公开(公告)号：US06642264B1

公开(公告)日：2003-11-04

申请号：US09958174

申请日：2001-10-05

申请人： Satoshi Hayashibe ,  Hirotsune Itahana ,  Masamichi Okada ,  Atsuyuki Kohara ,  Kyoichi Maeno ,  Kiyoshi Yahiro ,  Itsuro Shimada ,  Kazuhito Tanabe ,  Kenji Negoro ,  Takashi Kamikubo ,  Shuichi Sakamoto

发明人： Satoshi Hayashibe ,  Hirotsune Itahana ,  Masamichi Okada ,  Atsuyuki Kohara ,  Kyoichi Maeno ,  Kiyoshi Yahiro ,  Itsuro Shimada ,  Kazuhito Tanabe ,  Kenji Negoro ,  Takashi Kamikubo ,  Shuichi Sakamoto

IPC分类号： A61K31425

CPC分类号： C07D513/04 ,  A61K31/429

摘要： This invention relates to novel thiazolo[3,2-a]benzoimidazole derivatives represented by the following general formula (I). The compounds provided by the invention act specifically on metabotropic glutamate receptors and are used as medicaments. The invention also provides novel compounds useful as intermediates for the synthesis of the compounds of the invention. (Symbols in the formula represent the following meanings. R1: carbamoyl, carbonyl, oxy, amino, carbonylamino or the like which may be substituted; R2: hydrogen, lower alkyl or the like; and R3, R4 and R5: hydrogen, lower alkyl and the like which may be the same or different from one another.)

摘要翻译： 本发明涉及由以下通式（I）表示的新型噻唑并[3,2-a]苯并咪唑衍生物。 本发明提供的化合物特异性地代表代谢型谷氨酸受体并用作药物。 本发明还提供了可用作合成本发明化合物的中间体的新化合物（式中的符号表示以下含义：R 1：可以被取代的氨基甲酰基，羰基，氧基，氨基，羰基氨基等 R 2：氢，低级烷基等; R 3，R 4和R 5：氢，低级烷基等可以彼此相同或不同。）

公开(公告)号：US07084164B2

公开(公告)日：2006-08-01

申请号：US11232011

申请日：2005-09-22

申请人： Takahiko Tobe ,  Takashi Sugane ,  Wataru Hamaguchi ,  Itsuro Shimada ,  Kyoichi Maeno ,  Junji Miyata ,  Tetsuya Kimizuka ,  Takeshi Suzuki ,  Atsuyuki Kohara ,  Takuma Morita ,  Michael Arlt ,  Hartmut Greiner

发明人： Takahiko Tobe ,  Takashi Sugane ,  Wataru Hamaguchi ,  Itsuro Shimada ,  Kyoichi Maeno ,  Junji Miyata ,  Tetsuya Kimizuka ,  Takeshi Suzuki ,  Atsuyuki Kohara ,  Takuma Morita ,  Michael Arlt ,  Hartmut Greiner

IPC分类号： A61K31/41 ,  C07D249/08

CPC分类号： C07D249/08 ,  A61K31/41 ,  A61K31/4155 ,  A61K31/416 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/517 ,  A61K31/5377 ,  C07D249/10 ,  C07D249/12 ,  C07D249/14 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D405/04 ,  C07D405/06 ,  C07D405/10 ,  C07D405/12 ,  C07D405/14 ,  C07D409/10 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/10 ,  C07D495/04

摘要： The invention relates to a triazole derivative with an activity inhibiting glycine transporter and for use as a pharmaceutical drug, and a novel triazole derivative. The inventive triazole derivative has an excellent activity inhibiting glycine transporter and is useful as a therapeutic agent of dementia, schizophrenia, cognitive disorders, or cognitive disorders involved in various diseases such as Alzheimer disease, Parkinson's disease, or Huntington disease or the like, or spasm involved in diseases such as nerve degenerative diseases and cerebrovascular disorders, or the like. Particularly, the pharmaceutical drug is useful for the amelioration of learning disability of dementia and the like.

公开(公告)号：US5834460A

公开(公告)日：1998-11-10

申请号：US535047

申请日：1995-10-12

申请人： Ichio Noda ,  Masahiro Iwata ,  Shuichi Sakamoto ,  Kazuo Koshiya ,  Takuma Morita ,  Atsuyuki Kohara

发明人： Ichio Noda ,  Masahiro Iwata ,  Shuichi Sakamoto ,  Kazuo Koshiya ,  Takuma Morita ,  Atsuyuki Kohara

IPC分类号： C07D307/52 ,  C07D307/54 ,  C07D333/20 ,  C07D333/24 ,  C07D409/06 ,  A61K31/445 ,  A61K31/55 ,  C07D407/06 ,  C07D409/04

CPC分类号： C07D409/06 ,  C07D307/52 ,  C07D307/54 ,  C07D333/20 ,  C07D333/24 ,  Y02P20/55

摘要： A serine derivative represented by the general formula (I) ##STR1## (symbols in the formula represent the following meanings; X: a sulfur atom or an oxygen atom, Y: a nitrogen atom or CH, R.sup.1 and R.sup.2 : the same or different from each other and each represents a hydrogen atom, a lower alkyl group or a protecting group for the amino group, or R.sup.1 and R.sup.2 may be combined together to form a four- to nine-membered nitrogen-containing cycloalkyl group, R.sup.3 : a hydrogen atom, a carboxyl group, a protected carboxyl group, an aralkyl group, or a lower alkyl group unsubstituted or substituted with a hydroxyl group, R.sup.4 : a hydrogen atom or a hydroxyl group, R.sup.5 : a hydrogen atom or a lower alkyl group, A: a lower alkylene group, B: 1) a saturated or unsaturated four- to ten-membered nitrogen-containing cycloalkyl group unsubstituted or substituted with a lower alkyl group or an aralkyl group or 2) a bicyclic nitrogen-containing hydrocarbon ring radical resulting from the condensation of a four- to eight-membered nitrogen-containing cycloalkyl group with a benzene ring, and . . : a single or double bond) or a pharmaceutically acceptable salt thereof, which has an anti-PCP (phencyclidine) action and is useful as a psychotropic drug.

摘要翻译： PCT No.PCT / JP94 / 00697 Sec。 371 1995年10月12日第 102（e）日期1995年10月12日PCT 1994年4月26日PCT PCT。 第WO94 / 25450号公报 日期：1994年11月10日由通式（I）表示的丝氨酸衍生物（I）（式中的符号表示以下含义：X：硫原子或氧原子，Y：氮原子或CH， R1和R2彼此相同或不同，并且各自表示氢原子，氨基的低级烷基或保护基，或者R1和R2可以组合在一起形成四至九元的氮 - 含有环烷基，R3：氢原子，羧基，被保护的羧基，芳烷基或未取代或被羟基取代的低级烷基，R4表示氢原子或羟基，R5表示氢 原子或低级烷基，A：低级亚烷基，B：1）未被取代或被低级烷基或芳烷基取代的饱和或不饱和的四至十元含氮环烷基，或2）双环 由缩合产生的含氮烃环基团o f为具有苯环的四至八元含氮环烷基，和+ E， 。 + EE：单键或双键）或其药学上可接受的盐，其具有抗PCP（苯环利定）作用并且可用作精神药物。

公开(公告)号：US07034047B2

公开(公告)日：2006-04-25

申请号：US10848386

申请日：2004-05-19

申请人： Takahiko Tobe ,  Takashi Sugane ,  Wataru Hamaguchi ,  Itsuro Shimada ,  Kyoichi Maeno ,  Junji Miyata ,  Tetsuya Kimizuka ,  Takeshi Suzuki ,  Atsuyuki Kohara ,  Takuma Morita ,  Michael Arlt ,  Hartmut Greiner

发明人： Takahiko Tobe ,  Takashi Sugane ,  Wataru Hamaguchi ,  Itsuro Shimada ,  Kyoichi Maeno ,  Junji Miyata ,  Tetsuya Kimizuka ,  Takeshi Suzuki ,  Atsuyuki Kohara ,  Takuma Morita ,  Michael Arlt ,  Hartmut Greiner

IPC分类号： C07D239/08 ,  A61K31/4196

CPC分类号： C07D249/08 ,  A61K31/41 ,  A61K31/4155 ,  A61K31/416 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/517 ,  A61K31/5377 ,  C07D249/10 ,  C07D249/12 ,  C07D249/14 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D405/04 ,  C07D405/06 ,  C07D405/10 ,  C07D405/12 ,  C07D405/14 ,  C07D409/10 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/10 ,  C07D495/04

摘要： The invention relates to a triazole derivative with an activity inhibiting glycine transporter and for use as a pharmaceutical drug, and a novel triazole derivative. The inventive triazole derivative has an excellent activity inhibiting glycine transporter and is useful as a therapeutic agent of dementia, schizophrenia, cognitive disorders, or cognitive disorders involved in various diseases such as Alzheimer disease, Parkinson's disease, or Huntington disease or the like, or spasm involved in diseases such as nerve degenerative diseases and cerebrovascular disorders, or the like. Particularly, the pharmaceutical drug is useful for the amelioration of learning disability of dementia and the like.

摘要翻译： 本发明涉及具有活性抑制甘氨酸转运体并用作药物的三唑衍生物和新的三唑衍生物。 本发明的三唑衍生物具有优异的抑制甘氨酸转运蛋白的活性，可用作痴呆，精神分裂症，认知障碍或参与各种疾病如阿尔茨海默病，帕金森病或亨廷顿病等的认知障碍或痉挛的治疗剂 涉及诸如神经退行性疾病和脑血管障碍等疾病。 特别地，药物对于改善痴呆等的学习障碍是有用的。

公开(公告)号：US20060025461A1

公开(公告)日：2006-02-02

申请号：US11232011

申请日：2005-09-22

申请人： Takahiko Tobe ,  Takashi Sugane ,  Wataru Hamaguchi ,  Itsuro Shimada ,  Kyoichi Maeno ,  Junji Miyata ,  Tetsuya Kimizuka ,  Takeshi Suzuki ,  Atsuyuki Kohara ,  Takuma Morita ,  Michael Arlt ,  Hartmut Greiner

发明人： Takahiko Tobe ,  Takashi Sugane ,  Wataru Hamaguchi ,  Itsuro Shimada ,  Kyoichi Maeno ,  Junji Miyata ,  Tetsuya Kimizuka ,  Takeshi Suzuki ,  Atsuyuki Kohara ,  Takuma Morita ,  Michael Arlt ,  Hartmut Greiner

IPC分类号： A61K31/4196 ,  C07D403/02

CPC分类号： C07D249/08 ,  A61K31/41 ,  A61K31/4155 ,  A61K31/416 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/517 ,  A61K31/5377 ,  C07D249/10 ,  C07D249/12 ,  C07D249/14 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D405/04 ,  C07D405/06 ,  C07D405/10 ,  C07D405/12 ,  C07D405/14 ,  C07D409/10 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/10 ,  C07D495/04

摘要： The invention relates to a triazole derivative with an activity inhibiting glycine transporter and for use as a pharmaceutical drug, and a novel triazole derivative. The inventive triazole derivative has an excellent activity inhibiting glycine transporter and is useful as a therapeutic agent of dementia, schizophrenia, cognitive disorders, or cognitive disorders involved in various diseases such as Alzheimer disease, Parkinson's disease, or Huntington disease or the like, or spasm involved in diseases such as nerve degenerative diseases and cerebrovascular disorders, or the like. Particularly, the pharmaceutical drug is useful for the amelioration of learning disability of dementia and the like.