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公开(公告)号:EP3318557A3
公开(公告)日:2018-07-11
申请号:EP17202139.6
申请日:2012-08-30
发明人: ABUDUSAIMI, Mamuti , YE, Fangguo , SUN, Jiangqin , MIYAMOTO, Hisashi , CHENG, Jay-Fei , OKA, Daisuke
IPC分类号: C07D215/56 , C07D471/04 , A61K31/47 , A61K31/435
CPC分类号: C07D215/56 , C07D401/04 , C07D401/10 , C07D401/14 , C07D405/04 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D471/04 , C07D487/04 , C07D498/04 , C07D498/06 , C07D519/00
摘要: The present invention provides a compound represented by the formula (I)
wherein X is a hydrogen atom or a fluorine atom; R is a hydrogen atom or alkyl; R 1 is (1) cyclopropyl optionally substituted by 1 to 3 halogen atoms or (2) phenyl optionally substituted by 1 to 3 halogen atoms; R 2 is alkyl, alkoxy, haloalkoxy, a halogen atom, cyano, etc.; and R 3 is 7-oxo-7,8-dihydro-1,8-naphthyridinyl, 3-pyridyl, etc., or a salt thereof. The compound of the present invention has excellent antimicrobial activity against Clostridium difficile and is useful for the prevention or treatment of intestinal infection such as Clostridium difficile- associated diarrhea.-
公开(公告)号:EP0450097A1
公开(公告)日:1991-10-09
申请号:EP90915185.0
申请日:1990-10-18
发明人: OGAWA, Hidenori , MIYAMOTO, Hisashi , KONDO, Kazumi , YAMASHITA, Hiroshi , NAKAYA, Kenji , KOMATSU, Hajime , TANAKA, Michinori , KORA, Shinya , TOMINAGA, Michiaki , YABUUCHI, Yoichi
IPC分类号: C07D243 , A61K31 , A61P1 , A61P3 , A61P7 , A61P9 , A61P13 , A61P15 , C07D215 , C07D223 , C07D225 , C07D241 , C07D245 , C07D265 , C07D267 , C07D279 , C07D281 , C07D401 , C07D403 , C07D405 , C07D409 , C07D413 , C07D417 , C07D491 , C07D498
CPC分类号: C07D215/233 , C07D215/08 , C07D215/12 , C07D215/14 , C07D215/20 , C07D215/38 , C07D215/42 , C07D215/54 , C07D223/16 , C07D225/06 , C07D241/42 , C07D243/12 , C07D243/14 , C07D265/36 , C07D267/14 , C07D279/16 , C07D281/10 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D491/04 , C07D491/10
摘要: Nouveaux composés benzohétérocycliques de formule (I), dans laquelle R1 représente H, halogène, alkyle, amino éventuellement substitué, alcoxy; R2 représente H, halogène, alcoxy, phénylalcoxy, OH, alkyle, amino éventuellement substitué, carbamoyle-alcoxy, amino-alcoxy éventuellement substitué, benzoyloxy éventuellement substitué; R3 représente un groupe -NR4R5 ou -CO-NR11R12; R4 est H, benzoyle éventuellement substitué, alkyle; R5 est un groupe alpha [dans lequel R16 représente halogène, alkyle éventuellement substitué, OH, alcoxy, alcanoyloxy, alkylthio, alcanoyle, carboxy, alcoxycarbonyle, CN, NO2, amino éventuellement substitué, phényle, cycloalkyle, etc., ou un groupe -OA-NR6R7; m est compris entre 0 et 3], phényl-alcoxycarbonyle, alcanoyle, phényl-alcanoyle, etc.; R11 représente H ou alkyle; R12 représente cycloalkyle ou phényle éventuellement substitué; et W est un groupe -CH2)p (p étant compris entre 3 et 5) ou -CH=CH-(CH2)q (q étant compris entre 1 et 3), l'atome de carbone de ces groupes étant éventuellement remplacé par 0, S, SO, SO2 ou un groupe -N(R13)-, ces groupes comportant éventuellement de 1 à 3 substituants d'alkyle, alcoxycarbonyle, carboxy, OH, O, alcanoyloxy, etc. Ces composés présentent d'excellentes activités antagonistes de la vasopressine et sont utiles en tant que vasodilateurs, agents hypotensifs, diurétiques et inhibiteurs d'agglutination de plaquettes. On décrit également une composition antagoniste de la vasopressine contenant ce composé en tant qu'ingrédient actif.
摘要翻译: 式(I)的新型苯并杂环化合物,其中R 1为H,卤素,烷基,任选取代的氨基,烷氧基; R2代表H,卤素,烷氧基,苯基烷氧基,OH,烷基,任选取代的氨基,氨基甲酰基 - 烷氧基,任选取代的氨基 - 烷氧基,任选取代的苯甲酰氧基; R3是-NR4R5或-CO-NR11R12; R4是H,任选取代的苯甲酰基,烷基; R5是α-团[其中R 16代表卤素,任选取代的烷基,OH,烷氧基,烷酰氧基,烷硫基,烷酰基,羧基,烷氧基,CN,NO 2,任选取代的氨基,苯基,环烷基等,或基团-OA -NR6R7; m为0-3,苯基 - 烷氧基羰基,烷酰基,苯基 - 烷酰基等; R11是H或烷基; R12代表环烷基或任选取代的苯基; 和W是基团-CH 2)p(p在3和5之间)或-CH = CH-(CH 2)q(q在1和3之间)时,这些基团的碳原子任选被 O,S,SO,SO 2或基团-N(R 13) - ,这些基团可能包含1至3个烷基,烷氧基羰基,羧基,OH,O,烷酰氧基等的取代基 这些化合物具有优良的加压素拮抗剂活性,可用作血管扩张剂,降血压药,利尿剂和血小板凝集抑制剂。 还公开了含有该化合物作为活性成分的加压素拮抗剂组合物。
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公开(公告)号:EP2751083A1
公开(公告)日:2014-07-09
申请号:EP12827305.9
申请日:2012-08-30
发明人: ABUDUSAIMI, Mamuti , YE, Fangguo , SUN, Jiangqin , MIYAMOTO, Hisashi , CHENG, Jay-Fei , OKA, Daisuke
IPC分类号: C07D215/56 , C07D471/04 , A61K31/47 , A61K31/435
CPC分类号: C07D215/56 , C07D401/04 , C07D401/10 , C07D401/14 , C07D405/04 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D471/04 , C07D487/04 , C07D498/04 , C07D498/06 , C07D519/00
摘要: The present invention provides a compound represented by the formula (I) wherein X is a hydrogen atom or a fluorine atom; R is a hydrogen atom or alkyl; R
1 is (1) cyclopropyl optionally substituted by to 3 halogen atoms or (2) phenyl optionally substituted by 1 to 3 halogen atoms; R
2 is alkyl, alkoxy, haloalkoxy, a halogen atom, cyano, etc.; and R
3 is 7-oxo-7,8-dihydro-1,8-naphthyridinyl, 3-pyridyl, etc., or a salt thereof. The compound of the present invention has excellent antimicrobial activity against Clostridium difficile and is useful for the prevention or treatment of intestinal infection such as Clostridium difficile- associated diarrhea.-
公开(公告)号:EP1489080A1
公开(公告)日:2004-12-22
申请号:EP03788701.5
申请日:2003-09-09
发明人: YAMAMOTO, Akihiro , FUKUYAMA, Norihiro , OKAICHI, Yoshihiko , YAMADA, Yasuhiro , MIYAMOTO, Hisashi , TOMINAGA, Michiaki
IPC分类号: C07D401/12
CPC分类号: C07D401/12
摘要: The present invention provides a process for producing cilostazol [I] in a high yield and a high purity, by reacting a carbostyril derivative [II] with a tetrazole derivative [III] in the presence of an inorganic basic compound in a solvent of water, wherein water is used in an amount of 3 to 7-fold weight to that of the carbostyril derivative [II] and the inorganic basic compound is used in an amount of 1 to 6 mol per mol of the carbostyril derivative [II]. The process of the present invention is the improved and environment-friendly process for producing cilostazol being useful for pharmaceuticals.
摘要翻译: 本发明通过在无水碱性化合物存在下在水溶剂中使喹诺酮衍生物ÄIIu与四唑衍生物ÄIIIby反应,提供了以高产率和高纯度生产西洛他唑ÄI的方法,其中使用水 喹诺酮衍生物的量为3至7倍,无机碱性化合物的用量为每摩尔喹诺酮衍生物ÄIIÜ为1至6摩尔。 本发明的方法是用于制备用于药物的西洛他唑的改进和环境友好的方法。
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公开(公告)号:EP1489080B1
公开(公告)日:2011-01-26
申请号:EP03788701.5
申请日:2003-09-09
发明人: YAMAMOTO, Akihiro , FUKUYAMA, Norihiro , OKAICHI, Yoshihiko , YAMADA, Yasuhiro , MIYAMOTO, Hisashi , TOMINAGA, Michiaki
IPC分类号: C07D401/12
CPC分类号: C07D401/12
摘要: A carbostyril derivative [II] is reacted with a tetrazole derivative [III] in a water solvent used in an amount 3 to 7 times by weight the amount of the carbostyril derivative [II] in the presence of an inorganic basic compound used in an amount 1 to 6 times by mole the amount of the carbostyril derivative [II] to produce high-purity cilostazol [I] in high yield. The process for producing cilostazol, which is useful as a medicine, is an improved process safe for the environment. [I] [II] [III]
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公开(公告)号:EP3318557A2
公开(公告)日:2018-05-09
申请号:EP17202139.6
申请日:2012-08-30
发明人: ABUDUSAIMI, Mamuti , YE, Fangguo , SUN, Jiangqin , MIYAMOTO, Hisashi , CHENG, Jay-Fei , OKA, Daisuke
IPC分类号: C07D215/56 , C07D471/04 , A61K31/47 , A61K31/435
CPC分类号: C07D215/56 , C07D401/04 , C07D401/10 , C07D401/14 , C07D405/04 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D471/04 , C07D487/04 , C07D498/04 , C07D498/06 , C07D519/00
摘要: The present invention provides a compound represented by the formula (I)
wherein X is a hydrogen atom or a fluorine atom; R is a hydrogen atom or alkyl; R 1 is (1) cyclopropyl optionally substituted by 1 to 3 halogen atoms or (2) phenyl optionally substituted by 1 to 3 halogen atoms; R 2 is alkyl, alkoxy, haloalkoxy, a halogen atom, cyano, etc.; and R 3 is 7-oxo-7,8-dihydro-1,8-naphthyridinyl, 3-pyridyl, etc., or a salt thereof. The compound of the present invention has excellent antimicrobial activity against Clostridium difficile and is useful for the prevention or treatment of intestinal infection such as Clostridium difficile- associated diarrhea.摘要翻译: 本发明提供由式(I)表示的化合物,其中X是氢原子或氟原子; R是氢原子或烷基; R1为(1)任选被1至3个卤素原子取代的环丙基或(2)任选被1至3个卤素原子取代的苯基; R2为烷基,烷氧基,卤代烷氧基,卤素原子,氰基等; 和R3是7-氧代-7,8-二氢-1,8-二氮杂萘基,3-吡啶基等,或其盐。 本发明化合物对艰难梭菌具有优良的抗微生物活性,并且可用于预防或治疗肠道感染如艰难梭菌相关性腹泻。
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公开(公告)号:EP2751083B1
公开(公告)日:2017-12-27
申请号:EP12827305.9
申请日:2012-08-30
发明人: ABUDUSAIMI, Mamuti , YE, Fangguo , SUN, Jiangqin , MIYAMOTO, Hisashi , CHENG, Jay-Fei , OKA, Daisuke
IPC分类号: C07D215/56 , C07D471/04 , A61K31/47 , A61K31/435
CPC分类号: C07D215/56 , C07D401/04 , C07D401/10 , C07D401/14 , C07D405/04 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D471/04 , C07D487/04 , C07D498/04 , C07D498/06 , C07D519/00
摘要: The present invention provides a compound represented by the formula (I) wherein X is a hydrogen atom or a fluorine atom; R is a hydrogen atom or alkyl; R 1 is (1) cyclopropyl optionally substituted by 1 to 3 halogen atoms or (2) phenyl optionally substituted by 1 to 3 halogen atoms; R 2 is alkyl, alkoxy, haloalkoxy, a halogen atom, cyano, etc.; and R 3 is 7-oxo-7,8-dihydro-1,8-naphthyridinyl, 3-pyridyl, etc., or a salt thereof. The compound of the present invention has excellent antimicrobial activity against Clostridium difficile and is useful for the prevention or treatment of intestinal infection such as Clostridium difficile- associated diarrhea.
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公开(公告)号:EP0450097B1
公开(公告)日:1996-04-24
申请号:EP90915185.4
申请日:1990-10-18
发明人: OGAWA, Hidenori , MIYAMOTO, Hisashi , KONDO, Kazumi , YAMASHITA, Hiroshi , NAKAYA, Kenji , KOMATSU, Hajime , TANAKA, Michinori , KORA, Shinya , TOMINAGA, Michiaki , YABUUCHI, Yoichi
IPC分类号: A61K31/00 , C07D215/08 , C07D215/12 , C07D223/16 , C07D225/06 , C07D241/42 , C07D243/14 , C07D265/36 , C07D267/14
CPC分类号: C07D215/233 , C07D215/08 , C07D215/12 , C07D215/14 , C07D215/20 , C07D215/38 , C07D215/42 , C07D215/54 , C07D223/16 , C07D225/06 , C07D241/42 , C07D243/12 , C07D243/14 , C07D265/36 , C07D267/14 , C07D279/16 , C07D281/10 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D491/04 , C07D491/10
摘要: Novel benzoheterocyclic compounds of formula (I), wherein R1 is H, halogen, alkyl, optionally substituted amino, alkoxy; R2 is H, halogen, alkoxy, phenylalkoxy, OH, alkyl, optionally substituted amino, carbamoyl-alkoxy, optionally substituted amino-alkoxy, optionally substituted benzoyloxy; R3 is a group: -NR4R5 or -CO-NR?11R12; R4¿ is H, optionally substituted benzoyl, alkyl; R5 is a group α [R16 is halogen, optionally substituted alkyl, OH, alkoxy, alkanoyloxy, alkylthio, alkanoyl, carboxy, alkoxycarbonyl, CN, NO¿2?, optionally substituted amino, phenyl, cycloalkyl, etc., or a group: -O-A-NR?6R7¿; m is 0 to 3], phenyl-alkoxycarbonyl, alkanoyl, phenyl-alkanoyl, etc.; R11 is H or alkyl; R12 is cycloalkyl or optionally substituted phenyl; and W is a group: -(CH¿2?)p (p is 3 to 5) or -CH=CH-(CH2)q (q is 1 to 3), the carbon atom of these groups being optionally replaced by 0, S, SO, SO2 or a group: -N(R?13¿)- and further these groups having optionally 1 to 3 substituents of alkyl, alkoxycarbonyl, carboxy, OH, O, alkanoyloxy, etc., which have excellent vasopressin antagonistic activies and are useful as vasodilator, hypotensive agent, water diuretics, platelet agglutination inhibitor, and a vasopressin antagonistic composition containing the compound as the active ingredient.
摘要翻译: 式(I)的新型苯并杂环化合物,其中R 1为H,卤素,烷基,任选取代的氨基,烷氧基; R2是H,卤素,烷氧基,苯基烷氧基,OH,烷基,任选取代的氨基,氨基甲酰基 - 烷氧基,任选取代的氨基 - 烷氧基,任选取代的苯甲酰氧基; R3是基团:-NR4R5或-CO-NR11R12; R4是H,任选取代的苯甲酰基,烷基; R5是基团α[R16是卤素,任选取代的烷基,OH,烷氧基,烷酰氧基,烷硫基,烷酰基,羧基,烷氧羰基,CN,NO2,任选取代的氨基,苯基,环烷基等, -OA-NR6R7¿?; m为0〜3],苯基 - 烷氧基羰基,烷酰基,苯基 - 烷酰基等。 R11是H或烷基; R12是环烷基或任选取代的苯基; 和W是基团: - (CH 2 2)p(p为3-5)或-CH = CH-(CH 2)q(q为1-3),这些基团的碳原子任选被0 ,S,SO,SO 2或基团-N(R 13') - 和进一步具有1-3个烷基,烷氧基羰基,羧基,OH,O,烷酰氧基等取代基的这些基团,它们具有优良的加压素拮抗作用 可用作血管扩张剂,降血压剂,水利尿剂,血小板凝集抑制剂和含有该化合物作为活性成分的加压素拮抗组合物。
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公开(公告)号:EP0602209A1
公开(公告)日:1994-06-22
申请号:EP93913553.0
申请日:1993-06-22
发明人: OGAWA, H, 25-18, Nakakirai-Aza Nakasenishinoko-shi , MIYAMOTO, Hisashi , KONDO, Kazumi , YAMASHITA, Hiroshi , NAKAYA, Kenji , TANAKA, Michinori , KITANO, Kazuyoshi , KAN, Keizo , TOMINAGA, Michiaki , YABUUCHI, Yoichi
IPC分类号: A61K31
CPC分类号: A61K31/44 , A61K31/47 , A61K31/495 , A61K31/535 , A61K31/55
摘要: L'invention concerne un antagoniste de l'oxytocine qui comprend, comme ingrédient actif, le dérivé carbostyrile répondant à la formule (1) ou bien le composé benzohétérocyclique répondant à la formule (2), ou bien un sel pharmaceutiquement acceptable dudit dérivé ou dudit composé. L'antagoniste selon l'invention présente une excellente activité dirigée contre l'oxytocine et peut, par conséquent, être utilisé dans la prévention ou le traitement de maladies associées à l'oxytocine, notamment pour prévenir un accouchement prématuré, pour traiter les dysménorrhées et les endométrites, ou bien pour stopper le travail afin de pouvoir pratiquer une césarienne.
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