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1. 发明专利

IL235897A Prodrug of fluorine-containing amino acid 未知
公开(公告)号：IL235897A
公开(公告)日：2019-09-26
申请号：IL23589714
申请日：2014-11-25
申请人： TAISHO PHARMA CO LTD , TAKASHI HASHIHAYATA , NORIKAZU OTAKE , NAOKI MIYAKOSHI , KAZUNARI SAKAGAMI
发明人： TAKASHI HASHIHAYATA , NORIKAZU OTAKE , NAOKI MIYAKOSHI , KAZUNARI SAKAGAMI
IPC分类号： A61K31/265 , A61K31/221 , A61P25/00
摘要： Provided are a fluorine-containing amino acid prodrug represented by general formula (I) that makes a fluorine-containing amino acid which is a group 2 metabotropic glutamate receptor agonist into a prodrug, or a pharmaceutically acceptable salt thereof. More specifically, provided is a prodrug that increases the in vivo exposure and enhances the oral absorbability and other mucosal absorbability of a parent compound that acts on group 2 metabotropic glutamate receptors as an agent for the treatment or prevention of diseases in which group 2 metabotropic glutamate receptors are said to be involved, such as: schizophrenia, anxiety disorder and its related diseases, depression, bipolar disorder, epilepsy, developmental disorders, sleep disorders, and other neuropsychiatric diseases; and drug dependence, cognitive disorders, Alzheimer's disease, Huntington's chorea, Parkinson's disease, movement disorders associated with muscular rigidity, cerebral ischemia, cerebral insufficiency, spinal cord disorders, cephalopathy, and other neurological diseases.

2. 发明专利

IL235897D0 Prodrug of fluorine-containing amino acid 未知
公开(公告)号：IL235897D0
公开(公告)日：2015-02-01
申请号：IL23589714
申请日：2014-11-25
申请人： TAISHO PHARMA CO LTD , TAKASHI HASHIHYATA , NORIKAZU OTAKE , NAOKI MIYAKOSHI , KAZUNARI SAKAGAMI
IPC分类号： C07C20060101
摘要： Provided are a fluorine-containing amino acid prodrug represented by general formula (I) that makes a fluorine-containing amino acid which is a group 2 metabotropic glutamate receptor agonist into a prodrug, or a pharmaceutically acceptable salt thereof. More specifically, provided is a prodrug that increases the in vivo exposure and enhances the oral absorbability and other mucosal absorbability of a parent compound that acts on group 2 metabotropic glutamate receptors as an agent for the treatment or prevention of diseases in which group 2 metabotropic glutamate receptors are said to be involved, such as: schizophrenia, anxiety disorder and its related diseases, depression, bipolar disorder, epilepsy, developmental disorders, sleep disorders, and other neuropsychiatric diseases; and drug dependence, cognitive disorders, Alzheimer's disease, Huntington's chorea, Parkinson's disease, movement disorders associated with muscular rigidity, cerebral ischemia, cerebral insufficiency, spinal cord disorders, cephalopathy, and other neurological diseases.

3. 发明授权

US08642626B2 Ethinyl-pyrazole derivative 失效
标题翻译：乙烯基 - 吡唑衍生物
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。

4. 发明申请

US20130137865A1 HETEROARYL-PYRAZOLE DERIVATIVE 审中-公开
标题翻译：异丙基吡唑衍生物
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。

5. 发明授权

US08258133B2 2-amino-bicyclo[3.1.0]hexane-2, 6-dicarboxylic ester derivative 失效
标题翻译： 2-氨基 - 双环[3.1.0]己烷-2,6-二羧酸酯衍生物
公开(公告)号：US08258133B2
公开(公告)日：2012-09-04
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： A61K31/535
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。

6. 发明申请

US20120004232A1 2-AMINO-BICYCLO(3.1.0) HEXANE-2, 6-DICARBOXYLIC ESTER DERIVATIVE 失效
标题翻译： 2-氨基双酚（3.1.0）HEXANE-2，6-二甲氧基硅烷衍生物
公开(公告)号：US20120004232A1
公开(公告)日：2012-01-05
申请号：US13227942
申请日：2011-09-08
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： A61K31/535 , A61K31/27 , A61K31/21 , A61K31/265 , C07C61/13 , C07D265/30 , C07D317/08 , C07D307/87 , C07C69/96 , C07C271/24 , A61K31/365 , A61K31/195
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 administrationA 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，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。

7. 发明授权

US06500958B2 Carboxylic acid derivatives and process for producing the same 失效
标题翻译：羧酸衍生物及其制备方法
公开(公告)号：US06500958B2
公开(公告)日：2002-12-31
申请号：US10176528
申请日：2002-06-24
申请人： Atsuro Nakazato , Toshihito Kumagai , Kazunari Sakagami , Kazuyuki Tomisawa
发明人： Atsuro Nakazato , Toshihito Kumagai , Kazunari Sakagami , Kazuyuki Tomisawa
IPC分类号： C07D23500
CPC分类号： C07D235/02 , C07C62/26 , C07C65/40 , C07C69/757 , C07C2602/18 , C07D339/06 , C07D495/10
摘要： The present invention relates to compounds which are useful for efficient synthesis of 2-amino-4-oxobicyclo[3.1.0]hexane-2,6-dicarboxylic acids. The compounds according to the present invention comprise 2-oxobicyclo[3.1.0]hexane-6-carboxylic acid derivatives represented by the formula as follows: [wherein, R1 represents a hydrogen atom, a C1-C6 alkyl group, a C3-C6 cycloalkyl group, a C3-C6 cycloalkyl C1-C6 alkyl group, an aryl group, an aryl C1-C6 alkyl group, a C1-C6 alkoxy C1-C6 alkyl group, a C1-C6 hydroxyalkyl group, a C1-C6 alkylthio C1-C6 alkyl group, a C1-C6 mercaptoalkyl group, a tetrahydrofuranyl group, or a tetrahydropyranyl group; R2 and R3 are identical or different, and each represents a C1-C6 alkyl group, a C3-C6 cycloalkyl group, a C3-C6 cycloalkyl C1-C6 alkyl group, an aryl group, or an aryl C1-C6 alkyl group, or alternatively, R2 and R3 together represent —(CH2)n— (wherein n represents 2 or 3); and Y1 and Y2 are identical or different, and each represents a sulfur atom, an oxygen atom, or a nitrogen atom].
摘要翻译：本发明涉及可用于高效合成2-氨基-4-氧代双环[3.1.0]己烷-2,6-二羧酸的化合物。根据本发明的化合物包含2-氧代双环[3.1.0] 由下式表示的己烷-6-羧酸衍生物：[其中，R1表示氢原子，C1-C6烷基，C3-C6环烷基，C3-C6环烷基C1-C6烷基，芳基基团，芳基C1-C6烷基，C1-C6烷氧基C1-C6烷基，C1-C6羟基烷基，C1-C6烷硫基C1-C6烷基，C1-C6巯基烷基，四氢呋喃基，或四氢吡喃基; R2和R3相同或不同，各自表示C1-C6烷基，C3-C6环烷基，C3-C6环烷基C1-C6烷基，芳基或芳基C1-C6烷基，或或者，R2和R3一起表示 - （CH 2）n - （其中n表示2或3）; Y 1和Y 2相同或不同，各自表示硫原子，氧原子或氮原子]。

8. 发明授权

US06479674B1 Carboxylic acid derivatives and process for producing same 失效
标题翻译：羧酸衍生物及其制备方法
公开(公告)号：US06479674B1
公开(公告)日：2002-11-12
申请号：US09937212
申请日：2001-09-24
申请人： Atsuro Nakazato , Toshihito Kumagai , Kazunari Sakagami , Kazuyuki Tomisawa
发明人： Atsuro Nakazato , Toshihito Kumagai , Kazunari Sakagami , Kazuyuki Tomisawa
IPC分类号： C07D31500
CPC分类号： C07D235/02 , C07C62/26 , C07C65/40 , C07C69/757 , C07C2602/18 , C07D339/06 , C07D495/10
摘要： The present invention relates to compounds which are useful for efficient synthesis of 2-amino-4-oxobicyclo[3.1.0]hexane-2,6-dicarboxylic acids. The compounds according to the present invention comprise 2-oxobicyclo[3.1.0]hexane-6-carboxylic acid derivatives represented by the formula as follows: [wherein, R1 represents a hydrogen atom, a C1-C6 alkyl group, a C3-C6 cycloalkyl group, a C3-C6 cycloalkyl C1-C6 alkyl group, an aryl group, an aryl C1-C6 alkyl group, a C1-C6 alkoxy C1-C6 alkyl group, a C1-C6 hydroxyalkyl group, a C1-C6 alkylthio C1-C6 alkyl group, a C1-C6 mercaptoalkyl group, a tetrahydrofuranyl group, or a tetrahydropyranyl group; R2 and R3 are identical or different, and each represents a C1-C6 alkyl group, a C3-C6 cycloalkyl group, a C3-C6 cycloalkyl C1-C6 alkyl group, an aryl group, or an aryl C1-C6 alkyl group, or alternatively, R2 and R3 together represent —(CH2)n— (wherein n represents 2 or 3); and Y1 and Y2 are identical or different, and each represents a sulfur atom, an oxygen atom, or a nitrogen atom].
摘要翻译：本发明涉及可用于高效合成2-氨基-4-氧代双环[3.1.0]己烷-2,6-二羧酸的化合物。根据本发明的化合物包含2-氧代双环[3.1.0] 由下式表示的己烷-6-羧酸衍生物：[其中，R1表示氢原子，C1-C6烷基，C3-C6环烷基，C3-C6环烷基C1-C6烷基，芳基基团，芳基C1-C6烷基，C1-C6烷氧基C1-C6烷基，C1-C6羟基烷基，C1-C6烷硫基C1-C6烷基，C1-C6巯基烷基，四氢呋喃基，或四氢吡喃基; R2和R3相同或不同，各自表示C1-C6烷基，C3-C6环烷基，C3-C6环烷基C1-C6烷基，芳基或芳基C1-C6烷基，或或者，R2和R3一起表示 - （CH 2）n - （其中n表示2或3）; Y 1和Y 2相同或不同，各自表示硫原子，氧原子或氮原子]。

9. 发明申请

US20130123500A1 ETHINYL-PYRAZOLE DERIVATIVE 失效
标题翻译：乙烯基吡唑衍生物
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。

10. 发明申请

US20120116095A1 GLYCINE TRANSPORTER INHIBITORS 审中-公开
标题翻译：甘油运输车辆抑制剂
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。

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