl, phenyl or hydroxyl. group(s) bonded directly to one or more carbon atoms constituting said alkane by removing a hydrogen atom bonded to each of the carbon atoms placed at both ends thereof,
a straight-chain alkylene group having 1 to 5 carbon atoms which is a divalent group derived from a straight-chain alkene having a double bond formed between carbon atoms adjacent to each other by removing a hydrogen atom bonded to each of the carbon atoms placed at both ends thereof,
k being an integer of 2 to 5, - (CH 2 )p-CO-, p being an integer of 1 to 4, B being cyano, - NR 4 R 5 , a heterocyclic ring or a condensed aromatic ring. A pharmaceutical composition containing said compounds as active ingredient, and the use of said compound in the preparation of a medicament for the treatment of arrhythmia are also disclosed.

公开(公告)号：EP0304888A1

公开(公告)日：1989-03-01

申请号：EP88113786.3

申请日：1988-08-24

申请人： Eisai Co., Ltd.

发明人： Oinuma, Hitoshi ,  Yamanaka, Motosuke ,  Miyake, Kazutoshi ,  Hoshiko, Tomonori ,  Minami, Norio ,  Shoji, Tadao ,  Daiku, Yoshiharu ,  Sawada, Kohei ,  Nomoto, Kenichi

IPC分类号： C07D211/54 ,  C07D401/06 ,  C07D213/38 ,  C07D211/32 ,  C07D211/14 ,  C07C311/08 ,  A61K31/44 ,  A61K31/445 ,  A61K31/18

CPC分类号： C07D401/06 ,  C07D211/14 ,  C07D211/32 ,  C07D211/54 ,  C07D213/38 ,  Y10S514/821

摘要： Piperidine compounds of general formula (XX) are provided which are useful as medicaments for the treatment or prophylaxis of arrhythmia.
in which R¹ is a lower alkyl and W is:
wherein X is -S-, -SO- or -SO₂-; R² is hydrogen or -(CH₂) n -Y; n is an integer of 1 to 5; Y is an aryl, pyridyl or a substituted pyridyl group; X′ is -CO- or -CH(OH)-; p is an integer of 1 to 4; R¹² is hydrogen or a lower alkyl group; Y′ is -(CH₂) m -A; m is 1 or 2; A is an aryl, a substituted aryl, pyridyl or a substituted pyridyl group; R¹² and Y may form a 5- or 6-membered ring or a 5- or 6-membered ring having one or more substituents; and R²² is hydrogen, a halogen, a lower alkyl, a lower alkoxy or hydroxy.

摘要翻译： 提供通式（XX）的哌啶化合物是用作药物用于治疗或心律失常的预防是有用的。 其中R <1>是一个低级烷基，而W是： worin X为-S-， -​​ SO-或-SO 2 - ; [R <2>是氢或 - （CH 2）N-Y; n为1〜5的整数; Y为芳基，吡啶基或取代的吡啶基; X min为-CO-或-CH（OH） - ; p为1〜4的整数; [R <1> <2>是氢或低级烷基; ÿmin是 - （CH 2）M-A; m是1或2; A是芳基，取代的芳基，吡啶基或取代的吡啶基; [R <1> <2>和Y可以形成5-或6-元环或具有一个或多个取代基的5-或6-元环; 且R为氢<2> <2>是卤素的一个，低级烷基，低级烷氧基或羟基。