公开(公告)号：JP2001270883A

公开(公告)日：2001-10-02

申请号：JP2001009592

申请日：2001-01-18

申请人： EISAI CO LTD

发明人： OZAKI FUMIHIRO ,  KANEKO TOSHIHIKO ,  TABATA MUTSUKO ,  TAKAHASHI YOSHINORI ,  MIYAZAKI KAZUSHIRO ,  KAMATA JUNICHI ,  YOSHIDA ICHIRO ,  MATSUKURA MASAYUKI ,  SUZUKI HIROYUKI ,  YOSHINAGA TAKASHI ,  ISHIHARA HIROKI ,  KATO KOJI ,  SAWADA KOHEI ,  ONOKI TATSUHIRO ,  KOBAYASHI KIYOAKI ,  OKUBO MIYUKI

IPC分类号： C07D401/06 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5377 ,  A61P9/04 ,  A61P9/06 ,  A61P25/02 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14

摘要： PROBLEM TO BE SOLVED: To obtain a new compound having excellent Na+ channel inhibiting activity. SOLUTION: This compound is represented by general formula (I) [wherein ring A is a ring, or the like, of general formula (II) (wherein R1 is hydrogen atom, or the like; and R2 is hydrogen atom, or the like), or the like; W is optionally a substituted 1-6C alkylene group, or the like; Z is an optionally substituted 6-14C aromatic carbocyclic group, or the like; and (l) is an integer of 0 to 6] or a salt thereof, or a hydrate thereof.

公开(公告)号：JP2001270861A

公开(公告)日：2001-10-02

申请号：JP2001009591

申请日：2001-01-18

申请人： EISAI CO LTD

发明人： YAMAMOTO NOBORU ,  SUZUKI YUICHI ,  KIMURA MANAMI ,  NIITOME TETSUHIRO ,  IIMURA YOICHI ,  TERAMOTO TETSUYUKI ,  KANEDA YOSHIHISA ,  KANEKO TOSHIHIKO ,  KURUSU NOBUYUKI ,  SHINMYO DAISUKE ,  YOSHIKAWA YUKIE ,  HATAKEYAMA SHINJI

IPC分类号： C07D243/08 ,  A61K31/4025 ,  A61K31/403 ,  A61K31/404 ,  A61K31/438 ,  A61K31/4418 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/4439 ,  A61K31/445 ,  A61K31/4468 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/495 ,  A61K31/496 ,  A61K31/4995 ,  A61K31/551 ,  A61P3/00 ,  A61P9/00 ,  A61P9/10 ,  A61P25/00 ,  A61P25/06 ,  A61P25/08 ,  A61P25/16 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/26 ,  A61P25/28 ,  A61P43/00 ,  C07D207/09 ,  C07D207/337 ,  C07D209/14 ,  C07D209/42 ,  C07D211/22 ,  C07D211/32 ,  C07D211/34 ,  C07D211/46 ,  C07D211/58 ,  C07D213/22 ,  C07D213/36 ,  C07D213/57 ,  C07D215/04 ,  C07D215/12 ,  C07D235/14 ,  C07D235/30 ,  C07D241/04 ,  C07D263/32 ,  C07D263/38 ,  C07D271/06 ,  C07D277/28 ,  C07D277/82 ,  C07D295/14 ,  C07D295/18 ,  C07D307/54 ,  C07D307/81 ,  C07D319/20 ,  C07D333/24 ,  C07D333/60 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/04 ,  C07D405/06 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D471/10 ,  C07D487/08

摘要： PROBLEM TO BE SOLVED: To obtain a new compound having excellent calcium antagonism, in particular neuroselective calcium antagonism. SOLUTION: This new compound is represented by the formula [Ar is a (substituted) 5- to 14-membered aromatic cyclic group, or the like; ring A is either one ring selected from piperazine, homopiperazine and piperidine rings, and the like; ring B is a (substituted) 3-14C hydrocarbon ring, or the like; E is a single bond, a group of the formula CO, or the like; X is a single bond, oxygen atom, or the like; R1 is H, a halogen atom, OH, or the like; and D1, D2, W1 and W2 are each a single bond or a (substituted) 1-6C alkylene chain]. This new compound may assume a salt or hydrate form.

公开(公告)号：JP2588193B2

公开(公告)日：1997-03-05

申请号：JP10550887

申请日：1987-04-28

申请人： EISAI CO LTD

发明人： OGATA YOSHITAKE ,  IKEDA MAKOTO ,  NOMOTO SEIICHIRO ,  OKITA MAKOTO ,  SHIMOMURA NAOYUKI ,  KANEKO TOSHIHIKO ,  YAMANAKA TEIJI ,  HISHINUMA TAKAHARU ,  NAGAGAWA JUNICHI ,  HIROTA KAZUO ,  MYAMOTO KANAME ,  HORIE TOORU ,  WAKABAYASHI TSU

IPC分类号： C07D317/50 ,  A61K31/357 ,  A61K31/36 ,  A61K31/415 ,  A61K31/42 ,  A61K31/44 ,  A61K31/443 ,  A61P1/16 ,  C07D261/12 ,  C07D317/54 ,  C07D317/56 ,  C07D317/58 ,  C07D317/60 ,  C07D317/62 ,  C07D405/12 ,  C07D413/12

公开(公告)号：JPH07291967A

公开(公告)日：1995-11-07

申请号：JP27483694

申请日：1994-11-09

申请人： EISAI CO LTD

发明人： SODA SHIGERU ,  UEDA NORIHIRO ,  MIYAZAWA SHUHEI ,  TAGAMI KATSUYA ,  NOMOTO SEIICHIRO ,  OKITA MAKOTO ,  SHIMOMURA NAOYUKI ,  KANEKO TOSHIHIKO ,  FUJIMOTO MASATOSHI ,  MURAKAMI MANABU ,  OKETANI KIYOSHI ,  FUJISAKI HIDEAKI ,  SHIBATA HISASHI ,  WAKABAYASHI TSUNEO

IPC分类号： C07D401/12 ,  A61K31/44 ,  A61K31/4427 ,  A61P1/04

摘要： PURPOSE:To obtain a novel pyridine derivative which is useful as a digestive ulcer agent because it has high safety and excellent antiulcerative action. CONSTITUTION:A pyridine derivative of the formula I or a salt thereof. The derivative is obtained by reaction between compounds of the formulas II and III (Y is halogen, sulfonyloxy), preferably in the presence of an acid acceptor such as potassium carbonate in a solvent such as methanol at -40 deg.C - the boiling point of the solvent, preferably at about 0-60 deg.C. In another process, the reaction of a halide of the formula IV (Hal is halogen) with methanol is carried out, preferably in the presence of an acid acceptor in a solvent such as tetrahydrofuran at ice cooling temperature to the boiling point of the solvent to provide the compound.

公开(公告)号：JPH05247035A

公开(公告)日：1993-09-24

申请号：JP111993

申请日：1993-01-07

申请人： EISAI CO LTD

发明人： SODA SHIGERU ,  UEDA NORIHIRO ,  MIYAZAWA SHUHEI ,  TAGAMI KATSUYA ,  NOMOTO SEIICHIRO ,  OKITA MAKOTO ,  SHIMOMURA NAOYUKI ,  KANEKO TOSHIHIKO ,  FUJIMOTO MASATOSHI ,  MURAKAMI MANABU ,  OKETANI KIYOSHI ,  FUJISAKI HIDEAKI ,  SHIBATA HISASHI ,  WAKABAYASHI TSUNEO

IPC分类号： A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/54 ,  A61P1/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

摘要： PURPOSE:To obtain a new pyridine derivative effective as a therapeutic agent for peptic ulcer having high safety and excellently antiulcer action. CONSTITUTION:A compound of formula I [R and R are H, alkyl, alkoxy, carboxyl, halogen, etc.; X is 0, S or NR (R is H, alkyl, phenyl, etc.); Z is 0(CH2),-0-R ((p) is 1-3: R is H, alkyl, aryl, etc.), 0-(CH2)q-R ((q) is 1-3; R is halogen, alkoxycarbonyl, aryl, etc.), group of formula II to formula IV (R is acetoxy or alkyl) or OR (R is H, alkyl or aryl), etc.; (n) is 0-2; (m) is 2-10; J and K are H or alkyl) or its salt such as 2-[{4-(3-methoxypropoxy)-3- methylpyridin-2-yl)}methylsulfinyl]-1H-benzimidazole sodium salt. The compound of formula I wherein (n) is 0 is obtained by reacting a compound of formula V with a compound of formula VI (X is halogen or sulfonyloxy).

公开(公告)号：JPH0249792A

公开(公告)日：1990-02-20

申请号：JP11913289

申请日：1989-05-12

申请人： EISAI CO LTD

发明人： SODA SHIGERU ,  MIYAZAWA SHUHEI ,  UEDA NORIHIRO ,  TAGAMI KATSUYA ,  NOMOTO SEIICHIRO ,  OKITA MAKOTO ,  SHIMOMURA NAOYUKI ,  KANEKO TOSHIHIKO ,  FUJIMOTO MASATOSHI ,  MURAKAMI MANABU ,  OKETANI KIYOSHI ,  FUJISAKI HIDEAKI ,  SHIBATA HISASHI ,  WAKABAYASHI TSUNEO

IPC分类号： C07D513/14 ,  A61K31/54 ,  A61P1/04

摘要： NEW MATERIAL:The compound of formula I [R and R are H, lower alkyl, lower alkoxy, halogenated lower alkyl, halogen, etc.; R and R are H or lower alkyl; m is 2-10; Z is -OR (R is H, lower alkyl, aryl, etc.) or -O-(CH2)n-O-R (n is 1-3; R is H, lower alkyl, aryl, etc.); X is anion]. EXAMPLE:3-(3-Methoxy)propoxy-4-methyl-5H-pyrido[1',2':4,5][1,2,4]-thia diazino[2,3- a]benzimidazol-13-ium tetrafluoroborate. USE:An antiulcer agent having excellent action to suppress the secretion of gastric acid. PREPARATION:A pyridine derivative of formula III is subjected to thermal reaction in the presence of an acid.

公开(公告)号：JPS6479177A

公开(公告)日：1989-03-24

申请号：JP14714088

申请日：1988-06-15

申请人： EISAI CO LTD

发明人： SODA SHIGERU ,  UEDA NORIHIRO ,  MIYAZAWA SHUHEI ,  TAGAMI KATSUYA ,  NOMOTO SEIICHIRO ,  OKITA MAKOTO ,  SHIMOMURA NAOYUKI ,  KANEKO TOSHIHIKO ,  FUJIMOTO MASATOSHI ,  MURAKAMI MANABU ,  OKETANI KIYOSHI ,  FUJISAKI HIDEAKI ,  SHIBATA HISASHI ,  WAKABAYASHI TSUNEO

IPC分类号： C07D401/12 ,  A61K31/44 ,  A61K31/4427 ,  A61P1/04

摘要： NEW MATERIAL:A pyridine derivative expressed by formula I (R and R are H, lower alkyl, lower alkoxy, halogenated lower alkyl or halogen; R and R are H or lower alkyl; X is S, formula II or III; n is an integer of 1-6, provided that both R and R are not H when n is 1) and pharmacologically acceptable salt thereof. EXAMPLE:2-[4-{(2-Ethoxy)ethoxy}-3-methylpyridin-2-yl]methylthio-1H-ben zimida zole. USE:An agent for peptic ulcer. PREPARATION:A compound expressed by formula IV is reacted with a com pound expressed by formula V (Y is halogen or various sulfonyloxy groups) or a compound expressed by formula VI (Hal is halogen) is reacted with a compound expressed by the formula HO-(CH2)n-H to afford the aimed compound expressed by formula I (X is S), which, as desired, is then oxidized to provide the aimed compound expressed by formula I (X is formula II-III).

公开(公告)号：JPH09309879A

公开(公告)日：1997-12-02

申请号：JP14856996

申请日：1996-05-20

申请人： EISAI CO LTD

发明人： TANAKA MASAYUKI ,  OKITA MAKOTO ,  MIYAMOTO MITSUAKI ,  KANEKO TOSHIHIKO ,  KAWAHARA TETSUYA ,  AKAMATSU HIROSHI ,  CHIBA KENICHI ,  OHAISHI HIROSHI ,  SAKURAI HIDEKI ,  ABE SHINYA ,  KOBAYASHI SEIICHI ,  YAMANAKA TEIJI

IPC分类号： C07D335/06 ,  A61K31/35 ,  A61K31/352 ,  A61K31/38 ,  A61K31/382 ,  A61K31/47 ,  A61K31/535 ,  A61P29/00 ,  A61P37/00 ,  A61P43/00 ,  C07D215/22 ,  C07D311/22 ,  C07D491/052 ,  C07D495/04

摘要： PROBLEM TO BE SOLVED: To obtain an α,β-unsaturated ketone derivative useful for treating and preventing autoimmune disease such as chronic arthrorheumatism, inflammatory disease, etc., as interleukin 1 production suppressor. SOLUTION: This compound is represented by formula I [ring A is a group of formula II (ring B is an aromatic; R is H, a halogen, a lower alkyl, etc.; R is H, a lower alkyl, etc.; R is a group of formula III (R and R are each H, a lower alkyl, etc.; R is H, an aryl, etc.)] or its salt, e.g. 1,4-dihydro-7- ethyl-2-(4-hydroxy-4-methyl-3-oxo-1-pentenyl)-4-oxo-3,5,8-trimethoxyqu inoline. The compound of formula I is obtained by subjecting an aldehyde compound of formula IV (R to R are each H, OH, a halogen, a lower alkyl, etc.) to Witting reaction with a phosphorane of the formula (C6 H5 )3 P=CHCOR according to an ordinary method.

公开(公告)号：JPH08311032A

公开(公告)日：1996-11-26

申请号：JP14239495

申请日：1995-05-18

申请人： EISAI CO LTD

发明人： TANAKA MASAYUKI ,  OKITA MAKOTO ,  MIYAMOTO MITSUAKI ,  KANEKO TOSHIHIKO ,  KAWAHARA TETSUYA ,  AKAMATSU HIROSHI ,  CHIBA KENICHI ,  OHAISHI HIROSHI ,  SAKURAI HIDEKI ,  ABE SHINYA ,  KOBAYASHI SEIICHI ,  YAMANAKA TEIJI

IPC分类号： C07D335/06 ,  A61K31/35 ,  A61K31/352 ,  A61K31/38 ,  A61K31/382 ,  A61K31/435 ,  A61K31/47 ,  A61K31/495 ,  A61K31/505 ,  A61P29/00 ,  A61P37/00 ,  A61P43/00 ,  C07D215/22 ,  C07D215/227 ,  C07D215/26 ,  C07D215/36 ,  C07D215/48 ,  C07D311/58 ,  C07D471/04 ,  C07D491/052 ,  C07D495/04

摘要： PURPOSE: To obtain the subject compound exhibiting an excellent interleukin production-inhibiting action and useful for medicines for preventing and treating syndromes mediated with the interleukin 1. CONSTITUTION: A compound of formula I the ring A is a group of formula II [the ring B is a (substituted) aromatic ring; R is H, a halogen, (halogenated) lower alkyl, (heterogeneous atom-containing) cycloalkyl, a (substituted) (hetero) aryl(alkyl), etc.; R is H, a (halogenated) lower alkyl, a (heterogeneous atom- containing) cycloalkyl, an alkoxyalkyl, etc.,], a group of formula III, etc.; R is a group of formula IV [R , R are H, a (halogenated) lower alkyl, a (heterogeneous atom-containing) cycloalkyl, etc.; R is H, a (halogenated) lower alkyl, a (heterogeneous atom-containing) cycloalkyl, etc.,], etc.,}, its salt. For example, 1,4-dihydroxy-7-ethyl-2-(4-hydroxy-4-methyl-3-oxo-1-pentenyl)-4-oxo-3, 5,8- trimethoxyquionline.

公开(公告)号：JP2535532B2

公开(公告)日：1996-09-18

申请号：JP10372487

申请日：1987-04-27

申请人： EISAI CO LTD

发明人： OGATA YOSHITAKE ,  IKEDA MAKOTO ,  NOMOTO SEIICHIRO ,  OKITA MAKOTO ,  SHIMOMURA NAOYUKI ,  KANEKO TOSHIHIKO ,  YAMANAKA TEIJI ,  HISHINUMA TAKAHARU ,  NAGAGAWA JUNICHI ,  HIROTA KAZUO ,  MYAMOTO KANAME ,  HORIE TOORU ,  WAKABAYASHI TSU

IPC分类号： C07D317/60 ,  A61K31/335 ,  A61K31/357 ,  A61K31/36 ,  A61P1/16 ,  C07D317/70 ,  C07D493/04