公开(公告)号：US20080248485A1

公开(公告)日：2008-10-09

申请号：US10593034

申请日：2005-03-18

申请人： Keiko Shimamoto ,  Hideo Saji ,  Yuji Kuge ,  Masashi Ueda ,  Masamichi Satoh ,  Takayuki Nakagawa

发明人： Keiko Shimamoto ,  Hideo Saji ,  Yuji Kuge ,  Masashi Ueda ,  Masamichi Satoh ,  Takayuki Nakagawa

IPC分类号： C07C233/75 ,  G01N33/53

CPC分类号： C07B59/001

摘要： The present invention provides a radiolabeled ligand which is highly selective and potent for glutamate transporters and is usable in specifically detecting the glutamate transporter.Specifically, the present invention provides a 3-[3-(benzoylamido)benzyloxy]aspartic acid having a radioactive substituent on the benzoyl group which is represented by the following formula (1), or an ester or salt thereof: wherein X represents a substituent containing a radioactive atom(s) which is selected from a straight or branched lower aliphatic alkyl group, a hydroxyl group, a straight or branched lower aliphatic alkoxy group, an amino group, a straight or branched lower aliphatic acylamido group, a halogen atom and a straight or branched lower aliphatic haloalkyl group; and R1 and R2 each represents a hydrogen atom, a straight or branched lower aliphatic alkyl group or an acetoxymethyl group.

摘要翻译： 本发明提供了一种对谷氨酸转运蛋白具有高度选择性和有效的放射性标记配体，可用于特异性检测谷氨酸转运蛋白。 具体而言，本发明提供由下式（1）表示的苯甲酰基上具有放射性取代基的3- [3-（苯甲酰氨基）苄氧基]天冬氨酸或其酯或其盐：其中X表示取代基 含有选自直链或支链低级脂族烷基，羟基，直链或支链低级脂族烷氧基，氨基，直链或支链低级脂族酰氨基，卤素原子和 直链或支链低级脂族卤代烷基; R 1和R 2各自表示氢原子，直链或支链低级脂族烷基或乙酰氧基甲基。

公开(公告)号：US06344358B1

公开(公告)日：2002-02-05

申请号：US09321745

申请日：1999-05-28

申请人： Nobuya Matsuoka ,  Masamichi Satoh

发明人： Nobuya Matsuoka ,  Masamichi Satoh

IPC分类号： G01N3348

CPC分类号： G01N33/5058 ,  A61K31/00 ,  A61K31/445 ,  A61K31/4468 ,  A61K31/4545 ,  A61K31/495 ,  A61K31/496 ,  C07D211/58 ,  C07D211/96 ,  C07D213/81 ,  C07D295/185 ,  C07D295/192 ,  C07D295/205 ,  C07D295/26 ,  C07D401/12 ,  G01N33/5008 ,  G01N33/502 ,  G01N33/5088 ,  G01N2333/655

摘要： The present invention relates to an agent for the expression of long-term potentiation of synaptic transmission, which contains a compound having a brain somatostatin activation property as an active ingredient and to a screening method of an agent for the expression of long-term potentiation of synaptic transmission, which uses a soniatostatin releasing property as an index. The present invention is useful for the prophylaxis and/or treatment of cerebral diseases of dementia, amnesia, manic-depressive psychosis, schizophrenia, Parkinson's disease, psychosomatic disease and the like.

摘要翻译： 本发明涉及用于表达突变传播的长期增强作用的试剂，其包含具有作为活性成分的脑生长抑素活化性的化合物和用于表达长期增强作用的试剂的筛选方法 突触传递，使用超声抑素释放特性作为指标。 本发明可用于预防和/或治疗痴呆，遗忘症，躁狂抑郁精神病，精神分裂症，帕金森病，心身疾病等脑疾病。

公开(公告)号：US06613572B2

公开(公告)日：2003-09-02

申请号：US10041592

申请日：2002-01-10

申请人： Nobuya Matsuoka ,  Masamichi Satoh

发明人： Nobuya Matsuoka ,  Masamichi Satoh

IPC分类号： G01N3348

CPC分类号： G01N33/5058 ,  A61K31/00 ,  A61K31/445 ,  A61K31/4468 ,  A61K31/4545 ,  A61K31/495 ,  A61K31/496 ,  C07D211/58 ,  C07D211/96 ,  C07D213/81 ,  C07D295/185 ,  C07D295/192 ,  C07D295/205 ,  C07D295/26 ,  C07D401/12 ,  G01N33/5008 ,  G01N33/502 ,  G01N33/5088 ,  G01N2333/655

摘要： The present invention relates to an agent for the expression of long-term potentiation of synaptic transmission, which contains a compound having a brain somatostatin activation property as an active ingredient and to a screening method of an agent for the expression of long-term potentiation of synaptic transmission, which uses a somatostatin releasing property as an index. The present invention is useful for the prophylaxis and/or treatment of cerebral diseases of dementia, amnesia, manic-depressive psychosis, schizophrenia, Parkinson's disease, psychosomatic disease and the like.

摘要翻译： 本发明涉及用于表达突变传播的长期增强作用的试剂，其包含具有作为活性成分的脑生长抑素活化性的化合物和用于表达长期增强作用的试剂的筛选方法 突触传递，其使用生长抑素释放特性作为指标。 本发明可用于预防和/或治疗痴呆，遗忘症，躁狂抑郁精神病，精神分裂症，帕金森病，心身疾病等脑疾病。

公开(公告)号：US08097654B2

公开(公告)日：2012-01-17

申请号：US10593034

申请日：2005-03-18

申请人： Keiko Shimamoto ,  Hideo Saji ,  Yuji Kuge ,  Masashi Ueda ,  Masamichi Satoh ,  Takayuki Nakagawa

发明人： Keiko Shimamoto ,  Hideo Saji ,  Yuji Kuge ,  Masashi Ueda ,  Masamichi Satoh ,  Takayuki Nakagawa

IPC分类号： A61K31/166 ,  A61K31/167 ,  C07C237/40

CPC分类号： C07B59/001

摘要： The present invention provides a radiolabeled ligand which is highly selective and potent for glutamate transporters and is usable in specifically detecting the glutamate transporter.Specifically, the present invention provides a 3-[3-(benzoylamido)benzyloxy]aspartic acid having a radioactive substituent on the benzoyl group which is represented by the following formula (1), or an ester or salt thereof: wherein X represents a substituent containing a radioactive atom(s) which is selected from a straight or branched lower aliphatic alkyl group, a hydroxyl group, a straight or branched lower aliphatic alkoxy group, an amino group, a straight or branched lower aliphatic acylamido group, a halogen atom and a straight or branched lower aliphatic haloalkyl group; and R1 and R2 each represents a hydrogen atom, a straight or branched lower aliphatic alkyl group or an acetoxymethyl group.

摘要翻译： 本发明提供了一种对谷氨酸转运蛋白具有高度选择性和有效的放射性标记配体，可用于特异性检测谷氨酸转运蛋白。 具体而言，本发明提供由下式（1）表示的苯甲酰基上具有放射性取代基的3- [3-（苯甲酰氨基）苄氧基]天冬氨酸或其酯或其盐：其中X表示取代基 含有选自直链或支链低级脂族烷基，羟基，直链或支链低级脂族烷氧基，氨基，直链或支链低级脂族酰氨基，卤素原子和 直链或支链低级脂族卤代烷基; R 1和R 2各自表示氢原子，直链或支链低级脂族烷基或乙酰氧基甲基。