公开(公告)号：US20120010414A1

公开(公告)日：2012-01-12

申请号：US13257258

申请日：2010-03-19

申请人： Akito Yasuhara ,  Shuji Yamamoto ,  Hiroshi Ohta ,  Yoshihisa Shirasaki ,  Kazunari Sakagami ,  Masato Hayashi ,  Tsuyoshi Shibata ,  Youichi Shimazaki ,  Yuko Araki ,  Kumi Abe ,  Xiang-Min Sun

发明人： Akito Yasuhara ,  Shuji Yamamoto ,  Hiroshi Ohta ,  Yoshihisa Shirasaki ,  Kazunari Sakagami ,  Masato Hayashi ,  Tsuyoshi Shibata ,  Youichi Shimazaki ,  Yuko Araki ,  Kumi Abe ,  Xiang-Min Sun

IPC分类号： C07D471/04 ,  C07D405/12 ,  C07D409/12 ,  C07D405/14

CPC分类号： C07D471/04 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12

摘要： The present invention aims to provide novel compounds of formula [I] or pharmaceutically acceptable salts thereof that are based on a glycine uptake inhibiting action and which are useful in the prevention or treatment of such diseases as schizophrenia, Alzheimer's disease, cognitive dysfunction, dementia, anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsory disorder, social anxiety disorder, posttraumatic stress disorder, specific phobia, acute stress disorder, etc.), depression, drug addiction, spasm, tremor, and sleep disorder:

摘要翻译： 本发明旨在提供基于甘氨酸摄取抑制作用的新颖的式[I]化合物或其药学上可接受的盐，其可用于预防或治疗精神分裂症，阿尔茨海默病，认知功能障碍，痴呆， 焦虑症（广泛性焦虑障碍，恐慌症，强迫症，社会焦虑症，创伤后应激障碍，特定恐惧症，急性应激障碍等），抑郁症，药物成瘾，痉挛，震颤和睡眠障碍：

公开(公告)号：US08623898B2

公开(公告)日：2014-01-07

申请号：US13257258

申请日：2010-03-19

申请人： Akito Yasuhara ,  Shuji Yamamoto ,  Hiroshi Ohta ,  Yoshihisa Shirasaki ,  Kazunari Sakagami ,  Masato Hayashi ,  Tsuyoshi Shibata ,  Youichi Shimazaki ,  Yuko Araki ,  Kumi Abe ,  Xiang-Min Sun

发明人： Akito Yasuhara ,  Shuji Yamamoto ,  Hiroshi Ohta ,  Yoshihisa Shirasaki ,  Kazunari Sakagami ,  Masato Hayashi ,  Tsuyoshi Shibata ,  Youichi Shimazaki ,  Yuko Araki ,  Kumi Abe ,  Xiang-Min Sun

IPC分类号： C07D471/04 ,  C07D405/12 ,  C07D409/12 ,  C07D405/14 ,  A01N43/64 ,  A01N43/50 ,  A61K31/41

CPC分类号： C07D471/04 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12

摘要： The present invention aims to provide novel compounds of formula [I] or pharmaceutically acceptable salts thereof that are based on a glycine uptake inhibiting action and which are useful in the prevention or treatment of such diseases as schizophrenia, Alzheimer's disease, cognitive dysfunction, dementia, anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsory disorder, social anxiety disorder, posttraumatic stress disorder, specific phobia, acute stress disorder, etc.), depression, drug addiction, spasm, tremor, and sleep disorder:

摘要翻译： 本发明旨在提供基于甘氨酸摄取抑制作用的新颖的式[I]化合物或其药学上可接受的盐，其可用于预防或治疗精神分裂症，阿尔茨海默病，认知功能障碍，痴呆， 焦虑症（广泛性焦虑障碍，恐慌症，强迫症，社会焦虑症，创伤后应激障碍，特定恐惧症，急性应激障碍等），抑郁症，药物成瘾，痉挛，震颤和睡眠障碍：

公开(公告)号：US20120116095A1

公开(公告)日：2012-05-10

申请号：US13383513

申请日：2010-07-15

申请人： Akito Yasuhara ,  Kazunari Sakagami ,  Hiroshi Ohta ,  Masato Hayashi ,  Yoshihisa Shirasaki ,  Shuji Yamamoto ,  Youichi Shimazaki ,  Yuko Araki ,  Kumi Abe ,  Xiang-Min Sun

发明人： Akito Yasuhara ,  Kazunari Sakagami ,  Hiroshi Ohta ,  Masato Hayashi ,  Yoshihisa Shirasaki ,  Shuji Yamamoto ,  Youichi Shimazaki ,  Yuko Araki ,  Kumi Abe ,  Xiang-Min Sun

IPC分类号： C07D249/12 ,  C07D233/14

CPC分类号： C07D249/10

摘要： The present invention aims to provide novel compounds represented by formula [I] or pharmaceutically acceptable salts thereof: which are useful for prevention or treatment of diseases such as schizophrenia, Alzheimer's disease, cognitive impairment, dementia, anxiety disorders (e.g., generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, post-traumatic stress disorder, specific phobias, acute stress disorder), depression, drug dependence, convulsion, tremor, pain, or sleep disorders, based on their inhibitory effect against glycine uptake.

摘要翻译： 本发明旨在提供由式[I]表示的新化合物或其药学上可接受的盐：其可用于预防或治疗诸如精神分裂症，阿尔茨海默病，认知障碍，痴呆，焦虑症（例如广泛性焦虑症， 基于它们对甘氨酸摄取的抑制效果，恐慌症，强迫症，社交焦虑症，创伤后应激障碍，特异性恐惧症，急性应激障碍），抑郁症，药物依赖性，惊厥，震颤，疼痛或睡眠障碍。

公开(公告)号：US08729271B2

公开(公告)日：2014-05-20

申请号：US13823574

申请日：2011-09-16

申请人： Minoru Moriya ,  Akito Yasuhara ,  Kazunari Sakagami ,  Hiroshi Ohta ,  Kumi Abe ,  Shuji Yamamoto ,  Yuko Araki ,  Hiroki Urabe ,  Xiang-Min Sun

发明人： Minoru Moriya ,  Akito Yasuhara ,  Kazunari Sakagami ,  Hiroshi Ohta ,  Kumi Abe ,  Shuji Yamamoto ,  Yuko Araki ,  Hiroki Urabe ,  Xiang-Min Sun

IPC分类号： A01N43/40 ,  A61K31/44 ,  A01N43/64 ,  A61K31/41 ,  C07D213/00 ,  C07D401/00 ,  C07D419/00

CPC分类号： C07D405/14 ,  C07D233/90 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

摘要： The present invention aims to provide novel compounds of formula [I] or pharmaceutically acceptable salts thereof that are based on a glycine uptake inhibiting action and which are useful in the prevention or treatment of such diseases as schizophrenia, Alzheimer's disease, cognitive dysfunction, dementia, anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, posttraumatic stress disorder, specific phobia, acute stress disorder, etc.), depression, drug addiction, spasm, tremor, pain, and sleep disorder:

摘要翻译： 本发明旨在提供基于甘氨酸摄取抑制作用的新颖的式[I]化合物或其药学上可接受的盐，其可用于预防或治疗精神分裂症，阿尔茨海默病，认知功能障碍，痴呆， 焦虑障碍（广泛性焦虑症，惊恐障碍，强迫症，社会焦虑症，创伤后应激障碍，特定恐惧症，急性应激障碍等），抑郁症，药物成瘾，痉挛，震颤，疼痛和睡眠障碍：

公开(公告)号：US20130184460A1

公开(公告)日：2013-07-18

申请号：US13823574

申请日：2011-09-16

申请人： Minoru Moriya ,  Akito Yasuhara ,  Kazunari Sakagami ,  Hiroshi Ohta ,  Kumi Abe ,  Shuji Yamamoto ,  Yuko Araki ,  Hiroki Urabe ,  Xiang-Min Sun

发明人： Minoru Moriya ,  Akito Yasuhara ,  Kazunari Sakagami ,  Hiroshi Ohta ,  Kumi Abe ,  Shuji Yamamoto ,  Yuko Araki ,  Hiroki Urabe ,  Xiang-Min Sun

IPC分类号： C07D405/14 ,  C07D403/12 ,  C07D401/12

CPC分类号： C07D405/14 ,  C07D233/90 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

摘要： The present invention aims to provide novel compounds of formula [I] or pharmaceutically acceptable salts thereof that are based on a glycine uptake inhibiting action and which are useful in the prevention or treatment of such diseases as schizophrenia, Alzheimer's disease, cognitive dysfunction, dementia, anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, posttraumatic stress disorder, specific phobia, acute stress disorder, etc.), depression, drug addiction, spasm, tremor, pain, and sleep disorder:

摘要翻译： 本发明旨在提供基于甘氨酸摄取抑制作用的新颖的式[I]化合物或其药学上可接受的盐，其可用于预防或治疗精神分裂症，阿尔茨海默病，认知功能障碍，痴呆， 焦虑障碍（广泛性焦虑症，惊恐障碍，强迫症，社会焦虑症，创伤后应激障碍，特定恐惧症，急性应激障碍等），抑郁症，药物成瘾，痉挛，震颤，疼痛和睡眠障碍：

公开(公告)号：US08642626B2

公开(公告)日：2014-02-04

申请号：US13812437

申请日：2011-07-29

申请人： Toshio Nakamura ,  Kazunari Sakagami ,  Kazuhide Konishi ,  Kanako Yamamoto ,  Seiji Masuda ,  Yohei Matsuda ,  Kumiko Okada ,  Tsuyoshi Shibata ,  Hiroshi Ohta ,  Akito Yasuhara ,  Hiroshi Kawamoto

发明人： Toshio Nakamura ,  Kazunari Sakagami ,  Kazuhide Konishi ,  Kanako Yamamoto ,  Seiji Masuda ,  Yohei Matsuda ,  Kumiko Okada ,  Tsuyoshi Shibata ,  Hiroshi Ohta ,  Akito Yasuhara ,  Hiroshi Kawamoto

IPC分类号： A61K31/4439 ,  A61K31/415 ,  C07D231/12 ,  C07D231/20 ,  C07D231/38 ,  C07D403/06 ,  C07D401/06

CPC分类号： C07D231/12 ,  C07D231/14 ,  C07D231/20 ,  C07D231/38 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D403/04 ,  C07D403/06 ,  C07D413/04

摘要： Provided is a novel compound represented by formula [I] or a pharmaceutically acceptable salt thereof having antagonistic activity against group II metabolism-type glutamic acid (m-Glu) receptors. The compound or pharmaceutically acceptable salt thereof is useful as a prophylactic or therapeutic agent for diseases such as new mood disorders (depressive and bipolar disorders), anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, post-traumatic stress disorder, specific phobias, and acute stress disorder), schizophrenia, Alzheimer's disease, cognitive dysfunction, dementia, drug dependence, convulsions, tremors, pain, sleep disorders, and the like.

摘要翻译： 本发明提供由式[I]表示的新化合物或其对II类代谢型谷氨酸（m-Glu）受体具有拮抗作用的药学上可接受的盐。 化合物或其药学上可接受的盐可用作疾病的预防或治疗剂，例如新的情绪障碍（抑郁和双相性精神障碍），焦虑症（广泛性焦虑症，惊恐障碍，强迫症，社会焦虑症， 创伤性应激障碍，特异性恐惧症和急性应激障碍），精神分裂症，阿尔茨海默病，认知功能障碍，痴呆，药物依赖，惊厥，震颤，疼痛，睡眠障碍等。

公开(公告)号：US20130137865A1

公开(公告)日：2013-05-30

申请号：US13814869

申请日：2011-08-11

申请人： Toshio Nakamura ,  Kazunari Sakagami ,  Kazuhide Konishi ,  Kanako Yamamoto ,  Seiji Masuda ,  Yohei Matsuda ,  Kumiko Okada ,  Tsuyoshi Shibata ,  Hiroshi Ohta ,  Akito Yasuhara ,  Hiroshi Kawamoto ,  Hideaki Amada ,  Hiroki Urabe ,  Rie Nishikawa ,  Shuhei Kashiwa ASHIWA

发明人： Toshio Nakamura ,  Kazunari Sakagami ,  Kazuhide Konishi ,  Kanako Yamamoto ,  Seiji Masuda ,  Yohei Matsuda ,  Kumiko Okada ,  Tsuyoshi Shibata ,  Hiroshi Ohta ,  Akito Yasuhara ,  Hiroshi Kawamoto ,  Hideaki Amada ,  Hiroki Urabe ,  Rie Nishikawa ,  Shuhei Kashiwa ASHIWA

IPC分类号： C07D413/14 ,  C07D413/04 ,  C07D403/04 ,  C07D231/38

CPC分类号： C07D413/14 ,  C07D231/38 ,  C07D403/04 ,  C07D403/14 ,  C07D413/04

摘要： A compound represented by formula [I] and a pharmaceutically accepted salt of said compound are a novel compound and a pharmaceutically accepted salt thereof which exert antagonistic activity against group II metabotropic glutamate (mGlu) receptors, and are effective as a novel preventive or therapeutic agent for disorders such as mood disorders (depressive disorder, bipolar disorder, etc.), anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, posttraumatic stress disorder, a specific phobic disorder, acute stress disorder, etc.), schizophrenia, Alzheimer's disease, cognitive impairment, dementia, drug dependence, convulsions, shivering, pain, sleep disorders, and the like.

摘要翻译： 由式[I]表示的化合物和所述化合物的药学上可接受的盐是对II族代谢型谷氨酸（mGlu）受体具有拮抗作用的新化合物及其药学上可接受的盐，并且作为新的预防或治疗剂是有效的 用于诸如情绪障碍（抑郁障碍，双相情感障碍等），焦虑障碍（广泛性焦虑症，恐慌症，强迫症，社会焦虑症，创伤后应激障碍，特异性恐怖症，急性应激障碍等） ，精神分裂症，阿尔茨海默病，认知障碍，痴呆，药物依赖，抽搐，发抖，疼痛，睡眠障碍等。

公开(公告)号：US20130123500A1

公开(公告)日：2013-05-16

申请号：US13812437

申请日：2011-07-29

申请人： Toshio Nakamura ,  Kazunari Sakagami ,  Kazuhide Konishi ,  Kanako Yamamoto ,  Seiji Masuda ,  Yohei Matsuda ,  Kumiko Okada ,  Tsuyoshi Shibata ,  Hiroshi Ohta ,  Akito Yasuhara ,  Hiroshi Kawamoto

发明人： Toshio Nakamura ,  Kazunari Sakagami ,  Kazuhide Konishi ,  Kanako Yamamoto ,  Seiji Masuda ,  Yohei Matsuda ,  Kumiko Okada ,  Tsuyoshi Shibata ,  Hiroshi Ohta ,  Akito Yasuhara ,  Hiroshi Kawamoto

IPC分类号： C07D231/12 ,  C07D231/20 ,  C07D231/38 ,  C07D403/06 ,  C07D401/06

CPC分类号： C07D231/12 ,  C07D231/14 ,  C07D231/20 ,  C07D231/38 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D403/04 ,  C07D403/06 ,  C07D413/04

摘要： Provided is a novel compound represented by formula [I] or a pharmaceutically acceptable salt thereof having antagonistic activity against group II metabolism-type glutamic acid (m-Glu) receptors. The compound or pharmaceutically acceptable salt thereof is useful as a prophylactic or therapeutic agent for diseases such as new mood disorders (depressive and bipolar disorders), anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, post-traumatic stress disorder, specific phobias, and acute stress disorder), schizophrenia, Alzheimer's disease, cognitive dysfunction, dementia, drug dependence, convulsions, tremors, pain, sleep disorders, and the like.

摘要翻译： 本发明提供由式[I]表示的新化合物或其对II类代谢型谷氨酸（m-Glu）受体具有拮抗作用的药学上可接受的盐。 化合物或其药学上可接受的盐可用作疾病的预防或治疗剂，例如新的情绪障碍（抑郁和双相性精神障碍），焦虑症（广泛性焦虑症，惊恐障碍，强迫症，社会焦虑症， 创伤性应激障碍，特异性恐惧症和急性应激障碍），精神分裂症，阿尔茨海默病，认知功能障碍，痴呆，药物依赖，惊厥，震颤，疼痛，睡眠障碍等。

公开(公告)号：US20120028982A1

公开(公告)日：2012-02-02

申请号：US13269242

申请日：2011-10-07

申请人： Akito YASUHARA ,  Kazunari Sakagami ,  Hiroshi Ohta ,  Atsuro Nakazato

发明人： Akito YASUHARA ,  Kazunari Sakagami ,  Hiroshi Ohta ,  Atsuro Nakazato

IPC分类号： A61K31/5375 ,  C07C229/46 ,  C07D265/30 ,  C07C261/00 ,  A61K31/27 ,  A61K31/215

CPC分类号： C07C229/50 ,  C07D307/88

摘要： A drug effective for the treatment and prevention of psychiatric disorders such as schizophrenia, anxiety and related ailments thereof, depression, bipolar disorder and epilepsy. The drug antagonizes the action of group II metabotropic glutamate receptors and shows high activity in oral administration. A 2-amino-bicyclo[3.1.0]hexane-2,6-dicarboxylic ester derivative represented by formula [I] [wherein R1 and R2 are identical or different, and each represents a hydrogen atom, a C1-10alkyl group or the like; X represents a hydrogen atom or a fluorine atom; Y represents —OCHR3R4 or the like (wherein R3 and R4 are identical or different, and each represents a hydrogen atom, a C1-10alkyl group or the like; and n represents integer 1 or 2)], a pharmaceutically acceptable salt thereof or a hydrate thereof.

摘要翻译： 一种有效治疗和预防精神疾病如精神分裂症，焦虑及其相关疾病，抑郁症，双相情感障碍和癫痫的药物。 该药物拮抗II型代谢型谷氨酸受体的作用，并且在口服给药中显示高活性。 由式[I]表示的2-氨基 - 双环[3.1.0]己烷-2,6-二羧酸酯衍生物[其中R 1和R 2相同或不同，各自表示氢原子，C 1-10烷基或 喜欢; X表示氢原子或氟原子; Y表示-OCHR 3 R 4等（其中R 3和R 4相同或不同，并且各自表示氢原子，C 1-10烷基等; n表示1或2的整数）]，其药学上可接受的盐或 水合物。

公开(公告)号：US20100298561A1

公开(公告)日：2010-11-25

申请号：US12847392

申请日：2010-07-30

申请人： Akito YASUHARA ,  Kazunari Sakagami ,  Hiroshi Ohta ,  Atsuro Nakazato

发明人： Akito YASUHARA ,  Kazunari Sakagami ,  Hiroshi Ohta ,  Atsuro Nakazato

IPC分类号： C07C69/757 ,  C07C321/22 ,  C07D295/088 ,  C07C69/96 ,  C07D317/24 ,  C07D307/88

CPC分类号： C07C229/50 ,  C07D307/88

摘要： A drug effective for the treatment and prevention of psychiatric disorders such as schizophrenia, anxiety and related ailments thereof, depression, bipolar disorder and epilepsy. The drug antagonizes the action of group II metabotropic glutamate receptors and shows high activity in oral administration A 2-amino-bicyclo[3.1.0]hexane-2,6-dicarboxylic ester derivative represented by formula [I] [wherein R1 and R2 are identical or different, and each represents a hydrogen atom, a C1-10alkyl group or the like; X represents a hydrogen atom or a fluorine atom; Y represents —OCHR3R4 or the like (wherein R3 and R4 are identical or different, and each represents a hydrogen atom, a C1-10alkyl group or the like; and n represents integer 1 or 2)], a pharmaceutically acceptable salt thereof or a hydrate thereof.

摘要翻译： 一种有效治疗和预防精神疾病如精神分裂症，焦虑及其相关疾病，抑郁症，双相情感障碍和癫痫的药物。 该药物拮抗II型代谢型谷氨酸受体的作用，并且在口服给药中表现出高活性。由式[I]表示的2-氨基 - 双环[3.1.0]己烷-2,6-二羧酸酯衍生物[其中R1和R2为 相同或不同，并且各自表示氢原子，C 1-10烷基等; X表示氢原子或氟原子; Y表示-OCHR 3 R 4等（其中R 3和R 4相同或不同，各自表示氢原子，C 1-10烷基等; n表示1或2的整数）]，其药学上可接受的盐或 水合物。