公开(公告)号：US4256885A

公开(公告)日：1981-03-17

申请号：US749433

申请日：1976-12-10

申请人： Atsushi Kojima ,  Yoshitsugu Kohno ,  Yoshimasa Ike ,  Tatsuro Yokoyama ,  Makoto Odate

发明人： Atsushi Kojima ,  Yoshitsugu Kohno ,  Yoshimasa Ike ,  Tatsuro Yokoyama ,  Makoto Odate

IPC分类号： A61K31/505 ,  C07D20060101 ,  C07D239/00 ,  C07D239/10 ,  C07D239/30 ,  C07D239/54 ,  C07D307/04 ,  C07D307/22 ,  C07D405/04

摘要： A process for efficiently preparing 1-(2-tetrahydrofuryl)-5-fluorouracil useful as an antitumor agent or an antiviral agent which comprises reacting 5-fluorouracil with 2,3-dihydrofuran. This reaction proceeds advantageously in the presence of a reaction accelerator such as a Lewis acid in a polar solvent such as pyridine.

摘要翻译： 一种有效制备用作抗肿瘤剂或抗病毒剂的1-（2-四氢呋喃基）-5-氟尿嘧啶的方法，其包括使5-氟尿嘧啶与2,3-二氢呋喃反应。 该反应有利地在诸如吡啶等极性溶剂中的路易斯酸等反应促进剂的存在下进行。

公开(公告)号：US5204348A

公开(公告)日：1993-04-20

申请号：US780472

申请日：1991-12-03

申请人： Nobuyuki Fukazawa ,  Makoto Odate ,  Tsuneji Suzuki ,  Kengo Otsuka ,  Takashi Tsuruo ,  Wakao Sato

发明人： Nobuyuki Fukazawa ,  Makoto Odate ,  Tsuneji Suzuki ,  Kengo Otsuka ,  Takashi Tsuruo ,  Wakao Sato

IPC分类号： C07D215/20 ,  C07D215/22 ,  C07D215/227 ,  C07D215/26 ,  C07D215/36 ,  C07D215/38 ,  C07D217/02 ,  C07D239/74 ,  C07D241/42 ,  C07D401/12 ,  C07D405/12

CPC分类号： C07D215/227 ,  C07D215/20 ,  C07D215/26 ,  C07D215/36 ,  C07D215/38 ,  C07D217/02 ,  C07D239/74 ,  C07D241/42 ,  C07D401/12 ,  C07D405/12

摘要： Novel heterocyclic compounds, which are represented by the following general formula, useful as anticancer drug potentiaters having a potentiating effect on the incorporation of anticancer drugs into cancer cells, the compounds each synthesized by, for example, reacting a epoxy compound obtained by reacting a heterocyclic compound with an epihalogenohydrin, with an amine derivative.

摘要翻译： 由以下通式表示的新型杂环化合物可用作对抗癌药物掺入癌细胞具有增强作用的抗癌药物增效剂，所述化合物通过例如使通过使杂环反应获得的环氧化合物 与表卤代醇与胺衍生物的化合物。

公开(公告)号：US4990529A

公开(公告)日：1991-02-05

申请号：US334249

申请日：1989-04-06

申请人： Hiroyuki Yamashita ,  Makoto Odate ,  Hajime Iizuka ,  Hiroshi Kawazura ,  Yoshio Shiga ,  Hiroshi Namekawa

发明人： Hiroyuki Yamashita ,  Makoto Odate ,  Hajime Iizuka ,  Hiroshi Kawazura ,  Yoshio Shiga ,  Hiroshi Namekawa

IPC分类号： A61K31/415 ,  C07D231/06 ,  C07D401/04 ,  C07D401/06 ,  C07D403/06 ,  C07D405/06 ,  C07D405/14 ,  C07D409/06

CPC分类号： C07D231/06 ,  C07D401/04 ,  C07D401/06 ,  C07D403/06 ,  C07D405/06 ,  C07D405/14 ,  C07D409/06

摘要： 2-Pyrazoline derivatives of the formula (A): ##STR1## where R.sup.1 is a pyridyl, a pyrazyl or an alkoxyl group; and R.sup.2 is a hydrogen atom, an alkyl, a pyridyl, a furyl, phenyl or a substituted phenyl group, and to a process for producing the same. Therapeutic agents for treating cerebrovascular diseases containing, as the active ingredient, a 2-pyrazoline derivative represented by the formula (G): ##STR2## where R.sup.3 is a hydrogen atom, an alkyl, acetyl, an alkoxycarbonyl, an amino, benzoyl, a substituted benzoyl, a pyridylcarbonyl, a furylcabonyl, a thienylcarbonyl, a pyrazylocarbonyl, an N-substituted carbamoyl, an N-substituted thiocarbamoyl, or carboxyl group; and R.sup.4 is a hydrogen atom, an alkyl, a pyridyl, a thienyl, a furyl, cyclohexyl, phenyl or a substituted phenyl group or a pharmaceutically acceptable salt thereof. These therapeutic agents cope with cerebral edemas in the acute stage of cerebral apoplexy and regulates the whole-body and intracranial body circulation, thereby protecting ischemic lesions and minimizing the spread to affected parts.

公开(公告)号：US4296112A

公开(公告)日：1981-10-20

申请号：US104292

申请日：1979-12-17

申请人： Akira Matsubara ,  Hideaki Sakai ,  Makoto Odate ,  Toshio Suganuma ,  Takuo Nakano

发明人： Akira Matsubara ,  Hideaki Sakai ,  Makoto Odate ,  Toshio Suganuma ,  Takuo Nakano

IPC分类号： C07D501/34 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D501/20 ,  C07D501/24 ,  C07D501/36

CPC分类号： C07D501/24

摘要： A cephalosporanic acid of the general formula ##STR1## wherein A represents ##STR2## and the pharmaceutically acceptable salt and ester thereof.

摘要翻译： 一种通式为“IMAGE”的头孢菌素酸，其中A代表“IMAGE”及其药学上可接受的盐和酯。

公开(公告)号：US5405843A

公开(公告)日：1995-04-11

申请号：US123842

申请日：1993-09-09

申请人： Nobuyuki Fukazawa ,  Makoto Odate ,  Tsuneji Suzuki ,  Kengo Otsuka ,  Takashi Tsuruo ,  Wakao Sato

发明人： Nobuyuki Fukazawa ,  Makoto Odate ,  Tsuneji Suzuki ,  Kengo Otsuka ,  Takashi Tsuruo ,  Wakao Sato

IPC分类号： C07D215/20 ,  C07D215/22 ,  C07D215/227 ,  C07D215/26 ,  C07D215/36 ,  C07D215/38 ,  C07D217/02 ,  C07D239/74 ,  C07D241/42 ,  C07D401/12 ,  C07D405/12 ,  C07D403/12 ,  A61K31/38

CPC分类号： C07D215/227 ,  C07D215/20 ,  C07D215/26 ,  C07D215/36 ,  C07D215/38 ,  C07D217/02 ,  C07D239/74 ,  C07D241/42 ,  C07D401/12 ,  C07D405/12

摘要： Heterocyclic compounds useful as anticancer drug potentiaters having a potentiating effect on the incorporation of anticancer drugs into cancer cells are disclosed, the compounds each synthesized by, for example, reacting a epoxy compound obtained by reacting a heterocyclic compound with an epihalogenohydrin, with an amine derivative.

摘要翻译： 公开了用作抗癌药物加入癌细胞的增强作用的抗癌药物增效剂的杂环化合物，其通过例如使杂环化合物与表卤代醇反应获得的环氧化合物与胺衍生物 。

公开(公告)号：US5112817A

公开(公告)日：1992-05-12

申请号：US417780

申请日：1992-10-06

申请人： Nobuyuki Fukazawa ,  Makoto Odate ,  Tsuneji Suzuki ,  Kengo Otsuka ,  Takashi Tsuruo ,  Wakao Sato

发明人： Nobuyuki Fukazawa ,  Makoto Odate ,  Tsuneji Suzuki ,  Kengo Otsuka ,  Takashi Tsuruo ,  Wakao Sato

IPC分类号： C07D215/20 ,  C07D215/22 ,  C07D215/227 ,  C07D215/26 ,  C07D215/36 ,  C07D215/38 ,  C07D217/02 ,  C07D239/74 ,  C07D241/42 ,  C07D401/12 ,  C07D405/12

CPC分类号： C07D215/227 ,  C07D215/20 ,  C07D215/26 ,  C07D215/36 ,  C07D215/38 ,  C07D217/02 ,  C07D239/74 ,  C07D241/42 ,  C07D401/12 ,  C07D405/12

摘要： Novel heterocyclic compounds, which are represented by the following general formula, useful as anticancer drug potentiaters having a potentiating effect on the incorporation of anticancer drugs into cancer cells, the compounds each synthesized by, for example, reacting a epoxy compound obtained by reacting a heterocyclic compound with an epihalogenohydrin, with an amine derivative.

公开(公告)号：US4839376A

公开(公告)日：1989-06-13

申请号：US206812

申请日：1988-06-15

申请人： Hiroyuki Yamashita ,  Makoto Odate ,  Hajime Iizuka ,  Hiroshi Kawazura ,  Yoshio Shiga ,  Hiroshi Namekawa

发明人： Hiroyuki Yamashita ,  Makoto Odate ,  Hajime Iizuka ,  Hiroshi Kawazura ,  Yoshio Shiga ,  Hiroshi Namekawa

IPC分类号： A61K31/415 ,  C07D231/06 ,  C07D401/04 ,  C07D401/06 ,  C07D403/06 ,  C07D405/06 ,  C07D405/14 ,  C07D409/06

CPC分类号： C07D231/06 ,  C07D401/04 ,  C07D401/06 ,  C07D403/06 ,  C07D405/06 ,  C07D405/14 ,  C07D409/06

摘要： 2-Pyrazoline derivatives of the formula (A): ##STR1## where R.sup.1 is a pyridyl, a pyrazyl or an alkoxy group; and R.sup.2 is a hydrogen atom, an alkyl, a pyridyl, a furyl, phenyl or a substituted phenyl group, and to a process for producing the same. Therapeutic agents for treating cerebrovascular diseases containing, as the active ingredient, a 2-pyrazoline derivative represented by the formula (G): ##STR2## where R.sup.3 is a hydrogen atom, an alkyl, acetyl, an alkoxycarbonyl, an amino, benzoyl, a substituted benzoyl, a pyridylcarbonyl, a furylcarbonyl, a thienylcarbonyl, a pyrazylcarbonyl, an N-substituted carbamoyl, an N-substituted thiocarbamoyl, or carboxy group; and R.sup.4 is a hydrogen atom, an alkyl, a pyridyl, a thienyl, a furyl, cyclohexyl, phenyl or a substituted phenyl group or a pharmaceutically acceptable salt thereof. These therapeutic agents cope with cerebral edemas in the acute stage of cerebral apoplexy and regulates the whole-body and intracranial body circulation, thereby protecting ischemic lesions and minimizing the spread to affected parts.

公开(公告)号：US4273932A

公开(公告)日：1981-06-16

申请号：US116560

申请日：1980-01-29

申请人： Akira Matsubara ,  Hideaki Sakai ,  Makoto Odate ,  Takuo Nakano

发明人： Akira Matsubara ,  Hideaki Sakai ,  Makoto Odate ,  Takuo Nakano

IPC分类号： C07D215/56 ,  C07D499/04 ,  C07D499/64 ,  C07D499/68 ,  A61K31/47

CPC分类号： C07D215/56

摘要： Disclosed is a quinoline derivative having the general formula ##STR1## where A represents a six-membered hydrocarbon ring; X represents an oxygen atom, an .dbd.NOR.sup.1 group in which R.sup.1 is a hydrogen atom or a lower alkyl radical of from 1 to 5 carbon atoms, a hydroxyl group, or an --NHR.sup.2 group in which R.sup.2 is a hydrogen atom or an acyl group; and Y represents a hydrogen atom, a salt-forming radical, or an ester-forming radical. This quinoline derivative is a novel compound which has antiallergic effects in itself and is useful as an intermediate in the production of penicillin or cephalosporin derivatives.

摘要翻译： 公开了具有通式的喹啉衍生物，其中A表示六元烃环; X表示氧原子，其中R 1是氢原子或具有1至5个碳原子的低级烷基，羟基或其中R 2是氢原子或酰基的-NHR 2基团的= NOR1基团 ; Y表示氢原子，成盐基或成酯基。 该喹啉衍生物是本身具有抗过敏作用的新化合物，可用作青霉素或头孢菌素衍生物生产中的中间体。