公开(公告)号：EP2409976A1

公开(公告)日：2012-01-25

申请号：EP10753606.2

申请日：2010-03-19

申请人： Taisho Pharmaceutical Co., Ltd.

发明人： YASUHARA, Akito ,  YAMAMOTO, Shuji ,  OHTA, Hiroshi ,  SHIRASAKI, Yoshihisa ,  SAKAGAMI, Kazunari ,  HAYASHI, Masato ,  SHIBATA, Tsuyoshi ,  SHIMAZAKI, Youichi ,  ARAKI, Yuko ,  ABE, Kumi ,  SUN, Xiang-Min

IPC分类号： C07D405/12 ,  A61K31/4178 ,  A61K31/4196 ,  A61K31/437 ,  A61K31/4439 ,  A61P25/08 ,  A61P25/14 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P43/00 ,  C07D405/14 ,  C07D409/12 ,  C07D471/04

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并可用于预防或治疗诸如精神分裂症，阿尔茨海默氏病，认知功能障碍，痴呆等的疾病的新型式[I]化合物或其药学上可接受的盐。 焦虑症（广泛性焦虑症，恐慌症，强迫症，社交焦虑症，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：EP1637517B1

公开(公告)日：2010-11-10

申请号：EP04746867.3

申请日：2004-06-25

申请人： Taisho Pharmaceutical Co., Ltd.

发明人： YASUHARA, Akito ,  SAKAGAMI, Kazunari ,  OHTA, Hiroshi ,  NAKAZATO, Atsuro

IPC分类号： C07C229/50 ,  C07C235/06 ,  C07C247/04 ,  C07C323/61 ,  A61K31/216 ,  A61K31/365 ,  A61K31/357 ,  C07D307/88 ,  C07D317/34 ,  A61P9/10 ,  A61P25/00 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/28 ,  A61P25/30 ,  A61P43/00

CPC分类号： C07C229/50 ,  C07D307/88

摘要： A drug which is effective in treatments for and prevention of schizophrenia, anxiety, and diseases related to these, i.e., psychiatrical disorders such as depression, bipolar disorder, and epilepsy. The drug has high activity in oral administration and has an antagonistic effect on a Group II metabotropic glutamate receptor. It is a 2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic ester derivative represented by the formula [I]: [I] [wherein R1 and R2 are the same or different and each represents hydrogen, C1-10 alkyl, etc.; X represents hydrogen or fluorine; and Y represents, e.g., -OCHR3R4 (wherein R3 and R4 are the same or different and each represents hydrogen, C1-10 alkyl, etc. and n is an integer of 1 or 2)], a pharmaceutically acceptable salt of the derivative, or a hydrate of either.

摘要翻译： 对治疗和预防精神分裂症，焦虑症和与这些有关的疾病，即抑郁症，双相性精神障碍和癫痫等精神病症有效的药物。 该药在口服给药中具有高活性，并对II组代谢型谷氨酸受体具有拮抗作用。 它是由式[I]表示的2-氨基二环[3.1.0]己烷-2,6-二羧酸酯衍生物：[I] [其中R1和R2相同或不同，各代表氢，C1-10烷基 等; X代表氢或氟; Y表示例如-OCHR 3 R 4（其中R 3和R 4相同或不同，并且各自表示氢，C 1-10烷基等，并且n是1或2的整数）]，衍生物的药学上可接受的盐， 或任一种的水合物。

公开(公告)号：EP2617715A1

公开(公告)日：2013-07-24

申请号：EP11825276.6

申请日：2011-09-16

申请人： TAISHO PHARMACEUTICAL CO., LTD

发明人： MORIYA, Minoru ,  YASUHARA, Akito ,  SAKAGAMI, Kazunari ,  OHTA, Hiroshi ,  ABE, Kumi ,  YAMAMOTO, Shuji ,  ARAKI, Yuko ,  URABE, Hiroki ,  SUN, Xiang-Min

IPC分类号： C07D233/90 ,  A61K31/4178 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5377 ,  A61P25/04 ,  A61P25/08 ,  A61P25/14 ,  A61P25/18

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并可用于预防或治疗诸如精神分裂症，阿尔茨海默氏病，认知功能障碍，痴呆等的疾病的新型式[I]化合物或其药学上可接受的盐。 焦虑症（广泛性焦虑症，恐慌症，强迫症，社交焦虑症，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：EP2454240A1

公开(公告)日：2012-05-23

申请号：EP10799955.9

申请日：2010-07-15

申请人： Taisho Pharmaceutical Co., Ltd.

发明人： YASUHARA, Akito ,  SAKAGAMI, Kazunari ,  OHTA, Hiroshi ,  HAYASHI, Masato ,  SHIRASAKI, Yoshihisa ,  YAMAMOTO, Shuji ,  SHIMAZAKI, Youichi ,  ARAKI, Yuko ,  ABE, Kumi ,  SUN, Xiang-Min

IPC分类号： C07D233/90 ,  A61K31/4164 ,  A61K31/4196 ,  A61P25/00 ,  A61P25/04 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P43/00 ,  C07D249/10

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: [Formula 1] 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： 本发明的目的在于提供可用于预防或治疗精神分裂症，阿尔茨海默氏病，认知障碍，痴呆症，焦虑症（例如，精神分裂症， 广泛性焦虑症，恐慌症，强迫症，社交焦虑症，创伤后应激障碍，特定恐怖症，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 抵抗甘氨酸摄取。