公开(公告)号：US06831083B2

公开(公告)日：2004-12-14

申请号：US10239311

申请日：2002-09-20

申请人： Junya Fujiwara ,  Kazuya Sakai ,  Kenji Kibayashi ,  Fumiki Shimada ,  Yoshio Shiga ,  Shiro Takagi

发明人： Junya Fujiwara ,  Kazuya Sakai ,  Kenji Kibayashi ,  Fumiki Shimada ,  Yoshio Shiga ,  Shiro Takagi

IPC分类号： C07D40106

CPC分类号： C07D401/06 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/501 ,  C07D403/06 ,  C07D491/04 ,  C07D495/04

摘要： Using a compound selected from compounds represented by the following formula (1) (which include 3-phenyl-2-pyrazoline derivatives and 3-phenyl-tetrahydropyridazine derivatives) and pharmacologically acceptable salts thereof, an agent is provided which can activate glutamic acid transporter and which is useful for prevention and/treatment of cerebral ischemia (cerebral infarct and brain edema), amyotrophic lateral sclerosis (ALS), etc., all caused by glutamic acid toxicity.

摘要翻译： 使用选自由下式（1）表示的化合物（其包括3-苯基-2-吡唑啉衍生物和3-苯基 - 四氢哒嗪衍生物）的化合物及其药理学上可接受的盐，可以提供活化谷氨酸转运体和 可用于脑缺血（脑梗死和脑水肿），肌萎缩性侧索硬化（ALS）等的预防和治疗，均由谷氨酸毒性引起。

公开(公告)号：US5089622A

公开(公告)日：1992-02-18

申请号：US443577

申请日：1989-11-30

申请人： Seitaro Kajiya ,  Hajime Iizuka ,  Kunio Okumura ,  Junya Fujiwara ,  Norio Ohto ,  Hiroshi Kawazura ,  Yasuhiro Takahashi ,  Yoshio Shiga

发明人： Seitaro Kajiya ,  Hajime Iizuka ,  Kunio Okumura ,  Junya Fujiwara ,  Norio Ohto ,  Hiroshi Kawazura ,  Yasuhiro Takahashi ,  Yoshio Shiga

IPC分类号： C07D401/06

CPC分类号： C07D401/06

摘要： The present invention relates to a novel (-)-2-pyrazoline compound and therapeutic agents containing the same as an effective ingredient; furthermore, it relates to a method for optically resolving 1-(3-pyridylcarbonyl)-5-methyl-2-pyrazoline.

公开(公告)号：US5075449A

公开(公告)日：1991-12-24

申请号：US480852

申请日：1990-02-16

申请人： Seitaro Kajiya ,  Hajime Iizuka ,  Kunio Okumura ,  Junya Fujiwara ,  Norio Ohto ,  Hiroshi Kawazura ,  Yasuhiro Takahashi ,  Yoshio Shiga

发明人： Seitaro Kajiya ,  Hajime Iizuka ,  Kunio Okumura ,  Junya Fujiwara ,  Norio Ohto ,  Hiroshi Kawazura ,  Yasuhiro Takahashi ,  Yoshio Shiga

IPC分类号： C07D401/06

CPC分类号： C07D401/06

摘要： The present invention relates to a novel (-)-2-pyrazoline compound and therapeutic agents containing the same as an effective ingredient; furthermore, it relates to a method for optically resolving 1-(3-pyridylcarbonyl)-5-methyl-2-pyrazoline.

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：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.