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1. 发明申请

US20050119345A1 6-Fluorobicyclo[3.1.0]hexane derivatives 有权
标题翻译： 6-氟二环[3.1.0]己烷衍生物
公开(公告)号：US20050119345A1
公开(公告)日：2005-06-02
申请号：US10500101
申请日：2002-12-26
申请人： Atsuro Nakazato , Shigeyuki Chaki , Kazunari Sakagami , Ryoko Dean , Hiroshi Ohta , Shiho Hirota , Akito Yasuhara
发明人： Atsuro Nakazato , Shigeyuki Chaki , Kazunari Sakagami , Ryoko Dean , Hiroshi Ohta , Shiho Hirota , Akito Yasuhara
IPC分类号： A61K45/00 , A61K31/00 , A61K31/196 , A61K31/198 , A61K31/381 , A61P25/18 , A61P43/00 , C07C229/50 , C07C237/04 , C07C237/26 , C07C255/54 , C07D333/16 , A61K31/195 , C07C229/32
CPC分类号： A61K31/381 , A61K31/00 , A61K31/196 , A61K31/198 , C07C229/50 , C07C237/04 , C07C237/26 , C07C255/54 , C07C2601/08 , C07C2602/18 , C07D333/16
摘要： An antidepressant comprising, as an active ingredient, a compound having an antagonistic effect on group II metabotropic glutamate receptors, as well as a 2-amino-3-alkoxy-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivative of Formula [I]: [wherein R1 and R2, which may be the same or different, each represent a hydroxyl group, a C1-10 alkoxy group, etc.; R3 represents a C1-10 acyl group, a C1-6 alkoxy-C1-6 acyl group, etc.; and R4 and R5, which may be the same or different, each represent a hydrogen atom, a C1-10 alkyl group, etc.] or a pharmaceutically acceptable salt or hydrate thereof.
摘要翻译：作为活性成分的抗抑郁药，其具有对II型代谢型谷氨酸受体具有拮抗作用的化合物，以及2-氨基-3-烷氧基-6-氟 - 双环[3.1.0]己烷-2,6-二式[I]的二羧酸衍生物：其中R 1和R 2可以相同或不同，各自表示羟基，C 1〜 1-10个烷氧基等; R 3表示C 1-10烷基酰基，C 1-6烷氧基-C 1-6烷基，酰基等; 和R 4和R 5可以相同或不同，各自表示氢原子，C 1-10烷基，等]或其药学上可接受的盐或水合物。

2. 发明授权

US07157594B2 6-Fluorobicyclo[3.1.0]hexane derivatives 有权
标题翻译： 6-氟二环[3.1.0]己烷衍生物
公开(公告)号：US07157594B2
公开(公告)日：2007-01-02
申请号：US10500101
申请日：2002-12-26
申请人： Atsuro Nakazato , Shigeyuki Chaki , Kazunari Sakagami , Ryoko Dean , Hiroshi Ohta , Shiho Hirota , Akito Yasuhara
发明人： Atsuro Nakazato , Shigeyuki Chaki , Kazunari Sakagami , Ryoko Dean , Hiroshi Ohta , Shiho Hirota , Akito Yasuhara
IPC分类号： C07C69/74 , C07C61/113
CPC分类号： A61K31/381 , A61K31/00 , A61K31/196 , A61K31/198 , C07C229/50 , C07C237/04 , C07C237/26 , C07C255/54 , C07C2601/08 , C07C2602/18 , C07D333/16
摘要： An antidepressant comprising, as an active ingredient, a compound having an antagonistic effect on group II metabotropic glutamate receptors, as well as a 2-amino-3-alkoxy-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivative of Formula [I]: [wherein R1 and R2, which may be the same or different, each represent a hydroxyl group, a C1-10 alkoxy group, etc.; R3 represents a C1-10 acyl group, a C1-6 alkoxy-C1-6 acyl group, etc.; and R4 and R5, which may be the same or different, each represent a hydrogen atom, a C1-10 alkyl group, etc.] or a pharmaceutically acceptable salt or hydrate thereof.
摘要翻译：一种抗抑郁药，其包含对II族代谢型谷氨酸受体具有拮抗作用的化合物以及2-氨基-3-烷氧基-6-氟 - 双环[3.1.0]己烷-2,6-二式[I]的二羧酸衍生物：其中R 1和R 2可以相同或不同，各自表示羟基，C 1〜 1-10个烷氧基等; R 3表示C 1-10烷基酰基，C 1-6烷氧基-C 1-6烷基，酰基等; 和R 4和R 5可以相同或不同，各自表示氢原子，C 1-10烷基，等]或其药学上可接受的盐或水合物。

3. 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。

4. 发明申请

US20120028982A1 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]十六烷-2,6-二羧酸酯衍生物
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。

5. 发明申请

US20100298561A1 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：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。

6. 发明授权

US08076502B2 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：US08076502B2
公开(公告)日：2011-12-13
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： C07C69/74 , C07C61/12
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. 发明申请

US20090306408A1 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：US20090306408A1
公开(公告)日：2009-12-10
申请号：US12511482
申请日：2009-07-29
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： C07D317/18 , C07C69/753 , C07D305/12
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。

8. 发明授权

US07960579B2 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：US07960579B2
公开(公告)日：2011-06-14
申请号：US10562018
申请日：2004-06-25
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： A61K31/21 , C07C69/74 , C07C61/12
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。

9. 发明授权

US07381746B2 2-Aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivative 失效
标题翻译： 2-氨基二环[3.1.0]己烷-2,6-二羧酸衍生物
公开(公告)号：US07381746B2
公开(公告)日：2008-06-03
申请号：US10562010
申请日：2004-06-25
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： A01N37/12
CPC分类号： C07C323/61 , C07C229/28 , C07C317/48 , C07C2602/40 , C07D333/18
摘要： One object of the present invention is to provide a drug that is effective in treatments for and prevention of psychiatric disorders and in treatments for and prevention of neurological diseases, inhibiting a Group II metabotropic glutamate receptor.The object is solved by a 2-amino-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivative represented by formula [I]: (wherein R1 and R2 are the same or different, and each represents a hydrogen atom, C1-10alkyl group, etc; X represents a hydrogen atom or a fluorine atom; and Y represents an amino group, —SR3, —S(O)nR7, —SCHR3R4, —S(O)nCHR3R4, —NHCHR3R4, —N(CHR3R4)(CHR5R6), —NHCOR3 or —OCOR7), a pharmaceutically acceptable salt thereof, or a hydrate thereof and so on.
摘要翻译：本发明的一个目的是提供一种有效治疗和预防精神疾病以及治疗和预防神经系统疾病，抑制II族代谢型谷氨酸受体的药物。该目的通过由式[I]表示的2-氨基 - 双环[3.1.0]己烷-2,6-二羧酸衍生物来解决：（其中R 1和R 2） / SUP>相同或不同，各自表示氢原子，C 1-10烷基等; X表示氢原子或氟原子; Y表示氨基， - S 3 O 3，-S（O）n R 7，-SCHR 3，R 4，（S） - （O）n - ， - CHR 3 - - - - - - SO 4 - ， - -N（CHR 3 S 4）4（CHR 5 S 6），-NHCOR 其药学上可接受的盐或其水合物等等。

10. 发明申请

US20060142388A1 2-Aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivative 失效
标题翻译： 2-氨基二环[3.1.0]己烷-2,6-二羧酸衍生物
公开(公告)号：US20060142388A1
公开(公告)日：2006-06-29
申请号：US10562010
申请日：2004-06-25
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： A61K31/195 , C07C229/28
CPC分类号： C07C323/61 , C07C229/28 , C07C317/48 , C07C2602/40 , C07D333/18
摘要： One object of the present invention is to provide a drug that is effective in treatments for and prevention of psychiatric disorders and in treatments for and prevention of neurological diseases, inhibiting a Group II metabotropic glutamate receptor. The object is solved by a 2-amino-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivative represented by formula [I]: (wherein R1 and R2 are the same or different, and each represents a hydrogen atom, C1-10alkyl group, etc; X represents a hydrogen atom or a fluorine atom; and Y represents an amino group, —SR3, —S(O)nR7, —SCHR3R4, —S(O)nCHR3R4, —NHCHR3R4, —N(CHR3R4)(CHR5R6), —NHCOR3 or —OCOR7), a pharmaceutically acceptable salt thereof, or a hydrate thereof and so on.
摘要翻译：本发明的一个目的是提供一种有效治疗和预防精神疾病以及治疗和预防神经系统疾病，抑制II族代谢型谷氨酸受体的药物。该目的通过由式[I]表示的2-氨基 - 双环[3.1.0]己烷-2,6-二羧酸衍生物来解决：（其中R 1和R 2） / SUP>相同或不同，各自表示氢原子，C 1-10烷基等; X表示氢原子或氟原子; Y表示氨基， - S 3 O 3，-S（O）n R 7，-SCHR 3，R 4，（S） - （O）n - ， - CHR 3 - - - - - - SO 4 - ， - -N（CHR 3 S 4）4（CHR 5 S 6），-NHCOR 其药学上可接受的盐或其水合物等等。

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